rexresearch.com
rexresearch1.com
Shilajit Patents : Purification & Therapeutics
Purification :
METHOD FOR PRODUCING PROPYLENE GLYCOL EXTRACT OF SHILAJITFIELD: technological processes.SUBSTANCE: invention relates to a method for processing natural shilajit-containing feedstock, namely to a method for producing a propylene glycol extract of shilajit. Method for producing a propylene glycol extract of shilajit comprising extracting a purified shilajit-containing feedstock with an extractant being propylene glycol or a mixture of propylene glycol and water, under certain conditions, followed by filtration of the extract.EFFECT: described method provides an extract with a high extractable substance content and increased resistance to microbiological contamination.
RU2668517
The invention relates to methods for processing natural mumiyo-containing raw materials, specifically, methods for obtaining propylene glycol extracts of mumiyo - popular natural components of products in the cosmetics and perfume industry, household chemicals and detergents.
Shilajit is currently used in medicine both in its native form and in the form of various dosage forms (ointments, tablets, suppositories, etc.
) As a rule, mumiyo-containing raw materials contain up to 50% mumiyo in resinous form. To isolate mumiyo from natural raw materials, as a rule, multi-stage aqueous extraction is used, followed by filtering, drying and obtaining dry extracts, which are used in dosage forms
There is a known method for obtaining aqueous extracts of mumiyo, which consists in preliminary grinding of mumiyo-containing rock to a particle size of no more than 1 mm, extraction with distilled water, repeated filtration and subsequent evaporation of the filtrate to obtain an extract containing no more than 3.5% water, which is then tableted and packaged ( patent RU 2001618 A61K 35/00, publ.30.10.1993 G. )
There is also a known method for producing mumiyo extracts from mumiyo-containing raw materials by countercurrent dissolution in water until the solution density reaches 1.05-1.075 g/cm<sup>3</sup>, filtration and evaporation of the resulting solution, followed by tabletting (patent RU 2102989, A61K 35/00 publ.27.01.1998 G.).
There is also a known method for obtaining mumiyo extracts by extracting crushed raw materials with distilled water in a rotary pulsation extractor followed by removing water in a rotary film dryer (patent RU 2114626 A61K 35/12 publ.10.07.1998 G.).
There is also a known method for producing a bioactive extract based on mummies-containing raw materials.
The method involves the following stages: preliminary soaking in distilled water, ultrasonic treatment of the solution, settling and separation of the undissolved fraction by decantation, ultrafiltration, drying in a sublimation unit to a content of at least 95% of the mass fraction of dry substances, disinfection of the resulting product with mercury bactericidal lamps and vacuum packaging of the product (patent RU 2164411 A61K 35/00 publ. 27.03.2001).
However, the solid state of mumiyo extracts limits the possibility of using them in modern products of household chemicals and the cosmetic and perfume industry with low water content, and also increases the duration of the technological process for manufacturing cosmetic and perfume products due to the need to pre-dissolve the solid extracts in the desired solvent, filter the resulting solution, which also leads to higher prices for target products.
In addition, not every company has such an opportunity. Due to the low microbiological purity and short shelf life of aqueous extracts of mumiyo, their use in the production of cosmetics and perfumes is also greatly limited.
It is important to note that aqueous-alcoholic extracts of natural raw materials, previously widely used, are now extremely rarely used in the formulations of cosmetics and perfumes due to the fact that they belong to the class of flammable liquids and require special conditions for transportation, storage and use.
Moreover, after the introduction of excise taxes on alcohol-containing solutions, including aqueous-alcoholic extracts, the production of the latter in Russia sharply increased in price. It should be noted that there is another problem with the use of aqueous-alcoholic extracts, such as their exfoliating effect in cosmetic and hygienic detergents, which is especially noticeable in formulations containing pearl-forming and thickening components [M.Yu. Pletnev. Cosmetic and hygienic detergents. M.: “Chemistry”, 1990]. An alternative to aqueous-alcoholic extracts could be aqueous-glycerol extracts, however, due to the high viscosity of glycerol and low diffusion coefficients, the rate of mass transfer processes and the degree of extraction of active substances are extremely low. In addition, the high viscosity of aqueous glycerin extracts creates technological problems in their production and use in the formulation of cosmetic and hygiene products.
The chemical structure closest to glycerin is propylene glycol, which still has bactericidal activity.
In cosmetics, propylene glycol is used as a humectant, but having a lower viscosity (density comparable to water), it is also an excellent enhancer - a substance that helps active substances from cosmetic products easily penetrate the protective layer of the skin. All this makes propylene glycol extracts of mumiyo very attractive for use in household chemical products
The objective of the invention is to develop a method for producing liquid extracts of mumiyo for use in cosmetics, perfumes and household chemicals.
The technical result is propylene glycol extracts of mumiyo, maintaining microbiological purity during the guaranteed shelf life (up to 12 months) with a yield of extracted substances of at least 60%.
The technical result is achieved by the proposed method for producing propylene glycol extracts of mumiyo, according to which the extraction of purified mumiyo-containing raw materials is carried out with propylene glycol or a mixture of propylene glycol with water at a mass ratio of mumiyo-containing raw materials: extractant = 1: (10-20) for 2-4 hours at a stirring speed of no more than 40 rpm and temperature not higher than 35°C, followed by filtration of the extract.
The mixture of propylene glycol and water contains no more than 75 wt. % water.
When the water content in the extractant is more than 50 wt. % the preservative Microker IT is introduced into the extract in an amount of 0.01-0.05% by weight of the extract (a special case of the method implementation).
For extraction, mummy-containing raw materials were used according to TU 9377-003-21454432-14 in the form of a thick dark brown resin with a moisture content of 20%, propylene glycol according to TU 6-09-2434-81 or according to TU 2422-059-05766801-97.
Microker IT (a mixture of methylisothiazolinone and methylchloroisothiazolinone) - preservative manufactured by Thor GmbH, Germany.
The extract is filtered by known means, for example, through a paper or fabric filter.
Stirring at speeds above 40 rpm leads to the fact that some of the impurities contained in the feedstock are transferred into the extract in the form of an emulsion, contaminating the target product; in addition, separation of the emulsion requires considerable time, which is technologically and economically not feasible.
When extraction takes less than 2 hours, a high degree of extraction of extracted substances is not achieved; more than 4 hours is not economically feasible.
Increasing the temperature above the specified parameters is not recommended, since it leads to a decrease in the yield of the target product due to hydration and hydrolysis of the useful components of mumiyo at higher temperatures.
The ratio of the initial mummy-containing raw material and extractant below G. 10 is technologically impractical, because part of the extracted product is subsequently separated from the extract.
The ratio of the original mumiyo-containing raw material and extractant above 1:20 is not economically justified due to a decrease in the concentration of extracted mumiyo components, which leads to the need to introduce more extract into the formulations of cosmetics and household chemical products and, accordingly, to an increase in the cost of cosmetic products.
It is known that the demand for extracts is determined by two factors: biological value and resistance to microbiological contamination.
The biological value of extracts of plant raw materials is determined by the quantitative content of biologically active substances extracted from mummies-containing raw materials, in this case it will be determined by the amount of non-removable (dry) residue from the propylene glycol extract, determined in accordance with the Technical Specifications TU 9154-010-02700055-2002 letter A with amendments 1,2,3,4.5.
In terms of microbiological purity, extracts of plant raw materials must meet the sanitary requirements of SanPin 1.2.681-97; MUK 4.2.801-99, GF XII, part 1, section.
32 (OFS 42-0067-07).
Determination of the microbiological purity of the resulting extract was carried out in accordance with the Methodological Instructions MUK 4.2.801-99 “Methods of microbiological control of perfume and cosmetic products”.
The inventive method is illustrated by the following examples:
Example 1.
50 g of mummies-containing raw materials are loaded into a glass extractor equipped with a reflux condenser, a mechanical stirrer and a thermometer and 1000 g of propylene glycol are added.
The mixture is slowly stirred for 4 hours, periodically turning on the stirrer (rotation speed no more than 40 rpm) at a temperature not higher than 35°C. After cooling to room temperature, filter the solution using a paper or fabric filter.
The resulting dark brown extract is analyzed for standard quality indicators and microbiological purity.
The results of the analysis are presented in tables 1 and 2.
The yield of extractable substances (61.0%) is determined by the amount of non-removable (dry) residue.
Example 2.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of propylene glycol are added.
Next, the process is carried out similarly to example 1. The yield of extracted substances is 66.75%.
Example 3.
50 g of mummies-containing raw materials are loaded into the reaction container and 1000 g of extractant containing 950 g (95%) propylene glycol and 50 g (5%) distilled water are added. Next, the process is carried out similarly to example 1. The yield of extracted substances is 71.5%.
Example 4.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of extractant containing 475 g (95%) propylene glycol and 25 g (5%) distilled water are added. Next, the process is carried out similarly to example 1. The yield of extracted substances is 72.0%.
Example 5.
50 g of mummies-containing raw materials are loaded into the reaction container and 1000 g of extractant containing 750 g (75%) propylene glycol and 250 g (25%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 3 hours. The yield of extracted substances is 83.0%.
Example 6.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of extractant containing 375 g (75%) propylene glycol and 125 g (25%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 3 hours. The yield of extracted substances is 81.0%.
