Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
2000-11-03
2002-06-11
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
C424S400000, C424S450000, C424S451000
Reexamination Certificate
active
06403116
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to compositions and methods for providing aqueous formulations of aqueous insoluble dietary supplements. In particular, this invention relates to compositions and methods for providing an aqueous formulation of the dietary supplement coenzyme Q10.
2. Related Background Art
Formulations of aqueous-insoluble dietary supplements are known in the art. Nutritional supplements incorporating lipophilic or fat-soluble essential nutrients such as vitamins or fatty acids are widely used in human and animal health care.
One compound receiving particular attention lately as a nutritional supplement and therapeutic agent is coenzyme Q10 (“Co-Q10”), a naturally occurring coenzyme chemically named 2,3-dimethoxy-5-methyl-6-decaprenyl-1,4-benzoquinone. Co-Q10 is also known by the names ubiquinone, ubidecarenone, and Vitamin Q and is classified as a fat soluble quinone.
U.S. Pat. No. 5,989,583 (Anselem) discloses that Co-Q10 is an antioxidant with potential use as a dietary supplement to protect against age-related degeneration and as an adjuvant vitamin to prevent or treat many diseases. The patent also discloses that supplementary Co-Q10 has also reportedly shown beneficial influences in periodontal disease, certain blood circulation diseases, impaired memory, fatigue, coronary disease, irregular heartbeat, high blood pressure, immune system impairment, and the aging process. Moreover, coenzyme Q10 has been reported to be capable of improving one's performance in sports by enhancing the uptake and processing of oxygen in cells.
As disclosed in WO 95/05164, Co-Q10 is crystalline at room temperature and has a melting point of 49° C. Due to its isoprenoid side chain, Co-Q10 is extremely lipophilic and practically insoluble in water. As such, the bioavailability of the compound, if administered orally, would be limited due to the hydrophilic nature of the gastrointestinal system.
Several patents and published PCT applications disclose methods and compositions for administration of Co-Q10 that are said to improve the bioavailability of the compound. For example, U.S. Pat. No. 6,056,971 (Goldman) discloses solubilizing water insoluble dietary supplements such as Co-Q10 in a solubilizing agent, generally a non-ionic surface active agent, and an edible polyhydric alcohol to provide a liquid composition that is administered in gelatin capsules. U.S. Pat. No. 4,483,873 (Ohashi et al.) discloses aqueous solutions of Co-Q10 containing hydrogenated lecithin. U.S. Pat. No. 4,572,915 (Crooks) provides non-aqueous compositions of fat solubilized nutrients that are formed by admixing the fat solubilized nutrient with polyethoxylated caster oil and a pharmaceutically acceptable water miscible polyol. U.S. Pat. No. 5,989,583 (Anselem) discloses a dry solid lipid composition comprising therapeutically active lipophilic compound, a lipid comprising at least one solid fat and at least one phospholipid. U.S. Pat. No. 6,045,826 (Borowy-Borowski et al.) discloses water-soluble compositions of lipophilic compounds such as Co-Q10 with a structurally defined solubilizing agent having both hydrophobic and hydrophilic moieties. Finally, published PCT application WO 95/05164 (Westesen et al.) discloses aqueous formulations of “sparingly soluble substances” such as Co-Q10 comprising colloidal particles of supercooled melts.
Methyl sulfonyl methane (“MSM”), also known as dimethyl sulfone or sulfonylbismethane, has been disclosed as having potential therapeutic effects. For example, Heshler has disclosed the oral administration of MSM to animals including humans for ameliorating symptoms of gastrointestinal upset (U.S. Pat. No. 4,514,421), for treating parasitic infections (U.S. Pat. No. 4,914,135), and for use as assimilable source of dietary sulfur for improving poor health and maintaining good health (U.S. Pat. No. 4,616,039). Further, U.S. Pat. No. 5,891,853 (Shealy et al.) discloses compositions comprising MSM, vitamin C and beta-1,3-glucan to enhance levels of dehydroepiandrosterone (DHEA) in humans.
Thus, a composition comprising Co-Q10 and MSM is desirable for nutritional and therapeutic benefits and for use in promoting general health maintenance. Further, a composition comprising Co-Q10 and MSM in an aqueous form is desirable for ease of administration and for the anticipated increase in bioavailability of the lipophilic nutrient component Co-Q10. Moreover, an aqueous composition comprising Co-Q10 and MSM in a formulation that remains in aqueous suspension without substantial separation for extended periods is desirable for incorporation into beverages and liquid forms that are intended to be stored for extended periods of time before consumption.
Therefore, it is an object of this invention to provide a composition comprising Co-Q10 and MSM. It is also an object of this invention to provide an aqueous dispersable formulation of Co-Q10 for oral administration. It is further an object of the invention to provide a stable aqueous formulation of lipophilic nutrients such as Co-Q10.
These and additional objects and advantages of the present invention are shown from the description below. The disclosures of the patents and publications cited throughout this specification are incorporated in their entirety to more fully describe the invention and to demonstrate the state of the art.
SUMMARY OF THE INVENTION
This invention provides compositions comprising coenzyme Q10, methyl sulfonyl methane, citric acid, and at least one polysorbate material.
The invention also provides stable aqueous compositions for oral administration to an animal comprising an admixture of coenzyme Q10, citric acid, methyl sulfonyl methane, and at least one polysorbate materials dispersed in an aqueous medium.
The invention further provides a method of administering a nutritionally significant amount of coenzyme Q10 to an animal which comprises administering to the animal a composition comprising coenzyme Q10, methyl sulfonyl methane, citric acid, and at least one polysorbate material.
The invention also provides a method of administering a therapeutically effective amount of coenzyme Q10 to an animal in need of such therapy which comprises administering to the animal a composition comprising coenzyme Q10, methyl sulfonyl methane, citric acid, and at least one polysorbate material.
DETAILED DESCRIPTION
This invention provides compositions comprising coenzyme Q10, methyl sulfonyl methane, citric acid, and at least one polysorbate material.
Those skilled in the art recognize that all the ingredients of the claimed composition are substances readily available through commercial sources. For example, Co-Q10 can be obtained from Seltzer Chemical Co. (Carlsbad, Calif.), methyl sulfonyl methane can be obtained from Carolwood Corp. (Greensville, Pa.), citric acid is available from Textile Chemical Co. (Reading, Pa.), polysorbate materials are available from Lipo Chemical (Paterson, N.J.). In a preferred embodiment, the compositions also comprise at least one water-soluble polysaccharide, which are available from Cerestar Co. (Hammond, Ind.). Maltodextrin is the preferred water-soluble polysaccharide for the claimed compositions and methods.
As used herein, the term polysorbate material encompasses the widely available Polysorbate or Tween products which comprise oleate esters of sorbitol and its anhydrides typically copolymerized with about 20 moles of ethylene oxide per mole of sorbitol and sorbitol anhydride. The polysorbate materials intended are those that are soluble or well dispersible in water. The oleate esters have the structure:
In a preferred embodiment, the polysorbate material is a sorbitan mono-9-octadecenoate poly(oxy-1,2-ethanediyl) derivative wherein the sum of w, x, y, and z is 80 (Tween 80 or Polysorbate 80).
In a preferred embodiment, the composition of the invention comprises about 0.1% to about 10% coenzyme Q10, about 0.1% to about 10% methyl sulfonyl methane, about 0.1% to about 15% polysorbate material, about 0.1% to about 10% citric acid, and about 45
Anderson Mark L.
Kelker Abdullah
Evans Charesse L.
Fitzpatrick ,Cella, Harper & Scinto
Page Thurman K.
Triarco Inductries, Inc.
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