AU2011200677B2 - Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration - Google Patents
Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration Download PDFInfo
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- AU2011200677B2 AU2011200677B2 AU2011200677A AU2011200677A AU2011200677B2 AU 2011200677 B2 AU2011200677 B2 AU 2011200677B2 AU 2011200677 A AU2011200677 A AU 2011200677A AU 2011200677 A AU2011200677 A AU 2011200677A AU 2011200677 B2 AU2011200677 B2 AU 2011200677B2
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- coenzyme
- bioadhesant
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- 235000015872 dietary supplement Nutrition 0.000 title claims abstract description 64
- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 title claims abstract description 58
- 235000017471 coenzyme Q10 Nutrition 0.000 title claims abstract description 53
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 title claims abstract description 52
- 229940110767 coenzyme Q10 Drugs 0.000 title claims abstract description 20
- 238000000034 method Methods 0.000 title claims abstract description 13
- 239000000203 mixture Substances 0.000 title abstract description 12
- 238000009472 formulation Methods 0.000 title description 7
- 229920000148 Polycarbophil calcium Polymers 0.000 claims abstract description 12
- 239000002775 capsule Substances 0.000 claims abstract description 12
- 229950005134 polycarbophil Drugs 0.000 claims abstract description 11
- 229920002125 Sokalan® Polymers 0.000 claims abstract description 7
- BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical class COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229920002319 Poly(methyl acrylate) Polymers 0.000 claims abstract description 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 6
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000004584 polyacrylic acid Substances 0.000 claims abstract 2
- 150000002632 lipids Chemical class 0.000 claims description 15
- 239000003963 antioxidant agent Substances 0.000 claims description 11
- 235000006708 antioxidants Nutrition 0.000 claims description 11
- 230000003078 antioxidant effect Effects 0.000 claims description 9
- 210000002381 plasma Anatomy 0.000 claims description 8
- 239000002202 Polyethylene glycol Substances 0.000 claims description 7
- -1 acetyl CoQ10 Chemical compound 0.000 claims description 7
- 229920001223 polyethylene glycol Polymers 0.000 claims description 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 6
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 6
- 229920002674 hyaluronan Polymers 0.000 claims description 6
- 229960003160 hyaluronic acid Drugs 0.000 claims description 6
- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims description 6
- 235000010382 gamma-tocopherol Nutrition 0.000 claims description 5
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 5
- 239000002478 γ-tocopherol Substances 0.000 claims description 5
- QUEDXNHFTDJVIY-DQCZWYHMSA-N γ-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-DQCZWYHMSA-N 0.000 claims description 5
- 230000036470 plasma concentration Effects 0.000 claims description 4
- 229920000858 Cyclodextrin Polymers 0.000 claims description 3
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims description 3
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims description 3
- 241001529742 Rosmarinus Species 0.000 claims description 3
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims description 3
- OGBUMNBNEWYMNJ-UHFFFAOYSA-N batilol Chemical class CCCCCCCCCCCCCCCCCCOCC(O)CO OGBUMNBNEWYMNJ-UHFFFAOYSA-N 0.000 claims description 3
- 235000019136 lipoic acid Nutrition 0.000 claims description 3
- 150000003904 phospholipids Chemical class 0.000 claims description 3
- 229960002663 thioctic acid Drugs 0.000 claims description 3
- 229940057917 medium chain triglycerides Drugs 0.000 claims description 2
- 229940116351 sebacate Drugs 0.000 claims description 2
- 229920001577 copolymer Polymers 0.000 claims 3
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 3
- 239000000227 bioadhesive Substances 0.000 abstract description 9
- 239000000126 substance Substances 0.000 abstract description 6
- 239000000499 gel Substances 0.000 abstract description 4
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- 229920001059 synthetic polymer Polymers 0.000 abstract description 3
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- 238000010521 absorption reaction Methods 0.000 description 4
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- 229920000642 polymer Polymers 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- 238000000855 fermentation Methods 0.000 description 1
- 230000004151 fermentation Effects 0.000 description 1
- 238000010579 first pass effect Methods 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 230000004217 heart function Effects 0.000 description 1
- KUQWZSZYIQGTHT-UHFFFAOYSA-N hexa-1,5-diene-3,4-diol Chemical compound C=CC(O)C(O)C=C KUQWZSZYIQGTHT-UHFFFAOYSA-N 0.000 description 1
- 210000001700 mitochondrial membrane Anatomy 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- NPCOQXAVBJJZBQ-UHFFFAOYSA-N reduced coenzyme Q9 Natural products COC1=C(O)C(C)=C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)C(O)=C1OC NPCOQXAVBJJZBQ-UHFFFAOYSA-N 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000001839 systemic circulation Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229940035936 ubiquinone Drugs 0.000 description 1
- 150000003669 ubiquinones Chemical class 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/15—Vitamins
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Abstract
The present invention relates to compositions comprising Coenzyme Q10 (CoQ 10) and a bioadhesive substance. These compositions can take the form of dietary supplements in capsules, tablets, powder, gel, liquid, bar or in a single serving tube. The bioadhesive can be a synthetic polymer such as poly acrylic acid, hydroxypropyl methylcellulose, polycarbophil and poly methylacrylate derivatives. The invention also relates to methods of increasing uptake of Coenzyme Q10 because the bioadhesive substance increases the uptake of Coenzyme Q10 when taken orally in combination.