Example 7.
50 g of mummies-containing raw materials are loaded into the reaction container and 1000 g of extractant containing 500 g (50%) propylene glycol and 500 g (50%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 3 hours. The preservative Microker IT is added to the finished extract in an amount of 0.01% by weight of the extract. The yield of extracted substances is 97.25%.
Example 8.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of extractant containing 250 g (50%) propylene glycol and 250 g (50%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 3 hours. The preservative Microker IT is added to the finished extract in an amount of 0.01% by weight of the extract. The yield of extracted substances is 96.75%.
Example 9.
50 g of mummies-containing raw materials are loaded into the reaction container and 1000 g of extractant containing 250 g (25%) propylene glycol and 750 g (75%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 98.75%.
Example 10.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of extractant containing 125 g (25%) propylene glycol and 375 g (75%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 98.5%.
Example 11.
50 g of mummies-containing raw materials are loaded into the reaction container and 1000 g of extractant containing 50 g (5%) propylene glycol and 950 g (95%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 99.25%.
Example 12.
50 g of mummies-containing raw materials are loaded into the reaction container and 500 g of extractant containing 25 g (5%) propylene glycol and 475 g (95%) distilled water are added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 98.75%.
Example 13.
50 g of mummies-containing raw material is loaded into the reaction container and 1000 g of extractant - distilled water - is added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 99.75%.
Example 14.
50 g of mummies-containing raw material is loaded into the reaction container and 500 g of extractant - distilled water - is added. Next, the process is carried out similarly to example 1. Extraction time - 2 hours. The preservative Microker IT is added to the finished extract in an amount of 0.05% by weight of the extract. The yield of extracted substances is 99.5%.
The extracts obtained in accordance with examples 1-14 are transparent liquids of dark brown color, the quality indicators of which, given in table 1, comply with the requirements of TU 9154-010-02700055-2002 “Propylene glycol extracts, letter A” with amendments 1, 2,3,5,5 (for aqueous propylene glycol extracts) and TU 9154-014-12967730-2006 “Aqueous extracts of plant raw materials, letter A” (for aqueous extracts).
As follows from the data in Table 1, all extracts obtained (examples 1-14) have a yield of extractable substances of at least 60% (61.0 - 99.75).
The microbiological purity (Table 2) of water-propylene glycol extracts with a water content of no more than 50%, both with the use of a preservative in an amount of 0.01% and without the use of a preservative, is maintained during the warranty period - 12 months (examples 1-8).
With a further increase in the water content in the extracts, their microbiological purity is maintained for 12 months only if the preservative content is at least 0.05% (examples 9, 10). In aqueous extracts (examples 13,14) without a preservative, microbiological purity is maintained for no more than 5 days, with the use of 0.05% preservative - no more than 30 days. Thus, the declared technical result is achieved in cases where the extractant is propylene glycol or a mixture of propylene glycol and water containing no more than 75 mass% water.
The inventive method for producing propylene glycol extracts of mumiyo ensures the production of extracts with a high content of extractable substances (up to 98%) with increased resistance to microbiological contamination (up to 12 months from the date of manufacture) while maintaining organoleptic and physico-chemical quality indicators that comply with current regulatory documentation.
Note: * - preservative Microker IT is added in the amount of 0.01% by weight of the extract
Mineral Pitch Resin manufactured under a safe and low temperature procedure.
US2013280291
The invention claims a manufacturing method of the Mineral Pitch Resin also known as shilajit, silajit, mumije, mumie, momie, moomie, mumio, momia, brashgun, etc., and product variations thereof. The method produces genuine Mineral Pitch Resin, under a predetermined controlled method. Such method results into the Resin, which is verifiably free from harmful contaminants and is safe for humans to consume as a healing, tonifying and adaptogenic substance. Such resin passes authenticity tests, is of consistent quality and has preserved heat sensitive biologically active substances innate to raw material used to manufacture the Mineral Pitch.
BACKGROUND OF THE INVENTION
This inventions pertains to manufacturing of a premium and genuine mineral pitch resin (also known as shilajit, silajit, salajeet, mumije, mumie, momie, moomie,mumio, momia, brashgun, etc.) and formulations made with such resin, which itself is a potent medicinal, adaptogenic, nutraceutical, cosmetic and nutritional substance.
Mineral Pitch, known by multiple names in different cultures (shilajit, silajit, salajeet, mumije,mumie, momie, moomie,mumio, momia, brashgun, etc.) is one of the most potent adaptogenic stimulators known to mankind. It has been successfully used for thousands of years to by humans and animals to treat diseases, injuries and address nutritional deficiencies. Modern medical and nutritional science has confirmed and identified multiple health related benefits of the Resin.
The most common, but not only, known origin of Mineral Pitch is located in the mountains of various regions in Asia, Caucasus, Europe, Antarctica, etc. Traditionally, prior to advent of advanced pharmaceutical and chemical science, Mineral Pitch was primitively processed by intense methods of purification and heating.
The problems are that, both undue purification and/or excessive heating take the Mineral Pitch out of its traditional environment and often render it somewhat unsafe or less efficient. Purification can cause Mineral Pitch to be contaminated with harmful impurities. Excessive heating, usually over 39 degrees Celsius, will destroy multiple, valuable compounds such as enzymes, vitamins, and microflora indigenous to the Mineral Pitch.
Another substantial problem is counterfeit Shilajit imitation products by multiple manufacturers. Such imitation products usually come as powders and don't have most benefits of genuine Mineral Pitch Resins.
Popularity of the holistic, superfood and natural medicinal substances makes consistent low temperature and non-toxic, non-harsh purification process in the manufacturing of Mineral Pitch highly relevant. Absence of a standardized and precisely controlled manufacturing method for sourcing, collection, transportation, purification, concentration and packaging of Mineral Pitch is limiting for mass manufacturing of a safe, potent and sufficient market supply of a “live” Mineral Pitch resin paste.
This patent application solves the challenge. The novelty is stipulated by manufacturing Mineral Pitch resin in a production form and way which is consistently genuine, pure, safe, and temperature-controlled throughout the manufacturing cycle. This renders the Mineral Pitch to be qualified as “raw-live” and of a supreme quality. The invention also overcomes the challenge of safe and consistent mass manufacturing of this live nutriceutical. The product is a resin/paste form and not powder.
BRIEF SUMMARY/DESCRIPTION OF THE INVENTION
The invention deals with full cycle of manufacturing the premium quality Mineral Pitch Resin and formulations made with it in a way which results in superior quality and safety from microbiological, mineral and radiological contaminants in a controlled environment.
The Invention covers all the stages of the sourcing, logistics and manufacturing process of genuine Mineral Pitch Resin (also known as shilajit, silajit, mumije,mumie, momie, moomie,mumio, momia, brashgun, etc.) as well as manufacturing of said Resin with botanicals and various medicinal or cosmetic ingredients mixed into it. In contrast to traditional methods it implies a controlled and standardized procedure, which results resin of superior quality, safe for end consumers with intact heat sensitive enzymes and biologically active substances. In contrast to multiple imitation products the invention produces the Resin, which is safe to consume and has an effect closest to the pure raw material in nature with the innate biologically active substances. The said resin is not treated with hot organic solvents, such as ethanol or methanol, is not artificially oxygenated or acidified to boost any of the fractions of the resin's fractions. The resulting product, which is not a powder, with substantial glycine content, which is not fortified with fulvic acid or any other fillers and naturally passes authenticity tests for mineral pitch resins.
DETAILED DESCRIPTION OF THE INVENTION
Safe temperature regimes and grades consistently used: under 39 C (102.2 Fahrenheit)—1<st >grade premium quality, under 48 C (118.4 Fahrenheit)—2<nd >grade quality, higher temperatures—3<rd >grade quality.
Major tools and utensils: transportation containers supplied with UV light and temperature control or as alternative temperature controlled containers, clean rooms, clean room dehumidifiers, sterile vessels equipped with mixers and temperature control with or without dehumidifiers/demoisturizers, UV lamps or other source of light, sound or electro-magnetic disinfection, cutting—shaving—grating utensils, opaque transportation containers, biophotonic glass or apothecary jars, food grade alcohol or other food grade disinfectant.
Stages: 1. preparation 2. identification 3. collection 4. transportation 5. purification 6. concentration/demoisturization 7. packaging 8. transportation 9. repackaging
Methodology
All stages, with the partial exception of (8) transportation, take place at a constantly monitored and maintained environment, within a consistent temperature range of under 39 degrees Celsius for the first grade quality of product during the stages of manufacturing and under 48 degrees Celsius for the second grade quality of product and higher temperatures for the third grade quality.
Upon initiating the preparation cycle, the manufacturer is required to prepare the clean room facility, equipped with UV sterilization light (or other source of light, sound or any other form of electro-magnetic disinfection), dehumidifiers, temperature controlled increased area mixing or still vessels (alternatively equipped with dehumidifiers/demoisturizers), purified or sterilized (treated) water or liquid herbal extraction, transportation containers equipped with features of UV or any other form of disinfection or any other temperature control. Once the preparation cycle is complete, one may proceed to identification and collection of the raw material.
