Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-06-15
2001-03-06
Clardy, S. Mark (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S970000
Reexamination Certificate
active
06197813
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to stable vitamin C concentrate compositions for preparing finished products such as cosmetic and dermatologic preparations, food products, e.g., processed foods, beverages, and nutritional supplements, and medicinal, dental, opthalmic and surgical compositions for both enteral and parenteral introduction.
In another respect, the invention concerns finished products prepared from such concentrate compositions.
Another aspect of the invention pertains to methods of manufacturing such concentrate compositions and finished products.
In yet another respect, the invention relates to methods of using such finished products.
BACKGROUND OF THE INVENTION
Vitamin C has many known biological functions, e.g., acting as a wound healing accelerant. to prevent or treat periodontal disease, as an enzymatic co-factor, as a “sparing” agent against vitamin E depletion, as a collagen-synthesis stimulator, etc. Vitamin C is known to counteract oxygen-containing free radicals, including both the superoxide and hydroxyl radicals. These oxidative free radicals are generated in-vivo under a variety of normal and pathological conditions, and vitamin C is known for its ability to ameliorate conditions caused by oxygen free radicals, e.g., sunburn, cataracts, premature aging and a variety of other degenerative conditions.
Because of the beneficial effects attributed to vitamin C, many attempts have been made to formulate liquid vitamin C compositions. However, because of its notorious instability, particularly at higher pH's, pharmacologists and other scientists working in the field have had difficulty formulating stable liquid vitamin C compositions that would be useful in preparing various end-use products.
It would be highly desirable to provide vitamin C concentrate compositions, and end-use products prepared from these concentrates, which have improved physical stability and chemical stability under less acidic conditions.
It would also be highly desirable to provide such vitamin C concentrate compositions which are especially adapted for use in preparing a wide variety of end-use products, including cosmetic products, medical products, including dermatologic, dental, opthalmic and surgical products, wound healants, etc., and various food products, e.g., processed foods, beverages, nutritional supplements, etc.
PRIOR ART
U.S. Pat. No. 2,822,317 (Gulesich et al.) discloses a liquid aqueous composition which includes L-ascorbic acid (including ascorbyl fatty acid esters), a ferrous salt (including ferrous sulfate, lactate, gluconate, succinate, glutamate and choline citrate salts and complex salts) and a C
5
-C
6
polyhydric alcohol. This composition is said to have “satisfactory” stability at pH=2.0 to 3.5.
U.S. Pat. No. 5,587,149 (Punto et al.) discloses that solutions of ascorbic acid dissolved in polyethylene glycol (“PEG”) and then emulsified in a silicone fluid to form an (ascorbic acid+PEG)-in-silicone emulsion are physically “stable”, in the sense that they “do not exhibit creaming, sedimentation, or phase separation.” However, to prevent chemical degradation of the ascorbic acid, these emulsions are encapsulated in gelatin “twist-off” capsules.
U.S. Pat. No. 4,938,969 (Schinitsky et al.) discloses a composition of ascorbic acid, tyrosine and a water-soluble zinc salt, e.g., zinc sulfate, in “a tissue compatible vehicle” (e.g., mineral oil+sesame oil+glycerine+PEG), but does not report the chemical or physical stability of this composition.
U.S. Pat. No. 5,536,500 (Galey et al.) reviews several stabilization methods for vitamin C, involving physical techniques (e.g., incorporation in zeolites, etc.), chemical modification of the ascorbic acid molecule, such as conversion to the phosphodiester in combination with vitamin E, and functionalization of the enediol group by formation of phosphate, sulfate, ether or ester functions. Ascorbyl esters of cinnamic acid are disclosed, but neither the physical or chemical stability of such esters in liquid carriers is reported.
U.S. Pat. No. 5,140,043 (Darr et al.) discloses topical compositions of ascorbic acid (or a reducing analog), in a water-(glycol or polyol) carrier. It is asserted that the 12-week shelf stability is acceptable (≈100% ascorbic acid retention) only if the ratio of water to glycol/polyol carrier is high (e.g., at least 1:1) and the pH is maintained at ≦3.5.
U.S. Pat. No. 5,350,773 (Schweikert et al.) reports liquid compositions containing a fat-soluble substance are stabilized against “microbiological spoilage” for as long as six months, by dispersing the fat-soluble substance in a glycerol or glycerol-water continuous phase containing an ascorbyl fatty acid ester (e.g., ascorbyl palmitate) “emulsifier.”
U.S. Pat. No. 5,736,567 (Cantin et al.) discloses aqueous ascorbic acid-polyol-oil compositions, with relatively lower water contents than conventional cosmetic or dermatologic compositions.
DESCRIPTION OF THE INVENTION
BRIEF STATEMENT OF THE INVENTION
I have now discovered liquid Vitamin C concentrate compositions having improved stability, which are especially adapted for preparing finished products. These concentrate compositions include at least one mineral ascorbate, dissolved in at least one pharmacologically acceptable liquid organic polyol solvent for the mineral ascorbate(s). The concentrate compositions have a pH of at least about 5, preferably from about 5 to about 7.
According to another aspect of the invention, the concentrate composition preferably also contains at least one aldonic compound.
In yet another aspect, the concentrate composition of the invention preferably also includes a pharmacologically acceptable zinc compound, preferably a water-soluble zinc salt.
The invention also comprises a liquid vitamin C composition which includes the reaction product of at least one mineral ascorbate and at least one pharmacologically acceptable liquid polyol solvent for the mineral ascorbate.
The invention further includes liquid vitamin C compositions which include 4-hydroxy-5-methyl-3(2H)-furanone and/or 3-hydroxy-kojic acid, as well as such compositions which also include at least one aldonic compound and/or a pharmacologically acceptable zinc compound.
The invention also contemplates finished products prepared from the concentrate compositions and/or reaction products defined above.
According to another aspect of the invention, finished emulsion products comprise a continuous phase and a disperse phase, the concentrate composition being carried in one of these phases.
In still another respect, the invention includes methods for administering vitamin C which include the step of topically, orally, enterally or parenterally introducing to humans or animals, a finished product prepared from the above-defined concentrate composition.
According to yet another embodiment, the concentrate compositions/reaction products defined above include a compound which is characterized by the 285 nm high-performance liquid chromatographic (HPLC) peak which appears after the solvent front peaks and before the ascorbate peak, now identified as 4-hydroxy-5-methyl-3(2H)-furanone, i.e,
and such compositions and reaction products which also include 3-hydroxy-kojic acid, i.e.,.
Other aspects and features of the invention will become apparent to those skilled in the art from the following detailed description thereof, taken in conjunction with the drawings.
REFERENCES:
patent: 5173214 (1992-12-01), Kissel
patent: 5437880 (1995-08-01), Takaichi et al.
patent: 5658578 (1997-08-01), Ogawa et al.
patent: 5674527 (1997-10-01), Inoue et al.
patent: 5696169 (1997-12-01), Otsu et al.
patent: 5807542 (1998-09-01), Challis et al.
patent: 5906811 (1999-05-01), Hersh
patent: 5955083 (1999-09-01), Bonte et al.
patent: 5968533 (1999-10-01), Porter et al.
patent: 62-70309 (1987-03-01), None
Clardy S. Mark
Drummond & Duckworth
Oxycal Laboratories, Inc.
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