Description
WO 2006/110924 PCT/US2006/014416 DIETARY SUPPLEMENT FORMULATIONS FOR IMPROVED DELIVERY OF COENZYME Q10 AND METHODS OF ADMINISTRATION References Related to the Application [001] Under 35 U.S.C. § 119(e) this application claims the benefit of U.S. Provisional Application No. 60/671,404 filed April 14, 2005, which is hereby incorporated by reference in its entirety. Field of Invention [0021 In one aspect, the present invention relates to a formulation comprising Coenzyme Q10, or derivatives of Coenzyme Q10, and a bioadhesive substance. The formulation can be provided to an individual in the form of a dietary supplement to increase the uptake of Coenzyme Q10 to the blood. The present invention also relates to methods of increasing the level of Coenzyme Q10 in the blood plasma of an individual by administration of a dietary supplement comprising Coenzyme Q10 and a bioadhesive substance. Background of the Invention 10031 Coenzyme Q10, also known as ubiquinone (herein referred to as "CoQ10"), supports heart function as a component of the electron transport system, and as an antioxidant protects mitochondrial membranes and cholesterol from oxidation. Because CoQlO is of high molecular weight and is poorly soluble in water, various approaches have been taken to improve the dissolution and bioavailability of CoQ10 in dietary supplements. For example, CoQ10 has been complexed with cyclodextrins or solubilized with medium chain triglycerides to improve dissolution and availability of CoQ10. [004] Bioadhesives are generally defined as substances that adhere to a biological tissue for an extended period of time. Bioadhesives can be used to solve bioavailability problems by increasing the time that active ingredient resides at the site of absorption of the active ingredient. For example, mucoadhesants are a type of bioadhesive material that binds to the mucin layer of a biological membrane. Transmucosal delivery of biologically active substances offer advantages because mucus membranes are relatively permeable, allowing for the rapid uptake of an active substance into the systemic circulation and avoiding first pass metabolism. Mucoadhesants can WO 2006/110924 PCT/US2006/014416 also increase the residence time during which a substance may be absorbed, further increasing uptake. [0051 Because CoQ1O has limited solubility in water, various formulations have been tried to improve the absorption of CoQ10 administered in dietary supplements. However, the previous attempts to improve absorption have been inadequate or have other drawbacks. There exists a need for a dietary supplement containing CoQ10 in a formulation that results in improved absorption of the CoQ10 by an individual. Summary of the Invention [0061 In one aspect, the present invention relates to a dietary supplement comprising CoQlO and a bioadhesant. Derivatives of CoQ10, such as for example esterified CoQ1O or other CoQlO complexes, may also be used in the dietary supplements of the present invention. The bioadhesant may be a synthetic polymer such as poly (acrylic acid), hydroxypropyl methylcellulose, or poly (methylacrylate) derivatives. Alternatively, the mucoadhesant may be a naturally occurring polymer such as hyaluronic acid. Preferably, the bioadhesive should be lipophilic. The dietary supplement may be provided in any appropriate form for administration to an individual, such as a capsule, tablet, powder, gel, liquid, bar, or in a single serving tube. [0071 The dietary supplement may include additional ingredients, such as a lipid and an antioxidant for lipid stability. The dietary supplement may also contain excipients. When the dietary supplement is provided in a capsule or tablet, the dietary supplement may also include an enteric coating to protect the capsule or tablet as it passes through the stomach. [0081 In another aspect, the present invention relates to methods for increasing the level of CoQlO in an individual by administration of a dietary supplement comprising CoQ10, or a derivative of CoQ 10, and a bioadhesant. [0091 In yet another aspect, the present invention relates to methods for manufacturing a dietary supplement comprising CoQIO, or a derivative of CoQ1O, and a lipid mucoadhesant. 