Once the raw material is visually and/or chemically identified as the desired Mineral Pitch, a person collecting the material cleans (cuts, grates or shaves off) off the external layers of the identified Mineral Pitch. Next the collected material is briefly washed off with food grade alcohol and immediately placed in the thermo-controlled containers with or without UV sterilization light (or any other source of sterilization) activated. An alternative would be a container without a sterilization light (with or without any other source of sterilization). Raw materials from different types of containers are not combined until a laboratory analysis confirms processed materials for safety and uniformity. At the stage of collection the natural (weather) and controlled environment are to be monitored to stay under 39C or 48C. If the temperature exceeds 39C the raw materials for the 1<st >quality grade are not collected, if the temperature exceeds 48C the raw materials for the second quality grade are not collected. Any raw material collected under ambient temperatures of over 48C are to be placed n batches for the 3<rd >degree quality.
Once collected into the temperature controlled containers equipped with a source of disinfection, or alternatively without one, the raw material is transported into the clean room facility for processing. Once delivered into the facility all operations take place in the clean rooms under exposure to UV light (or any other mentioned above source of disinfection). Alternatively the process can take place in the clean rooms without a UV light source of disinfection. The raw initially cleaned material is taken out from the containers and is once again very briefly washed/wiped with food grade alcohol. Next the material of different temperature grades is separated and dissolved in sterile or other form of water or liquid (deionized, purified, mineralized, geographically sourced, magnetically treated, structured, informationally programmed, etc.). The solution is filtered multiple times through filters in order to rid off impurities, sediment, sand, etc. The process of adding water and filtration may be repeated up to 50 times with various types of filters, ensuring elimination of particles as small as several micrometers or several hundred nanometers. Once the filtration is complete the filtrate may or may not be mixed with other desired herbal extracts, minerals or other substances which would be beneficial to the efficacy of the final product/Mineral Pitch formulation. All of the procedures mentioned in this paragraph take place within temperature-controlled environments of under 39C for the 1<st >grade quality and under 48 degrees C. for the second grade quality. This process may take place in vacuum, under pressure or exposure to different sound or electromagnetic waves.
Next the filtrate is transferred to the temperature controlled vessel equipped, or not, with an inbuilt dehumidification system and a mixer or stirrer. The alternative to the inbuilt dehumidification/demoisturization system can be a dehumidification system as a part of the clean room environment. The filtrate is mixed and dehumidified/demoisturized, which turns it into a resin/paste form. Generally the resin will have a humidity level under but not limited to 20%. All of the procedures mentioned in this paragraph take place within a clean room, temperature controlled environment of under 39C for the 1<st >grade quality and under 48 degrees C. for the second grade quality and above for the third grade quality...
Process for preparing purified shilajit composition from native shilajit
US2003039662
A purified shilajit composition is provided herein from native shilajit. The composition has an abundance of bioactive components, particularly, at least 0.3%, preferably 0.4-1%, by weight, oxygenated dibenzo-alpha-pyrones and at least 60%, preferably 65-70%, by weight of fulvic acids of low-to-medium molecular weight ({overscore (Mn of 700-2000) with an E4/E6 ratio of 8-10 at lambd465-665 nm, and whose 2% aqueous solution has a pH of >=7. Personal care, pharmaceutical and nutritional use formulations of the purified shilajit composition also are described.
1. Field of the Invention
This invention relates to shilajit compositions, and particularly to purified shilajit compositions obtained from native shilajit, which compositions have an abundance of defined bio-active constituents and are devoid of toxic components, and to personal care, pharmaceutical and nutritional use formulations thereof.
2. Description of the Prior Art
Rejuvenating changes in one's body can be initiated and effected by nutrition, herbs and herbo-minerals. Aging and its associated problems are a degenerative disease, which, however, is preventable and treatable. The aging process involves the action of highly reactive free radicals, produced systemically, which interact with other cellular compounds and produce oxidative damages and eventually kills cells and tissues and impairs the immune function of the organism. Such free radical damage accumulates and increases with age, creating degenerative diseases, such as Alzheimer's, cardiovascular, arthritis, cancer and over a hundred other diseases.
DNA, the cellular building block of the body, is very sensitive to oxidative stress. Although repairs to damaged DNA are constantly being made, the cell's mechanism cannot keep up with the number of mutations that occur in the organism, particularly in the aged. Mitochondria, the part of the cell that is responsible for producing cellular energy, has its own DNA, but it does not have a repair mechanism to give it protection against free radical induced damage. The mutation of mitochondrial DNA therefore produces a greater adverse effect than DNA mutation elsewhere in the system. Researchers in recent years have shown that certain individual natural supplements, such as omega-3-polyunsaturated fatty acids and metabolites thereof, oxygenated dibenzo-[alpha]-pyrones, and their O-acylesters, as well as hydroxyacetophenones and ([alpha]-lipoic acids, can protect against oxidative damage to mitochondrial DNA.
Accordingly, it is desired in this invention to provide a purified composition of bioactive agents to protect the body against free radical damage.
Native shilajit is a blackish-brown exudation, of variable consistencies, obtained from steep rocks of different formations found in the Himalayas at altitudes between 1000-5000 m, from Arunachal Pradesh in the East, to Kashmir in the West. Shilajit also is found in other mountain ranges of the world, e.g. Afganisthan (Hindukush, Badakh-Shan), Australia (Northern Pollock Ranges), and in the former USSR (Tien-Shan, Pamir, Caucasus, Ural). Native shilajit is believed to arrest aging and also produce rejuvenation, two important attributes of an Ayurvedic rasayan medicine. Considerable controversy, however, has existed in the literature concerning the nature and chemical character of shilajit. It has been variously described as a bitumen (asphalt), a mineral resin, a plant fossil, a substance of mixed plant and animal origin, or an inorganic substance.
Generally, native shilajit contains two classes of organic compounds, namely, (a) humic substances and (b) non-humic organic metabolites. Humic substances are the the major organic constituents of native shilajit, present in an amount of about 80-85% therein, and have molecular weights ranging from several thousands for humic acids (HAs), and up to several million for polymeric humins (HMs), to only a few hundred for its fulvic acid (FAs) component. These substances also are found in soils and sediments distributed over the earth's surface, occurring in almost all terrestrial and aquatic environments. Humic substances are produced by the interactions of plants, algae, and mosses (bryophtes), with microorganisms, by a process known as humification. Humification of latex- and resin-bearing plants is primarily responsible for the production of the water-soluble humic substances.
The non-humic substances of shilajit are low molecular weight (Mw) compounds of plant and microbial origin, occurring in and around shilajit bearing rocks. The remaining non-humic organic masses in shilajit comprise a mixture of low Mw aromatic, aliphatic alicyclic, and heterocyclic (N- and S-containing) compounds. Of particular biological interest are low Mw oxygenated dibenzo-[alpha]-pyrones (DBP) and hydroxyacetophenones (HAPs).
The biological effects of shilajit are believed to be due to the two distinct classes of bioactive compounds: (i) DBPs, both mono- and bis-compounds thereof, in free and metal-ion conjugated forms; and (ii) fulvic acids (FAs) from shilajit-humic substances, which function as a carrier for the bioactive DBPs. However, native shilajit rhizospheres from different origins suffer from the presence of only small amounts of (i) and (ii) therein. Large amounts of contaminants, e.g. high Mw polymeric quinones, humins (HMs), and inorganic substances are present. Furthermore, shilajit rhizospheres are always heavily infested at its periphery with a large array of microorganisms, some of which are producers of mycotoxins. Thus, the potential risk of ingesting shilajit in its native form, or only after rudimentary purification, with no control or defined standards, is quite apparent.
The prior art in this field is described in the "Information Disclosure Statement", attached hereto. Other cumulative prior art is exemplified by the following references:
(1) S. Ghosal et al, Phytotherapy Res., 1991, 5, 211.
(2) S. Bhaumik, S. Chartopadhyay and S. Ghosal, Phytotherapy Res., 1993, 7, 425.
(3) Y. C. Kong et al, Int. J. Crude Drug Res., 1987, 25, 179.
(4) S. Ghosal, S. K. Singh and R. S. Srivastava, J. Chem. Res., 1988, 196.
(5) M. V. S. Sultanbawa, Tetrahedron, 1980, 36, 1465.
(6) S. B. Scharya et al, Indian J. Exp. Biol., 1988, 26, 775.
(7) S. Ghosal et al, Phytotherapy Res., 1989, 6, 249.
Accordingly, it is an object of this invention to provide a purified shilajit composition which is standardized with respect to its bioactive chemical components, and which is devoid of toxic materials therein.
A particular object of this invention is to provide purified shilajit compositions having an abundance of bioacbve components, particularly oxygenated dibenzo-[alpha]-pyrones (DBPs), and carrier molecules, which are low-to-medium molecular weight fulvic acids (FAs) present in abundant amouts in the composition.
Another object herein is to provide personal care, pharmaceutical and nutritional use formulations containing a predetermined amount of said purified shilajit composition.
These and other objects and features of the invention will be made apparent from the following description thereof.
