Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2001-09-21
2003-05-06
Lankford, Jr., Leon B. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
C424S400000, C424S401000, C424S195180, C424S484000
Reexamination Certificate
active
06558712
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to delivery systems for active ingredients, and, more particularly, to a water-soluble delivery system for pharmaceutical, nutritional and cosmetic active ingredients, which includes a purified Shilajit composition obtained by extraction from native Shilajit containing a carrier which is purified fulvic acid, and, wherein the active ingredient is added to and present in voids of the carrier.
2. Description of the Prior Art
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; these substances have molecular weights ranging from several thousand for humic acids (HAs), to up to several million for polymeric humins (HMs) and only a few hundred for its fulvic acid (FAs) component. Humic substances also are found in soils and sediments distributed over the earth's surface, occurring in almost all terrestrial and aquatic environments. Sedimentary rock humic substances are produced by the interactions of marine fossils, 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 water-soluble humic substances.
The non-humic substances of Shilajit are low molecular weight (M
w
) compounds of marine fossil, plant and microbial origin, occurring in and around Shilajit-bearing rocks. The remaining non-humic organic masses in Shilajit comprise a mixture of low M
w
aromatic, aliphatic alicyclic, and heterocyclic (N- and S-containing) compounds. Of particular biological interest are low M
w
oxygenated dibenzo-&agr;-pyrones (DBP) and hydroxyacetophenones (HAPs).
The ancestral origin of Shilajit now has been established as invertebrate fossils of the phylum: Mollusca, of the Mesozoic period (60-200 million years ago). Shilajit arises from the continental drift and plate tectonic effect, reached from the ocean-bed to sedimentary mountain top; and by bacterial interaction-humification which formed Shilajit humus-paleohumus. However, native Shilajit material varies considerably with respect to quality and the amount of bioactive materials therein. Furthermore processing of native Shilajit involves very complicated and tedious procedures. Recently, collection of good quality native Shilajit material has been improved so that, correspondingly, the output of a purified Shilajit product can be expected to be much improved.
The biological effects of Shilajit are believed to be due to the two distinct classes of bioactive compounds, namely: (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 such bioactive compounds. Large amounts of contaminants, e.g. high M
w
polymeric quinones, humins (HMs), and inorganic substances; however, are present. Shilajit rhizospheres also are 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; these references are located in the related co-pending patent application. 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 water-soluble delivery system for active ingredients such as pharmaceutical, nutritional and cosmetic ingredients using a purified fulvic acid carrier having voids therein into which an active ingredient can be incorporated for effective and controlled delivery of the active therefrom.
Another object of this invention is to provide such a delivery system which can augment the bioavailability of drugs for the user.
A feature of the invention is the provision of a stable delivery system including a purified fulvic acid carrier having predetermined molecular weight and void sizes which can accept different active ingredients advantageously to deliver and release them smoothly at cell-receptor sites.
Another feature of the invention is the enhanced water solubility of active drug ingredients.
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 stable, water-soluble delivery system which includes (a) a purified Shilajit composition preferably containing at least 40% by weight of purified fulvic acid carrier, obtained by extraction of native Shilajit so that the fulvic acid carrier is substantially without bioactive components therein. The purified fulvic acid carrier is characterized by having a sponge-like structure punctured by voids of about 200-1000 Å in diameter and a molecular weight, {overscore (M)}n, of about 700-2500, ({overscore (M)}n is a number average molecular weight); and (b) an active material, e.g. a water-insoluble ingredient, added to and filling voids in the purified fulvic acid carrier.
Preferably, the purified fulvic acid carrier has an E
4
/E
6
absorption ratio of about 6-10, at &lgr; 465/665 nm.
Most preferably, the delivery system of the invention potentiates the bioactivity of a drug, nutritional or cosmetic ingredient incorporated into the voids of the purified fulvic acid carrier.
Still most preferably, the active ingredient suitably is present in an amount of about 0.5 to 40% by weight of the fulvic acid carrier.
DETAILED DESCRIPTION OF THE INVENTION
The difference between Shilajit-based fulvic acid (FAs) and alluvial soil-derived fulvic acids lies in the core structures of the fulvic acids (FAs) in these compositions. Shilajit-FAs contains 3,8-oxygenated dibenzo-&agr;-pyrone as the core nucleus, which, upon repeated oxidation, and Michael addition reactions by nucleophile-containing oxygen, nitrogen and carbon ions, in association with various lipid moieties, produce a multiplayer micellar structure. In contrast, alluvial soil-FAs are composed essentially of aromatic hydroxy acids and polyphenols derived from phenolic oxidations. Both these FAs contain different metal ions, especially Fe, Co, Zn, Ca, etc., associated with the FAs. The metals in Shilajit-FAs are well-organized, multicentered, metal-ion associated products which, in the case of iron,
Davis Ruth A.
Katz Walter
Lankford , Jr. Leon B.
Natreon Inc.
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