US2017216224A1PendingUtilityA1
Solid particulate compositions comprising coenzyme q10
Est. expiryMar 18, 2031(~4.7 yrs left)· nominal 20-yr term from priority
Inventors:Irwin C. Jacobs
A61K 9/1617A61K 9/16A61K 9/107A61K 31/122A61K 9/1652
54
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Claims
Abstract
The present invention generally relates to improvements in the bioavailability and/or solubility of coenzyme Q10. For example, the present invention relates to methods for preparing particulate compositions including coenzyme Q10 that generally comprise dispersing and/or dissolving the coenzyme Q10 throughout a suitable solvent, and combining the coenzyme Q10 and an encapsulating (e.g., microencapsulating) agent. The present invention also generally relates to particulate compositions comprising coenzyme Q10 that exhibit improved bioavailability and/or solubility as compared to previous coenzyme Q10 products.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A solid particulate composition comprising coenzyme Q10, the particulate composition comprising microparticulates comprising coenzyme Q10, wherein the microparticulates comprising coenzyme Q10 have a particle size distribution such that at least about 90% by weight of the microparticulates have a particle size of from about 1 to about 4 μm.
2 . The composition of claim 1 wherein coenzyme Q10 constitutes at least about 10% by weight of the solid particulate composition.
3 . The composition of claim 1 wherein coenzyme Q10 constitutes from about 10% to about 50% by weight of the solid particulate composition.
4 . The composition of claim 1 wherein the particles comprise:
a solid matrix comprising an encapsulator; and
the microparticulates dispersed throughout the solid matrix.
5 . The composition of claim 4 wherein the encapsulator is selected from the group consisting polysaccharides, methylcellulose, hydroxypropyl methylcellulose, hydroxyethylcellulose, hydroxypropylethylcellulose, sodium carboxymethylcellulose, crystalline cellulose, ethylcellulose, polyvinylpyrrolidone, pectin, gum arabic, gum tragacanth, acacia, gelatin, and mixtures thereof.
6 . The composition of claim 4 wherein the encapsulator comprises a starch.
7 . The composition of claim 4 wherein the microparticulates comprise coenzyme Q10 and at least one surfactant.
8 . The composition of claim 7 wherein the microparticulates comprise a first surfactant having an HLB of at least about 9 and a second surfactant having an HLB of less than about 7.5.
9 . The composition of claim 8 wherein the first surfactant is selected from the group consisting of tocopherol polyethylene glycol succinate, polyvinylpyrrolidone, polyoxyethylene stearate, sodium cholate, deoxycholate and taurocholate.
10 . The composition of claim 8 wherein the second surfactant is selected from the group consisting of phosphatidyl choline, phosphatidyl serine, phosphatidyl inositol, phosphatidylglycerol, dioleoyl phosphatidylcholine, dioleoylphosphatidylglycerol, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine, phosphatidylethanolamines, phosphatidylserines, sphingomyelins, poly gylcerol esters, ethoxylated castor oil, a phospholipid derived from soy, or a phospholipid derived from milk-fat globule membrane.
11 . The composition of claim 1 wherein at least about 50% of the coenzyme Q10 is present in an amorphous state.
12 . A solid particulate composition comprising coenzyme Q10, wherein the solid particles have a particle size distribution such that at least about 50% by weight of the particles have an overall particle size of from about 6 μm to about 25 μm in diameter, and wherein the solid particles are in the form of a water-soluble matrix comprising an encapsulator having discrete microparticulates of coenzyme Q10 dispersed throughout the water-soluble matrix.
13 . The composition of claim 12 wherein at least about 50% by weight of the solid particles have an overall particle size of from about 8 μm to about 15 μm in diameter.
14 . The composition of claim 12 wherein at least about 50% by weight of the discrete coenzyme Q10 microparticulates have a particle size of less than about 10 μm.
15 . The composition of claim 12 wherein at least about 50% by weight of the discrete coenzyme Q10 microparticulates have a particle size of less than about 5 μm.
16 . A solid particulate composition comprising coenzyme Q10, a first surfactant having a hydrophile-lipophile balance (HLB) of at least 8, a second surfactant having a hydrophile-lipophile balance (HLB) of less than 8, and a water-soluble encapsulator, wherein the encapsulator is selected from the group consisting of starches and chemically modified starches, and wherein the weight ratio of the encapsulator to the first surfactant is from about 0.5:1 to about 4:1.
17 . The composition of claim 16 wherein the chemically modified starch comprises dextrin, maltodextrin, succinylated starch, alkaline-modified starch, bleached starch, oxidized starch, enzyme-treated starch, distarch phosphate, acetylated starch, hydroxypropyl starch, hydroxyethyl starch, octenyl succinic anhydride starch, cationic starch, carboxymethylated starch, or a combination thereof.
18 . The composition of claim 16 comprising discrete coenzyme Q10 microparticulates comprising coenzyme Q10 associated with the first surfactant and the second surfactant.
19 . The composition of claim 18 wherein at least about 50% by weight of the discrete coenzyme Q10 microparticulates have a particle size of less than about 10 μm.
20 . The composition of claim 18 wherein at least about 50% by weight of the discrete coenzyme Q10 microparticulates have a particle size of less than about 5 μm.Cited by (0)
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