SUMMARY OF THE INVENTION
What is provided in this invention is a purified shilajit composition, without toxic components, obtained by extraction of native shilajit whose biologically active components are present in weight amounts of:
(a) at least 0.3%, preferably 0.4-1%, of an oxygenated dibenzo-[alpha]-pyrone (DBP), its di- and/or tetramers, and their esters; and
(b) at least 60%, preferably 65-70%, of low-to-medium molecular weight Mw({overscore (M)}n) fulvic acids (FAs), ({overscore (M)} is a number average molecular weight), having an E4/E6 absorption ratio of 8 to 10 at [lambda]465/665 nm.
The composition of the invention, as a 2% aqueous solution, has a pH of >7, preferably 7-8.
Preferably (a) is a methanol soluble 3-OH or 3, 8 (OH)2 DBP derivative, or their C16-C22 acyl esters; and (b) is a water soluble FAs.
Preferably the purified shilajit composition also includes, 0.01% to 0.4% of ([omega]-polyunsaturated fatty acids; 0.1-0.4 of a mono- or di-hydroxy-acetophenone, or C16-C22 acyl esters thereof; and 0.05 to 0.3% of [alpha]-lipoic acid.
Preferably, the fulvic acid component in (b) has an E4/E6 ratio of about 9-10.
Preferably, the purified shilajit composition also contains about 3-12% of benzoic acid, m-OH benzoic acid or C16-C22 alkanol esters thereof; and about 0.5-1% of -N and -S heterocyclic and other aromatic compounds.
The composition herein is further characterized by the substantial absence of humic acid and polymeric humins.
DETAILED DESCRIPTION OF THE INVENTION
In accordance with the invention, there is provided a purified shilajit composition, without toxic components, obtained by extraction of native shilajit whose biologically active components are present in weight amounts of:
(a) at least 0.3%, preferably 0.4-1%, of an oxygenated dibenzo-[alpha]-pryone (DBP), its di- and/or tetramers, and their esters; and
(b) at least 60%, preferably 65-70%, of low-to-medium molecular weight Mw({overscore (M)}n) fulvic acids (FAs), ({overscore (M)}n is a number average molecular weight), having an E4/E6 absorption ratio of 8 to 10 at [lambda]465/665 nm.
The purified shilajit of the invention includes (a) mono- or di-hydroxy or tetrameric dibenzo-[alpha]-pyrones (DBP) having the formulas shown below:
Image available on "Original document"
and (b) fulvic acids (FAs) which are a 4'-methoxy-6-carbomethoxybiphenyis (MCB) having the formula: XXX where R<1>, R<2 >and R<3≥H and R<4≥CO2Me.
The methanol soluble portion of the purified shilajit composition also includes 0.1-0.5% 3-OH dibenzo-[alpha]-pyrone; 0.3-1.5% 3,8-diOH dibenzo-[alpha]-pyrone; 0.001-0.1% eicosapentaenoic acid; 0.005-0.01% docosapentaenoic acid; 0.01-0.3% docosahexaenoic acid; 0.1-0.2% 2-hydroxyacetophenone; 0.01-0.2% 2,4-dihydroxyacetophenone and 0.05-0.3% [alpha]-lipoic acid.
The composition of the invention finds particular application in personal care, pharmaceutical and nutritional use formulations, suitably at a use level of 0.1 to 60% by weight of the composition, preferably about 0.2 to 10% in personal care formulations.
The purified shilajit compositions of the invention are obtained by an extraction procedure from native shilajit rock exdudate, as follows:
(a) powdering native shilajit exdudate and dissolving it in water as solvent,
(b) filtering the mixture to remove insoluble substances,
(c) evaporating water from the filtrate to obtain a brown viscous residue,
(d) extracting the residue with a hot organic solvent, e.g. methanol, to obtain both a soluble fraction which includes low Mw bioactive phenolic compounds particularly oxygenated dibenzo-[alpha]-pyrones, and insoluble shilajit humic substances,
(e) adding dilute aqueous NaOH to the insoluble shilajit humic portion to precipitate polymeric quinones,
(f) acidifying the filtrate below a pH of about 3 to precipitate humic acids leaving a brown acidic solution of fulvic acids,
(g) fractionating said acidic solution by passing it over activated carbon to provide a solution of low-to-medium Mw fulvic acids,
(h) passing the fulvic acid solution through a H<+>ion-exchange resin to concentrate the fulvic acids in solution,
(i) evaporating the solution, and
(j) combining the low-to-medium Mwfulvic acids Mw 700-2000, with the low Mwbioactive phenolic compounds in a suitable proportion, e.g. 9:1 by weight.
Standardization of purified shilajit compositions is controlled analytically so that the composition contains (a) at least 0.3%, preferably 0.4-1%, of oxygenated dibenzo-[alpha]-pyrones including mono-and dimers of 3,8-dihydroxy-dibenzo-[alpha]-pyrones (in free and metal ion conjugated forms) (by HPLC analysis, chemical analysis); (b) low-to-medium Mwfulvic acids (Mw 700-2000) in an amount of at least 60%, preferably 65-70% (HPTLC E4/E6 analysis at different pH levels; range 8-10, preferably 9-10; and electron spin resonance spectroscopy); and with metal ions (Fe (II/III), Cu(II) and Zn (II) and Mg(ll) ions in conjugated forms of (3-5%).
The 2% aqueous solution of the composition of the invention has a pH ≥7. A low pH indicates the presence of substantial amounts of humic acid, humins and polymeric humus, which, accordingly, are essentially absent herein.
The thus-obtained purified shilajit composition according to the invention has the relative abundance of bioactive constituents given in Table 1 below.
TABLE 1
Relative Abundance of Bioactive
Constituents in Purified Shilajit Composition
DBPs & di- or tetramers
3-OH & 3,8-(OH)2 Hydroxy (mono-di) Benzoic acid or its N,S,-heterocyclic &
dibenzo-[alpha]-pyrone acetophenones, or long chain esters other aromatic
A. or its esters C16-C22 its esters C16-C22 C16-C22 compds Amt (%) >0.3 0.1-0.4 3-12 0.5-1
B. Fulvic acids Amt (%) >60
The presence of the following additional compounds (see Structures 1-8 below), and their amounts, in the purified shilajit composition of the invention, obtained in the methanol extract, have been established by comprehensive chromatographic (HPTLC, HPLC, GLC) and spectroscopic (GC-MS, NMR) analyses using specific markers. (See Table 2).
TABLE 2
Compound (Str. No.) Amount (%) (w/w)
EPA (1) 0.001-0.1
DPA (2) 0.005-0.01
DHA (3) 0.01-0.3
3-OH-DBP (4) 0.1-0.5
3,8-di-OH-DBP (5) 0.3-1.5
2-OH HAP (6) 0.1-0.2
2,4-di-OH HAP (7) 0.01-0.2
LA (8) 0.05-0.3
where:
EPA -[omega]-3-polyunsaturated fatty acids (str. 1); (C20:5 [omega] 3, eicosapentaenoic acid).
DPA -[omega]-3-polyunsaturated fatty acid (str. 2).
DHA -[omega]-3-polyunsaturated fatty acid (str. 3), (C22:6 [omega] 3, docosahexaenoic acid).
HAPs - Hydroxyacetophenones (str. 6).
LA - Alpha-lipoic acid (str. 8).
Preferably, the purified shilajit composition of the invention contains 0.01 to 0.4% of [omega]-3-polyunsaturated fatty acids, 0.1 to 0.4% of hydroxyacetophenone, and 0.05 to 0.3% of [alpha]-lipoic acid.
A typical purified shilajit composition of the invention is further characterized by the parameters given in Table 3 below.
TABLE 3
Purified Shilajit Composition
Appearance Fine powder
Color Dark brown
Taste Bitter
Odor Characteristic
pH of 2% aqueous solution 7.01
Water soluble ext. value (% w/w) 92.0
Alcohol soluble ext. value (% w/w) 26.8
Total DBP (HPTLC) 0.427%
% Fulvic acid 65.3%
E4/E6 value 9.56
Total mineral matter 18.48%
(Fe, Cu, Zn, Ca, Mg)
Acid insoluble mineral matter 4.18%
Use Formulations of Invention Composition
A. Personal Care
...In summary, the purified shilajit composition of the invention includes defined bioactive compounds which impart therapeutic properties to the composition. Present in abundant amounts, the oxygenated dibenzo-[alpha]-pryones (DBPs), particularly, 3-hydroxy and 3,8-dihydroxy DBPs, elicit the bioactivities of antioxidant, adaptogenic and immuno-modulatory responses inside the system of recipients, and the low-to-medium Mw ({overscore (M)}n) (700 to 2,000) fulvic acids (FAs), having an E4/E6 ratio of 6-10, ensure the bioavailability of the DBP by acting as an efficient carrier for the DBPs.
The purified shilajit composition herein also is characterized by a minimum presence of humic acid, humans, polyphenolics, terpenoids, phytosteroids, amino acids, metal ions, moisture, mineral metallic ions and acid insoluble minerals, and the absence of toxic ingredients.
Therapeutics :
The present invention relates to pharmaceutical or veterinary or nutritional compositions of polyherbal extracts useful as anti-viral or immune-supporting agents. Particularly, the present invention of polyherbal composition comprises of extracts of Withania somnifera, Mangifera indica and purified Shilajit. This cost effective immune-supporting agent is ideal for use during the maintenance phase of the treatment, following an initial viral load reduction phase in which it is used as an adjuvant to conventional anti-viral drug therapy. The anti-viral and immune-supporting composition of this invention can perhaps be the sole basis of treatment where affordability is an issue. Additionally, this composition is used for the treatment, prevention or management of immune-supporting system in primates in need, especially human... comprising administering an effective amount of plant extracts of Withania somnifera and Mangifera indica and an extract of purified Shilajit obtained from rock exudates.