2 WO 2006/110924 PCT/US2006/014416 Detailed Description of Preferred Embodiments 10010] In a first aspect, the present invention is directed to a dietary supplement comprising CoQ10 and a bioadhesant. The CoQ10 is preferably derived from fermentation and consists substantially of the natural trans configuration synthesized by humans, although the invention is not limited in this regard and any appropriate form or derivative of CoQ10 may be used. The dietary supplement contains sufficient CoQ10 to increase the level of CoQ10 in the blood plasma of an individual. In preferred embodiments, the dietary supplement contains between about 10mg to about 1000 mg of CoQ10, preferably between 30 mg to about 300 mg of CoQ10, and more preferably between about 100 mg and about 200 mg of CoQ10. [00111 CoQ10 derivatives comprising CoQl0 complexed or combined with other molecules, may be used in the dietary supplements of the present invention. Any appropriate form of CoQ10 that may be combined with a bioadhesant may be used in the dietary supplement. For example, esterified ubiquinones, such as for example acetyl CoQ10, succinyl CoQ10, or propionyl CoQ10, may be used. Alternatively, CoQ10 complexes, such as polyoxyethanyl alpha-tocopheryl sebacate (PTS)-CoQlO complex or CoQ10-cyclodextrin complex, may be used. In the following description of preferred embodiments, it should be understood that a CoQ10 derivative may be used in place of CoQ 10 in the embodiments described. [0012] In addition to CoQ10, the dietary supplement includes a bioadhesant. Preferably, the bioadhesant is lipophilic, although the invention is not limited in this regard. The bioadhesant may be a mucoadhesant. Any appropriate mucoadhesant known to those skilled in the art may be used in the composition. Examples of bioadhesants that may be used in the composition include synthetic polymers, such as poly (acrylic acid), hydroxypropyl methylcellulose, or poly (methyl-acrylate) derivatives. These materials may be copolymerized with polyethylene glycol (PEG) or poly (vinyl pyrrolidone) (PVP) to improve interpenetration and interdiffusion into the mucosal surface. [0013] In one embodiment of the invention, polycarbophil is used as the bioadhesant, such as for example the polycarbophil manufactured by Noveon, Inc. of Cleveland, Ohio. Polycarbophils are polymers of acrylic acid crosslinked with divinyl glycol. 3 WO 2006/110924 PCT/US2006/014416 [0014] Naturally occurring polymers, such as, for example, hyaluronic acid, may also be used as bioadhesants in the formulations of the present invention. [00151 The dietary supplements may contain nutrients in addition to CoQl0. For example, the dietary supplements may contain vitamin or other ingredients. The dietary supplements may also contain a lipid, such as for example phospholipids, a medium chain triglyceride, diglycerides or monoglycerides, and may also contain an antioxidant for lipid stability. Antioxidants that may be used for this purpose include, without limitation, gamma tocopherol, alpha lipoic acid, rosemary, ascorbyl palmitate or any other lipid antioxidant known to those skilled in the art. Additionally, excipients may be added to aid in tableting, as carriers, or for any other reason associated with the manufacture or storage of dietary supplements. [0016] In one embodiment, the dietary supplement is provided in form of a softgel. The softgel may be made from any material known to those skilled in the art, such as for example gelatin, glycerin and water. The softgel may contain between 10 mg and 1000 mg, and preferably between about 30 mg and about 200 mg, of CoQ1O and between 10 mg and 1000 mg, and preferably between about 30 mg to about 500 mg, of a bioadhesant, such as for example polycarbophil. The softgel may further comprise between 10 mg and 1000 mg of a lipid, such as for example a medium chain triglyceride, diglycerides or monoglycerides. In addition, the softgel may contain an antioxidant for lipid stability. The softgel may also contain another lipid, such as phospholipids (for example, phosphatidylcholine) in a range of 100 mg to 1000 mg. Antioxidants that may be used for this