POLYHERBAL COMPOSITIONS AND METHODS FOR TREATING VIRAL INFECTIONS
US7250181
Detail Description of the Invention
1. Description of the Poly-Herbal Composition The polyherbal composition of the present invention contains the extracts of two plants Withania somnifera and Mangifera indica and an extract of rock exudates - purified Shilajit, A method for the treatment of viral infections is also disclosed. An effective amount of the polyherbal composition is administered one or more times a day either alone or as an adjuvant to an existing anti-viral therapy. a. Extract of Withania somnifera
Withania somnifera Dunn., referred to as Ashwagandha in Ayurvedic medicine, is reputed for promoting health and longevity by increasing defense against disease, arresting the aging process, revitalizing the body in debilitating conditions. W. somnifera is also known to have positive effects on mental functions and memory, and can be classified in modern terminology as an adaptogen (Sharma, P.V. (1978). In Dravyaguna Vijnan, 4th edition, p. 763-765, Chaukhamba Sansthan, Varanasi, India; Ghosal, S. (1986). In pursuit of Standardization of Ayurvedic Drugs, Ann. Natl. Acad. Ind. Med., 1, 1-14). Typically, commercially available extracts of Withania somnifera lack the beneficial chemical constituents in appreciable quantities for which Aswhwagandha is reputed for, instead they contain:
- Traces of glycowithanolide or completely devoid of glycowithanolides
- Large amount of withanolide aglycones - High level of polysaccharides and low levels of oligosaccharides
- Toxic tropane-type alkaloids, scopolamine
The quality of W. somnifera extract is improved by using the process reported in the U.S. Patent Nos. 6,153,198 and 6,713,092 Bl, which are herein incorporated by reference, and is a suitable process for obtaining the extract of W. somnifera. The extraction procedure provides a new and improved extract powder composition, which contains all the desired bioactive ingredients in optimized concentrations and ratios. The composition is stable, bio-available, and non-toxic.
Using this procedure, any parts of the plant of W. somnifera can be used in the present invention to obtain the extract provided it is devoid or have a trace amount of toxic tropane-type alkaloid, scopolamine. Preferred extract is the standardized extract containing glycowithanolides, withanolide agylcone and oligosaccharides and devoid or have a only a trace amount of toxic tropane-type alkaloid.
b. Extract of Mansifera indica
Mangifera indica is widely found in many tropical and sub-tropical regions, and mango is one of the most popular edible fruits in the world. Aqueous decoction of mango stem bark has been traditionally used for the treatment of menorrhagia, scabies, diarrhea, syphilis, diabetes, cutaneous infection, and anemia. Chemical studies performed with this extract have enabled the isolation and identification of phenolic acids, phenolic esters, flavan-3-ols, mangiferin, which is the predominant component of this extract...
Any parts of the plant of M. indica can be used in the present invention to obtain the extract. Preferably the extract contains at least 2% mangiferin and 2% mangiferin- and other xanthone glycosides along with other polyphenolics. Preferred standardized extract is obtained from M. indica bark. If needed, mangiferin from other plant sources can be blended with M. indica extract.
Preferred composition of the present invention includes an extract of M. indica bark comprising, by weight, (1) at least 2%, preferably to 5 to 10 %, most preferably 11 to 25% of mangiferin, and (2) at least 1% mangiferin and other xanthone O-glycosides.
Optionally, the M. indica extract of the present invention may contain other polyphenolics. The extract has about 70% water-soluble fraction.
c. Purified Shilajit
Shilajit is regarded as a panacea in many traditional systems of medicine, practiced worldwide. While many regard Shilajit as a potent immunomodulator and antioxidant, very few know what are the major bioactive constituents present in Shilajit.
Purified Shilajit of the present invention composed of three distinct classes of bioactive compounds: (A) Low- and medium-Mw (mol. wt.) non-humic organic compounds, comprising free and conjugated (e.g., fattyacyl, aminoacyl, lipoidal) DBPs; (B) dibenzo- alpha-pyrones chromoproteins (DCPs) comprising: (i) dibenzo-alpha-pyrones or their derivatives, (ii) phosphocreatine, (iii) chromo-peptides of molecular weights of about < 2 KD and (iv) lipids having fatty acyl esters of glycerol; and (C) fulvic acids of low to medium molecular weight (Mn about 700 to 2,000). The fulvic acids are polymeric units of 3,8-oxygeneated dibenzo-alpha-pyrone (or derivatives) repeat units.
These three classes of compounds are essentially of marine animal origin, - fossil invertebrates, among which mollusks/Ammonites constitute the major contributors. Humification process and residence time on different rock surfaces would result in shilajit of different grades and composition of desirable and undesirable constituents. Hence, preferably the bioactive and supportive constituents of the shilajit are considered in the purification and standardization of shilajit.
Any process can be used to obtain purified Shilajit for the present inventive composition. Preferably the extract contains all three bioactive compounds (A, B and C) mentioned above and has substantially low levels of polymeric quinones and humus and humic acids.
2. Pharmaceutical or Veterinary or Nutritional Composition
CI. Results of the Study
In the present open study, total 19 patients (3F; 16 M), mean age 29.7 + 5.6 years (range: 42.0 - 22.0), mean weight 61.7 ± 10.3 Kg (range: 37.0 - 78.0) and with mean duration of AIDS defining illness 126.8 days were enrolled to evaluate the efficacy and safety of new polyherbal composition. None of the patients received any anti-retroviral drugs. One patient died, and one was lost for follow up at the end of 6 months therapy....
...after 6 and 12 months treatment. Fatigue, anorexia, fever, cough, and skin rash were the most common presenting symptoms. Treatment with the herbal drug reduced incidence and severity of symptoms. There was marked improvement in symptoms like myalgia, fever, cough, and anorexia with treatment. Highly significant improvement was noticed in the Karnofsky score from baseline value of 80 (60 - 100) to 85 (70 - 100), and 90 (80 -100) at the end of 6, and 12 months respectively... The mean % decrease in viral load was 19 & 68% after 6 & 12 months treatment...
Herbo-mineral composition
US2003198695
A herbo-mineral composition includes a mineral-complexing agent which is purified Shilajit containing dimeric and/or oligomeric dibenzo-alpha-pyrones (DBPs), and, optionally, in synergistic combination with an extract of Emblica officinalis containing gallo/ellagi-tannoids (GET), and, one or more added minerals, such as iron, copper or chromium. The composition in the example where the added mineral is iron is particularly effective in treating iron-deficiency anemia by rapidly absorbing ferrous iron into the blood stream without side effects.
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to herbo-mineral compositions for treating mineral-deficient conditions, and, more particularly, to compositions which include a bioactive metal-complexing agent which is purified Shilajit containing purified dimeric and oligomeric dibenzo-[alpha]-pyrones (DBPs), obtained from native Shilajit, and, optionally, in synergistic combination with gallo/ellagi tannoids (GET) extracted from the Emblica officinalis plant, and an added mineral supplement, such as iron, copper, chromium and the like, which compositions can be readily absorbed in the body without gastric upset or side effects.
2. Description of the Prior Art
Anemia is defined as a deficiency of erythrocytes or hemoglobin per unit volume of blood. Its clinical manifestations are pallor of mucous membrane, dullness and listlessness due to relative tissue hypoxia. In its later stages, anemia is manifested by an increase in the rate and force of the heart beat, and extreme weakness. These symptoms also are associated with a decreased ability to fight infections, or to cope with any kind of stress, for example, a pregnancy, lactation in females, or normal growth in children.
The most common anemias are deficiency anemias arising from lack of iron, folic acid and/or cyanocobalamine. In developing countries, it is iron deficiency that results in most of the clinically observed cases of anemia. This form of deficiency often arises from parasitic infestation, particularly in children, an increased demand and limited iron supply from repeated pregnancies, or chronic blood loss with menstrual irregularities like hemorrhagic. Thus a higher incidence of iron deficiency anemia is observed in the female population and in growing children. For proper treatment, it is necessary to provide iron in therapeutic doses in a form that is easily absorbed by the body without side effects.
An average human male has about 4.5 g of iron in its body. Normally, about 1 mg of iron is absorbed from his diet daily, and the same amount is excreted during the same period. Since the total plasma iron turnover per day is about thirty times that of the iron absorption ratio, an extremely efficient mechanism for maintenance of iron balance must exist in the body. Even a slight disturbance of iron metabolism leads to iron-deficiency or an iron-overload, both being detrimental to health.
There are two kinds of iron in the diet which affect the mechanism of iron absorption, namely, haem-iron and non-haem iron, each utilizing separate receptors on the mucosal cells. After the uptake of haem-iron into the mucosal cells, its porphyrin ring is split by a special enzyme (haemoxygenase) within the cells and its iron is released. For non-haem iron, receptors on the luminal side compete with complexing luminal ligands for the iron ions; accordingly, its iron can only be absorbed into the cells and pass the mucosal membrane in the ferrous form. Therefore reducing substances must be present in the mucin layer of the mucosal cells for ferrous iron to be absorbed.