purpose include, without limitation, gamma tocopherol, alpha lipoic acid, rosemary, ascorbyl palmitate or any other lipid antioxidant known to those skilled in the art. [0017] Examples of embodiments of the invention are provided below. It will be understood that the following examples are provided as an aid to understanding the invention, and are not intended to limit the invention in any way. [0018] Example 1 - Dietary Supplement in Capsule Form [00191 CoQ10 Between 30 mg to 200 mg 4 WO 2006/110924 PCT/US2006/014416 [00201 Bioadhesant (e.g.Polycarbophil) to capacity of capsule [0021] Gamma tocopherol 4 mg [00221 Enteric coating Optional [0023] Excipients Optional [0024] Example 2 - Dietary Supplement in Tablet Form [00251 CoQ10 Between 10 mg to 100 mg [0026] Bioadhesant (e.g.Polycarbophil) Between 10 mg to 1200 mg [0027] Gamma tocopherol 4 mg [0028] Enteric coating Optional [00291 Excipients Optional [00301 Example 3 - Dietary Supplement in Softgel Form [0031] CoQ10 Between 10 mg to 1000 mg [0032] Bioadhesant (e.g. polycarbophil) Between 10 mg to 1000 mg [0033] Lipid Between 10 mg to 1000 mg [00341 Antioxidant Between 4 mg to 200 mg [0035] In another aspect, the present invention provides methods for increasing the level of CoQ10 in the plasma of an individual by administration of a dietary supplement comprising CoQ10 and a bioadhesant. Preferably, the administration of the dietary supplement will result in a plasma concentration of CoQ 10 of between about 2 pg/ml and about 4 Rg/ml, as compared to typical plasma CoQ10 plasma levels of between 0.6 sg/ml to 0.8 g/mtL The dietary supplement may be administered in the form of one or more tablets, capsules, or softgels, in the form of a liquid or gel, or in a bar or other nutritional supplement. The amount of dietary supplement to be 5 WO 2006/110924 PCT/US2006/014416 administered depends on the quantity of CoQ10 in each dose (i.e. tablet, capsule, softgel, etc.), and the weight of the individual. The quantity to be administered to achieve a desired plasma level can be easily determined by a person skilled in the art. 10036] The dietary supplements of the present invention can be manufactured using methods known to those skilled in the art. The components may be mixed and placed in the proper form for preparation of tablets, capsules, soft gels liquids or any other desired form using production known production methods. [0037] As will be recognized by those of ordinary skill in the art based on the teachings herein, numerous changes may be made to the above-described embodiments of the invention without departing from its scope as described above and defined in the appended claims. For example, combinations of CoQ10 or one or more derivatives of CoQ10 may be used, and combinations of bioadhesants may be used in a dietary supplement formulation. Accordingly, this detailed description of preferred embodiments is to be taken in an illustrative, as opposed to a limiting, sense. 6
Claims (20)
1. An ingestible dietary supplement comprising in a soft gel capsule from about 75 mg to about 1000 mg of Coenzyme Q10 and from about 75 mg to about 1000 mg of a bioadhesant selected from the group consisting of polycarbophil, hyaluronic acid, a copolymer comprising at least one of poly (acrylic acid), hydroxypropyl methylcellulose or poly (methyl-acrylate) derivatives, copolymerized with at least one of polyethylene glycol, polyvinyl pyrrolidone, and combinations thereof, wherein the bioadhesant in the dietary supplement increases the residence time in the digestive tract to increase the blood plasma Coenzyme Q10 levels to from between about 2 ug/ml to about 4 ug/ml.
2. The dietary supplement of claim 1, wherein the dietary supplement contains between about 100 mg and about 1000 mg of Coenzyme Q10.
3. The dietary supplement of claim 1 or 2, wherein the dietary supplement contains between about 100 mg and about 200 mg of Coenzyme Q10.
4. The dietary supplement of claim 2, wherein the dietary supplement contains between about 100 mg and about 1000 mg of a bioadhesant.
5. The dietary supplement of claim 3, wherein the dietary supplement contains between about 100 mg and about 500 mg of a bioadhesant.