About two-thirds of iron in the body is found in haemoglobin, the rest in myoglobin, various other iron-containing enzymes and iron-transport proteins e.g., transferrin. Excess iron is stored as ferritin and haemosiderin, the latter being an insoluble product which occasionally is involved in the systemically deleterious free radical reaction known as the Fenton reaction.
When an iron over-dose occurs, or even a slight disturbance in iron metabolism, a Post-Fenton (Haber-Weiss) reaction can generate hydroxyl radicals with concomitant breaking of DNA strands, activation of poly-ADP ribose synthetase and NAD depletion, resulting in a marked reduction in cellular energy. These deleterious effects, which are consequences of the body's inability to dispose of excess iron, are manifested as gastro-intestinal bleeding and peripheral vascular collapse. Such symptoms also are found when high doses of inorganic iron compounds are taken which are not present in the form of iron complexes and/or iron chelates.
There are many expensive iron preparations available in the market today for the prevention and treatment of anemia. However, their effectiveness is uncertain, or associated with side-effects, and many need to be taken by injection. For example, parentral iron therapy is painful and often associated with development of anaphylaxis or late serum sickness; hence it is not suitable for many anemia patients. Oral iron therapy, on the other hand, requires heavy doses of ferrous salts, and may cause gastrointestinal distress, abdominal pain, nausea, vomiting, constipation or diarrhea, often in more than 25% of patients. Since iron therapy needs to be continued for at least 6 months, iron-supplementation with commonly available preparations often is required to rebuild reticulo-endothelial iron content.
Other mineral-deficient conditions in the body are known, which stem from an imbalance of, for example, chromium, copper, zinc, manganese and/or other elemental minerals. The present invention also addresses these conditions...
SUMMARY OF THE INVENTION
What is described herein is a herbo-mineral composition for the treatment or prevention of mineral-deficient conditions which includes purified Shilajit containing dimeric and/or oligomeric dibenzo-[alpha]-pyrones (DBPs), optionally, but preferably, in synergistic combination with an extract of the Emblica officinalis plant containing gallo/ellagi-tannoids (GET), and an added mineral supplement. The DBPs (and GETs) are the primary bioactive constituents in the composition. These complexing agents exert their natural reducing activity on the added mineral, e.g. iron, chromium, copper, zinc, manganese and the like, to maintain it in a bioavailable and effective oxidation state.
The DBPs in the composition suitably have a molecular weight ranging from about 450 to 2500 Daltons, preferably 500-700 Daltons, which allows for ready absorption of the metal ion-DBP complex from a fine, aqueous colloidal suspension of the composition.
DETAILED DESCRIPTION OF THE INVENTION
The composition of the invention is a herbo-mineral formulation useful for the treatment and prevention of mineral-deficient conditions e.g. anemia, in both children and adults. The composition is an admixture of dimeric and/or oligomeric dibenzo-[alpha]-pyrones (DBPs), e.g. as metallic complexes, isolated from purified and processed Shilajit*, and an added mineral, e.g. iron, chromium, copper, zinc, manganese, and the like. The composition preferably also includes a herbal extract of Emblica officinalis** which contains small molecular weight gallo-ellagi tannoids (GET). When present, the GET herbal extract synergistically enhances the coordinating site of the DBP-metal complex to maintain the complex in its reduced state, e.g. iron in the ferrous state, which can be more effectively utilized in the synthesis of hemoglobin. * U.S. patent application Ser. No. 09/860,890, filed May 18, 2001, incorporated by reference herein. ** U.S. Pat. No. 6,124,688, incorporated by reference herein.
In the past, when iron in the ferrous form was given without complexation, it was rapidly converted into ferric iron in the body resulting in poor iron absorption as well as formation of toxic free radicals. In the complexed form in the composition of this invention, ferrous iron is not converted into ferric form because ferrous iron is complexed with the DBPs (and GETs) which become trapped and stabilized in the micropores (d=100-150 A) of the purified Shilajit.
The dimeric and oligomeric DBP-humato-ferrate (Fe<2+>) complex in the composition herein suitably has a low molecular weight of about 450-2500 Daltons, preferably 500-700 Daltons, commensurate with rapid absorption of the added mineral in the body.
The following Table illustrates the defined composition of the invention:
TABLE
Suitable Preferred
Ingredient Amount (mg) Amount (mg)
Purified Shilajit 5-200 10-25
Emblica officinalis extract 0-500 50-150
Added Mineral Supplement 0.1-250 5-25
A typical composition of the invention, in the form of 100 ml of syrup, for example, includes about 200 mg of purified Shilajit, about 500 mg of Emblica officinalis extract, and about 250 mg of added mineral, e.g. Natural Product, which contains w/w 35-40% Fe and 15-18% Cu, and excipients, to q.s. The resultant formulation is a viscous, pourable liquid, dark-brown in color, with a pleasant odor, and a sweet-to-mildly bitter taste. The composition has a density of about 1.2 g/ml, a pH of 4.4, and a solids content (w/w) of 68%...
EXAMPLE 1
IRON PREPARATION CAPSULE
Ingredient Quantity per capsule (mg)
Purified Shilajit 25
Emblica officinalis 50
Elemental Iron 10
Excipients q.s.
EXAMPLE 2
IRON PREPARATION SYRUP
Ingredient Quantity per 100 ml (mg)
Purified Shilajit 250
Emblica officinalis 500
Elemental Iron 100
Excipients q.s.
Since slow release and re-absorption of the metal ion are inherent properties of the DBP-metal complex, the composition of the invention does not suffer from the limitations of prior compositions, e.g. amino acid-mineral chelates. These compositions exhibit metal ion irreversibility, which leave the metal ion in the undesirable higher oxidation state. For example, in iron-amino acid chelates, two of the six coordination sites of iron are unfilled by aqua-ligands, which increases the possibility of oxidation of ferrous to ferric iron. By contrast, in the present iron-DBP complex, all the coordination sites of ferrous iron are occupied; hence, ferrous iron therein is not readily oxidizable to ferric iron.
Moreover, while iron in the ferrous state in amino-acid chelates can experience difficulty in absorption and release of its iron, iron in the complexed ferrous form in the composition of this invention is released smoothly and absorbed readily into iron-deficient cells. In such an iron-complex, the molar ratio of ligand-to-iron is higher than that of the metal ion; hence, free iron which is not absorbed is again complexed with ligand(s) to prevent a Fenton reaction and its resultant free radical induced damage. Thus, the invention composition assures maximum absorption of iron without toxicity problems.
The iron-organo complex of the invention also is observed to behave similarly to transferrin because its iron can enter various cells of the body to synthesize iron-containing enzymes and proteins. Receptor-mediated endocytosis then can present the transferrin-like iron entity to the iron-deficient cells where it can enter the cytoplasm in a vacuole. At an acidic pH, the contents of the vacuole then can release iron from the iron-chelate with various cellular constituents, e.g. citrate, ATP and GTP. The iron-free assembly is then ejected from the cells for recapture of iron from an iron-free pool.
As a fine colloidal suspension with water, the composition of the invention can act as a potent and tenacious scavenger of both transition and fixed valency metal ions and thus it is capable of penetrating into different cell types. The invention complex, moreover, does not degrade in the presence of free radicals; instead, it can interact with free radicals to generate additional complexing and chelating entities (e.g. during interaction with an iron overload), which can further sequester toxic metal ions. Thus, in small amounts, the invention composition is capable of handling a large amount of iron overload to modulate the iron content in the body with notable beneficial results.
The DBP-polyphenol moieties present in the complex of the invention also is effective in reducing Fe<3+> to Fe<2+>; thus it will systemically mobilize and funtionalize systemic iron to hemoglobin. These moieties can abstract Fe<3+> from free metal ions to form readily absorbable Fe<2+> complexes, and to present and slowly release the metal ion to metal-deficient receptors.
In summary, the composition of the invention is an effective herbo-mineral formulation for prevention and treatment of several forms of anemia caused by hemorrhage, parasitic infestation, nutritional deficiencies, etc. in both children and adults, and in quickly raising the hemoglobin level of blood, e.g. by 1 gm/dl or more per week, without side effects. It also is especially useful for persons with mal-absorption syndromes, those suffering from chronic inflammatory disease, for people who have been taking NSAIDs for long periods, and for individuals suffering from inefficient production of erythrocytes, or increased loss of RBC in hemorrhagic anemia, and also for persons who normally do not respond to conventional chemical metal preparations.
Vitamin/mineral composition
US5405613
A composition comprising Shilajit or an extract thereof in a vitamin and/or mineral preparation. Shilajit is a compact mass of vegetable organic matter, composed of a gummy matrix interspersed with vegetable fibres and minerals. Substances which have been identified in Shilajit include moisture, gums, albuminoids, calcium, potassium, nitrogen, silica, resin, vegetable matter, magnesium, sulphur, iron, chloride, phosphorous, iodine, glycosides, tannic acid, benzoic acid and a number of vitamins and enzymes. The invention further relates to a method to restore energetic balance or intensity, or to support or enhance a bioenergetic field in a mammal comprising administering to a mammal an effective amount of Shilajit or an extract thereof...