6. The dietary supplement of claim 4, wherein the bioadhesant comprises poly (vinyl pyrrolidone) (PVP).
7. The dietary supplement of claim 5, wherein the bioadhesant comprises polyacrylic acid.
8. The dietary supplement of claim 5, wherein the bioadhesant comprises hyaluronic acid.
9. The dietary supplement of claim 5, wherein the bioadhesant comprises polycarbophil.
10. The dietary supplement of claim 5, further comprising a combination of at least one lipid and an antioxidant for lipid stability. 7 8
11. The dietary supplement of claim 10, wherein the lipid is selected from the group consisting of phospholipids, medium chain triglycerides, diglyceride, monoglycerides, and combinations thereof.
12. The dietary supplement of claim 11, wherein the antioxidant for lipid stability is selected from the group consisting of gamma tocopherol, alpha lipoic acid, rosemary, ascorbyl palmitate, and combinations thereof.
13. An ingestible dietary supplement comprising in a soft gel capsule from about 75 mg to about 1000 mg of a derivative of Co010 and from about 75 mg to about 1000 mg of a bioadhesant selected from the group consisting of polycarbophil, hyaluronic acid, a copolymer comprising at least one of poly (acrylic acid), hydroxypropyl methylcellulose or poly (methyl-acrylate) derivatives, copolymerized with at least one of polyethylene glycol, polyvinyl pyrrolidone, and combinations thereof, wherein the bioadhesant in the dietary supplement increases the residence time in the digestive tract to increase the blood plasma Coenzyme Q10 levels to from between about 2 ug/ml to about 4 ug/ml.
14. The dietary supplement of claim 13, wherein the derivative of CoQ1O is selected from the group consisting of acetyl CoQ10, succinyl CoQ10, propionyl CoQ10, polyoxyethanyl alpha-tocopheryl sebacate (PTS)-CoQ1O complex, CoQ10-cyclodextrin complex, and combinations thereof, and further comprising a member selected from the group consisting of polyethylene glycol (PEG), poly (vinyl pyrrolidone) (PVP), and combinations thereof.
15. A method for increasing the level of Coenzyme Q10 or a derivative thereof in an individual comprising the step of administering to the individual an ingestible dietary supplement comprising in a soft gel capsule from about 75 mg to about 1000 mg of Coenzyme Q10 and from about 75 mg to about 1000 mg of a bioadhesant selected from the group consisting of polycarbophil, hyaluronic acid, a copolymer comprising at least one of poly (acrylic acid), hydroxypropyl methylcellulose or poly (methyl-acrylate) derivatives, copolymerized with at least one of polyethylene glycol, polyvinyl pyrrolidone, and combinations thereof, wherein the bioadhesant in the dietary supplement increases the residence time in the digestive tract to increase the blood plasma Coenzyme Q10 levels to from between about 2 ug/ml to about 4 ug/ml.
16. The method of claim 15, wherein the dietary supplement is administered to achieve a blood plasma concentration of Coenzyme Q10 of between about 2 pg/ml and about 4 pg/ml. 8 9
17. The method of claim 15, wherein the dietary supplement contains between about 100 mg and about 1000 mg of Coenzyme Q10.
18. The method of claim 16 or 17, wherein the dietary supplement contains between about 100 mg and about 200 mg of Coenzyme Q10.