In the Eastern world, a compound known as Shilajit (silajit) has a history of use as a folk remedy for various disorders, including genito-urinary diseases, diabetes, gall stones, jaundice, enlarged spleen, fermentative dyspepsia, worms, digestive disorders, piles, epilepsy, nervous disorders, eczema, anaemia, anorexia, asthma etc. Shilajit has also been used as a tonic to help retain youthful vigour. Shilajit has been administered either by itself or in combination with certain other ayurvedic (herbal) medicines...
Shilajit is a natural exudate ejected from rocks during hot weather in the lower Himalayas, Vindhya and other mountain tracts and Nepal, or it may be a tar formed in the earth from the decomposition of vegetable substances. (See the Indian Materia Medica, pages 23 to 32 for a detailed discussion of the composition and properties of Shilajit). It is a compact mass of vegetable organic matter, composed of a gummy matrix interspersed with vegetable fibres and minerals. Substances which have been identified in Shilajit include moisture, gums, albuminoids, calcium, potassium, nitrogen, silica, resin, vegetable matter, magnesium, sulphur, iron, chloride, phosphorous, iodine, glycosides, tannic acid, and a number of vitamins and enzymes. Shilajit also contains benzoic acid, a compound which, along with its derivatives, has been used as a component of nutritional vitamin and mineral preparations...
The present inventor has also surprisingly found that when a small amount of Shilajit is added to a vitamin or mineral preparation, the energetic properties of the vitamin or mineral preparation are enhanced. In particular, the present inventor has found that the addition of a small amount of Shilajit to a vitamin or mineral preparation increases the energy field of the entire preparation to at or near the vibratory level of pure Shilajit.
REVITALIZING AYURVEDA SUPPLEMENT FOR MALESThe invention relates to a revitalizing Ayurveda supplement for males, prepared of oriental plants and East- and West-European flora, employed to prophylactic purposes in the treatment of several metabolic malfunctions and/or for stimulating some physiological functions of the organism, playing a nutritive part with respect thereto. The claimed supplement comprises 80 g of Asparagus racemosus (sin A javanicus); 90 g Asphaltum (shilajit); 60 g of Boerhavia diffuza; 70 g of Centipeda minima; 10 g of Cinnamomi cortex (cinnamon); 30 g of Chlorophitum arundinaceum; 20 g of Corallium rubrum (Coral Bhasm); 10 g of Elletaria cardamomum; 100 g of Gummi accacia; 10 g of Mesua ferrea; 80 g of Mucuna prurita; 10 g of Miristica fragrans; 40 g of Spheranthus indicus; 120 g of Sida cordifolia; 70 g of Strichnos potatorum; 80 g of Tribulus terrestris; 10 g of Piper longum; 20 g of Zinci carbonas and 20 g of Zingiber officinale. All these components, as powder, are mixed, homogenized and processed as uncoated tablets of 500 mg and are administered orally, one tablet every evening, half an hour before meals, with warm milk, for at least 30 days. It is a highly revitalizing agent for males due to containing tonic, aphrodisiac and stimulant compounds, essential oils, tannins and mineral micro- and oligoelements.
RO117897
COMPOSITION CONTAINING SHILAJIT OR EXTRACT THEREOF
WO2005041990
The present invention relates to a novel use of Shilajit or the extract thereof.
More particularly, the present invention relates to a composition containing Shilajit or the extract thereof, which has the activity of enhancing the metabolic function of the entire human body, resulting in an improvement in sexual function and an increase in reproductive function, and thus, has beneficial effects on nutritional tonic, sexual function improvement, infertility treatment, and the like.
[Technical Background]
Shilajit (botanical name: Asphaltum), also known as mineral pitch, is a natural exudate oozed from rocks during hot weather in the lower Himalayas, Vindhya and other mountain tracts. Shilajit is a compact mass of vegetable organic matter, composed of a gummy matrix interspersed with vegetable fibers and minerals. Shilajit is known to include moisture, gums, albuminoids, calcium, potassium, nitrogen, silica, resin, vegetable matter, magnesium, sulphur, iron, chloride, phosphorous, iodine, glycosides, tannic acid, benzoic acid, vitamins and enzymes.
Meanwhile, in countries around the Himalayas, Shilajit has been traditionally used for general physical strengthening, anti-aging, blood sugar stabilization, injury healing, enhanced brain functioning potency, bone density increase, immune system strengthening, arthritis treatment, and hypertension treatment.
US Patent No. 5,405, 613 discloses that the addition of Shilajit or the extract thereof to a vitamin/mineral preparation has the effect of increasing the energetic properties of the vitamin/mineral preparation.
Moreover, US Patent No. 6,440, 436 discloses a method of purifying bioactive components of Shilajit. Also, this patent discloses that the Shilajit extract purified by this method may be used as a skin care and protection formulation or a pharmaceutical or nutritional formulation. The Shilajit composition disclosed in the patent contains, as biologically active components, 0.3% by weight of oxygenated dibenzo-a-pyrone and 60% by weight of low-molecular weight fulvic acid.
The literatures mentioned in this specification is incorporated herein by reference in its entirety.
The present inventors have conducted studies on screening of natural substances having the effects of restoring physical reproductive function and treating impotency, infertility, etc. , without side effects, and consequently found that the administration of Shilajit to human beings shows an improvement in sexual function, and the administration of Shilajit to white rats shows an increase in sperm number for males and a shortening the diestrus stage in estrous cycle for females, thereby completing the present invention...
Preferably, the inventive composition contains a Shilajit extract obtained by purifying the bioactive fractions of Shilajit. The bioactive fractions of Shilajit include 0. 3% by weight of oxygenated dibenzo-a-pyrones and 60% by weight of low-molecular weight fulvic acid. A method of obtaining such bioactive fractions of Shilajit is disclosed in US6440436 in detail.
The inventive composition has the activity of enhancing the metabolic function of the entire human body so as to improve sexual function and to enhance reproductive function.
The administration of the inventive composition to adult men for a given period increases erection number and lengthens erection maintenance time.
Thus, the inventive composition will be useful as foods or drugs for the improvement of sexual function or the strengthening of reproductive function. Also, the inventive composition is derived from natural substances, used in Himalayan region encompassing India, China, Tibet and parts of Central Asia for a long time and thus, advantageous in that it has secured safety and little or no side effects.
Generally, the causes of male infertility include semen or sperm abnormalities, sperm transport disorders, and aspermia. Among such causes, more than a half are spermatogenesis disorder caused by the disorder of testis function of making sperms, and the abnormality of sperm components.
The causes of female infertility are very various, and it is not easy to find these causes. Typical causes include the interruption of tubal patency, and ovulation disorders, such as amenorrhoea, anovulatory menstruation, and sporadic anovulatory disorders.
The administration of the inventive composition to white rats causes a remarkable increase in the sperm number of the testes and epididymides of the white rats for males, and shortens the diestrus stage in estrous cycles of the white rats for females.
Thus, the inventive composition may be effectively used to treat male infertility caused by sperm deficiency or to treat female infertility caused by ovulation abnormalities.
As can be seen in Table 6,6 of 7 volunteers answered that the erection maintenance time lengthened and the erection number in one sexual intercourse increased.
This indicates that the erection maintenance time and the erection number were generally increased.
In the results of the answer survey on erection degree, 2 of 7 volunteers answered that the erection degree was improved. Also, 2 of 5 persons who have not reached complete ejaculation answered that ejaculation was improved...
REGULATION OF STEROIDOGENIC ACTIVITY BY USING PURIFIED SHILAJIT
US2016220609
TECHNICAL FIELD
The present invention relates to promoting steroidogenic activity in the body of a mammal, including human, through the use of Shilajit.
BACKGROUND
Shilajit is composed of rock humus, rock minerals and organic substances that have been compressed by layers of rock mixed with marine organisms and microbial metabolites. It oozes out of the rocks in the Himalayas at higher altitudes ranging from 1000-5000 meters as black mass and is regarded as a maharasa (super-vitalizer) in Ayurveda, the traditional Indian system of medicine, dating back to 3500 B.C. Shilajit contains fulvic acids as the main components along with dibenzo-a-pyrones (“DBPs”) and dibenzo-a-pyrone chromoproteins.
Fulvic acid complex, derived from shilajit, is an assembly of naturally occurring low and medium molecular weight compounds comprising oxygenated dibenzo-alpha-pyrones (DBPs), both in reduced as well as in oxidized form, as the core nucleus, and acylated DBPs and lipids as partial structural units, along with fulvic acids (“FAs”). Fulvic acid complex material derived from alluvial sources lack DBPs; instead, the core nucleus of alluvial fulvic acid is comprised of benzoic acid. Thus, the active constituents of shilajit contain dibenzo-alpha-pyrones and related metabolites, small peptides (constituting non-protein amino acids), some lipids, and carrier molecules (fulvic acids). See, Ghosal, S., et al., “Shilajit Part 1—Chemical constituents,” J. Pharm. Sci. (1976) 65:772-3; Ghosal, S., et al., “Shilajit Part 7—Chemistry of Shilajit, an immunomodulatory ayurvedic rasayana,” Pure Appl. Chem. (IUPAC) (1990) 62:1285-8; Ghosal, S., et al., “The core structure of Shilajit humus,” Soil Biol. Biochem. (1992) 23:673-80; and U.S. Pat. Nos. 6,440,436 and 6,869,612 (and references cited therein); all hereby incorporated by reference herein.
Shilajit finds extensive use in Ayurveda, for diverse clinical conditions. For centuries people living in the isolated villages in Himalaya and adjoining regions have used Shilajit alone, or in combination with, other plant remedies to prevent and combat problems with diabetes (Tiwari, V. P., et al., “An interpretation of Ayurvedica findings on Shilajit,” J. Res. Indigenous Med. (1973) 8:57). Moreover being an antioxidant it will prevent damage to the pancreatic islet cell induced by the cytotoxic oxygen radicals (Bhattacharya S. K., “Shilajit attenuates streptozotocin induced diabetes mellitus and decrease in pancreatic islet superoxide dismutase activity in rats,” Phytother. Res. (1995) 9:41-4; Bhattacharya S. K., “Effects of Shilajit on biogenic free radicals,” Phytother. Res. (1995) 9:56-9; and Ghosal, S., et al., “Interaction of Shilajit with biogenic free radicals,” Indian J. Chem. (1995) 34B:596-602). It has been proposed that the derangement of glucose, fat and protein metabolism during diabetes, results into the development of hyperlipidemia. In one study, Shilajit produced significant beneficial effects in lipid profile in rats (Trivedi N. A., et al., “Effect of Shilajit on blood glucose and lipid profile in alloxan-induced diabetic rats,” Indian J. Pharmacol. (2004) 36(6):373-376).
As discussed, shilajit has been used to treat various ailments. It is also recommended as a performance enhancer. Fulvic acids (FAs) are reported to elicit many important roles in biological systems of plants, in animals as well as humans, including: (a) improvement of bioavailability of minerals and nutrients, (b) serve as electrolytes, (c) detoxification of toxic substances including heavy metals, (d) perform as antioxidants, and (e) improvement of immune function.
Furthermore, dibenzo-a-pyrones have been hypothesized to participate in the electron transport inside the mitochondria, thus facilitating production of more ATP, leading to increased energy. Thus, shilajit is found to increase energy, among other beneficial qualities.
In view of the above, it would be desirable to provide a method of using shilajit for improvement of mitochondrial function thus increasing energy in a human or animal. If a way could be found to stimulate steroidogenic gene expression related to skeletal muscle activity to provide increased energy using Shilajit, this would provide a valuable contribution to the medical and nutritional arts.
SUMMARY
An objective of the present invention is to develop a method of using Shilajit for promoting steroidogenic activity in the body of a mammal, for example, a human.
A method for promoting steroidogenic activity in a mammal is provided, comprising administering to the mammal in need of such treatment an effective amount of a purified Shilajit, wherein energy levels in the mammal are increased.
DETAILED DESCRIPTION
In one embodiment a gene expression study was conducted on the skeletal muscle of mice with Shilajit, 3,8-dihydroxy-dibenzo-a-pyrone (3,8-(OH)2-DBP), and placebo to determine the effect of these compounds on expression of genes related to skeletal muscle activity.
In another embodiment, a human clinical study was conducted with supplementation of Purified Shilajit for 8 weeks and skeletal muscle tissue was analyzed for gene expression.
It is contemplated that the compositions used herein may be administered advantageously in a mammal for inducing or promoting steroidogenic activity. As used herein, a mammal may include, but is not limited to, a human, a dog, a horse, or a cat.
Materials: Purified Shilajit (PrimaVie®, Natreon, Inc., New Brunswick, N.J.) is a standardized dietary supplement ingredient extracted and processed from Shilajit bearing rocks, containing not less than about 50% by weight fulvic acids (FAs), at least about 10% by weight dibenzo-a-pyrone chromoproteins, and at least 0.3%, or more, by weight total dibenzo-a-pyrones (DBPs).
3,8-(OH)2-DBP (99.0% pure, Natreon, Inc., New Brunswick, N.J.).
Procedure for Studies in Mice Using Shilajit and DBPs...
Procedure for Human Clinical Study ...
Gene Expression Profiling using GeneChip® Assay...
Results:
The following genes for steroid biosynthesis were up regulated or induced in mice by Shilajit:
(1) Hsd3b5: hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 5.
(2) Stard3: START domain containing 3. Start domain-containing protein 3; STARD3, a.k.a. metastatic lymph node 64: MLN64. Expression of MLN64 leads to increased pregnenolone secretion and that steroidogenic activity resides in the C terminus of the protein. Pregnenolone, also known as 3α,5β-tetrahydroprogesterone (3α,5β-THP), is an endogenous steroid hormone involved in the steroidogenesis of progestogens, mineralocorticoids, glucocorticoids, androgens, and estrogens, as well as the neuroactive steroids.
(3) Star: steroidogenic acute regulatory protein. Studies of Star in MA10 cells in the absence of hormone stimulation was sufficient to induce steroid production. This study concluded that Star is required for hormone-induced steroidogenesis.
(4) HSD3B1: 3-beta-hydroxysteroid dehydrogenase 1. 3-Beta-hydroxysteroid dehydrogenase catalyzes the oxidation and isomerization of delta-5-3-beta-hydroxysteroid precursors into delta-4-ketosteroids, thus leading to the formation of all classes of steroid hormones.
The steroidogenic genes may be up-regulated by Shilajit in accordance with an embodiment of the present invention. Other steroidogenic genes that may be upregulated include, but are not limited to: androgen binding protein alpha (Abpa), and oxysterol binding protein 2 (Osbp2).
3,8-(OH)2-DBP did not show significant effect on steroidogenic activity in mice.
Table 1 shows fold change results for several representative steroidogenic genes, in accordance with a hierarchical gene cluster array showing genes up-regulated in mice treated with Purified Shilajit. In particular, these genes are demonstrating up-regulation or induction in muscle tissue with Purified Shilajit.
Table 2 shows fold change for several steroidogenic genes in the human clinical study. These results are based on gene chip analysis of skeletal muscle samples from three subjects out of a total of 20 subjects. In particular, these genes are demonstrating up-regulation or induction in muscle tissue with Purified Shilajit. Gene chip analysis of the samples from the remaining subjects is pending and the statistical significance of these results is expected to improve after the results when all 20 subjects are statistically analyzed....
HEALTH MAINTENANCE FOOD
JP2007135494
The present invention relates to a novel use of Shilajit or the extract thereof. More particularly, the present invention relates to a composition containing Shilajit or the extract thereof, which has the activity of enhancing the metabolic function of the entire body, resulting in an improvement in sexual function and an increase in reproductive function, and thus has effects on nutritional tonic, sexual function improvement, infertility treatment, and the like.
ANTI-CANCER AND ANTI-PROLIFERATIVE COMPOSITIONS, AND METHODS FOR THEIR USE IN TREATING CANCER
CA3169459
PROMOTING MUSCLE BUILDING AND REPAIR AND TREATING DISORDERS RELATED TO COLLAGEN AND PERTINENT PROTEINS BY USING SHILAJIT
CA3173584
PROTECTION AGAINST CORONAVIRUS INFECTION BY EXTRACTS AND EXTRACT COMPONENTS
WO2022040321
FEED COMPOSITION COMPRISING CANNABIDIOL AND FULVIC ACID...
KR102278512
Herbal Nutraceutical Formulation to Reduce Oxidative Stress, Viral and Microbial Infections, and Inflammation
US2021220419
METHOD OF IMPROVING MUSCLE AND CONNECTIVE TISSUE WITH SHILAJIT
US2021169927
AGENT FOR INHIBITING SEBUM PRODUCTION OR ACCUMULATION, AGENT FOR PREVENTING OR IMPROVING DYSKERATOSIS, AND AGENT FOR PREVENTING OR IMPROVING ACNE
JP2021042151
METHOD TO EXTRACT A PHARMACEUTICAL COMPOSITION FROM A THERAPEUTIC COMPOUND
US2021023127
IMPROVEMENT OF BLOOD MICROPERFUSION TO SKIN BY SHILAJIT
CA3104621
COMPOSITION FOR TREATMENT AND MANAGEMENT OF POLYCYSTIC OVARIAN SYNDROME AND METHOD OF PREPARATION THEREOF
US2020197477
Functional chewing gum comprising phytonutrients and adaptogenic herbs
US2020214978
Composition for treatment and management of Dementia and Cognitive dysfunction and method of preparation thereof
US2020197474
IMPROVEMENT OF BLOOD MICROPERFUSION TO SKIN BY SHILAJIT
US2019388322
Medium composition for in vitro fertilization comprising shilajit or its extract as effective component and method of in vitro fertilization using the same
KR102027561
Herbo-mineral Formulation for prevention, treatment and management of Renal Disorders and method of preparation thereof
US2019134087
CHROMIUM-CONTAINING COMPOSITIONS FOR IMPROVING ENDOTHELIAL FUNCTION AND CARDIOVASCULAR HEALTHChromium-three cation containing compositions in combination with Phyllanthus emblica extract and Shilajit are useful for improvement of endothelial function and cardiovascular health, including treatment of type 2 diabetes and metabolic syndrome.
US2016015740