19. An ingestible dietary supplement substantially as herein described with reference to the examples.
20. A method for increasing the level of Coenzyme Q10 or a derivative thereof in an individual comprising the steps substantially as herein described with reference to the examples. 9
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2011200677A AU2011200677B2 (en) | 2005-04-14 | 2011-02-17 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US67104005P | 2005-04-14 | 2005-04-14 | |
| US60/671,040 | 2005-04-14 | ||
| PCT/US2006/014416 WO2006110924A2 (en) | 2005-04-14 | 2006-04-14 | Dietary supplement formulations for improved delivery of coenzyme q10 and methods of administration |
| AU2006235633A AU2006235633A1 (en) | 2005-04-14 | 2006-04-14 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
| AU2011200677A AU2011200677B2 (en) | 2005-04-14 | 2011-02-17 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2006235633A Division AU2006235633A1 (en) | 2005-04-14 | 2006-04-14 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2011200677A1 AU2011200677A1 (en) | 2011-03-17 |
| AU2011200677B2 true AU2011200677B2 (en) | 2012-08-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| AU2006235633A Abandoned AU2006235633A1 (en) | 2005-04-14 | 2006-04-14 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
| AU2011200677A Expired - Fee Related AU2011200677B2 (en) | 2005-04-14 | 2011-02-17 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2006235633A Abandoned AU2006235633A1 (en) | 2005-04-14 | 2006-04-14 | Dietary supplement formulations for improved delivery of coenzyme Q10 and methods of administration |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1940455A4 (en) |
| CN (1) | CN101500599A (en) |
| AU (2) | AU2006235633A1 (en) |
| CA (1) | CA2604952A1 (en) |
| WO (1) | WO2006110924A2 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI22465B (en) * | 2007-03-15 | 2010-10-29 | Valens Int. D.O.O. | New combination of water soluble forms of coenzyme q10 and l-carnitin, procedure of preparation and application |
| CN101480381B (en) * | 2009-01-21 | 2013-01-02 | 郑微 | Coenzyme Q10 pharmaceutical composition |
| CN102793167B (en) * | 2012-08-17 | 2014-06-11 | 福州复美达生物科技有限公司 | Rosemary antioxidant coenzyme Q10 capsule and preparation method thereof |
| CN105561329A (en) * | 2016-01-22 | 2016-05-11 | 辽宁万嘉医药科技有限公司 | Cyclodextrin triad-supramolecular inclusion compound compounded by water-soluble coenzymes Q10 and alpha-lipoic acid and preparing method |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030072798A1 (en) * | 2000-01-13 | 2003-04-17 | Alpharx Inc. | Solid self-emulsifying dosage form for improved delivery of poorly soluble hydrophobic compounds and the process for preparation thereof |
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|---|---|---|---|---|
| IT1191608B (en) * | 1985-02-01 | 1988-03-23 | Zambon Spa | PHARMACEUTICAL COMPOSITION AND PHARMACEUTICAL FORMS THAT CONTAIN IT |
| IL117773A (en) * | 1996-04-02 | 2000-10-31 | Pharmos Ltd | Solid lipid compositions of coenzyme Q10 for enhanced oral bioavailability |
| US5891469A (en) * | 1997-04-02 | 1999-04-06 | Pharmos Corporation | Solid Coprecipitates for enhanced bioavailability of lipophilic substances |
| JPH11165128A (en) * | 1997-12-04 | 1999-06-22 | Namiki Precision Jewel Co Ltd | Driving device of vibration actuator |
| US6395311B2 (en) * | 1998-04-29 | 2002-05-28 | Univera Pharmaceuticals, Inc. | Multicomponent biological vehicle |
| US6045826A (en) * | 1999-04-02 | 2000-04-04 | National Research Council Of Canada | Water-soluble compositions of bioactive lipophilic compounds |
| US6403116B1 (en) * | 2000-11-03 | 2002-06-11 | Triarco Inductries, Inc. | Coenzyme Q10 formulation |
| DE10064219B9 (en) * | 2000-12-22 | 2009-02-12 | Nasalis Pain Relief International Gmbh | Novel pharmaceutical composition containing fentanyl and / or its derivatives |
| US6652891B2 (en) * | 2001-12-12 | 2003-11-25 | Herbasway Laboratories, Llc | Co-enzyme Q10 dietary supplement |
-
2006
- 2006-04-14 AU AU2006235633A patent/AU2006235633A1/en not_active Abandoned
- 2006-04-14 EP EP06758378A patent/EP1940455A4/en not_active Withdrawn
- 2006-04-14 CN CNA2006800175160A patent/CN101500599A/en active Pending
- 2006-04-14 CA CA002604952A patent/CA2604952A1/en not_active Abandoned
- 2006-04-14 WO PCT/US2006/014416 patent/WO2006110924A2/en active Application Filing
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2011
- 2011-02-17 AU AU2011200677A patent/AU2011200677B2/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030072798A1 (en) * | 2000-01-13 | 2003-04-17 | Alpharx Inc. | Solid self-emulsifying dosage form for improved delivery of poorly soluble hydrophobic compounds and the process for preparation thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2011200677A1 (en) | 2011-03-17 |
| EP1940455A4 (en) | 2011-01-26 |
| CN101500599A (en) | 2009-08-05 |
| WO2006110924A2 (en) | 2006-10-19 |
| AU2006235633A1 (en) | 2006-10-19 |
| EP1940455A2 (en) | 2008-07-09 |
| CA2604952A1 (en) | 2006-10-19 |
| WO2006110924A3 (en) | 2009-04-16 |
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