Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai
Reexamination Certificate
2001-02-22
2001-10-09
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ether doai
C514S458000, C514S474000, C514S556000, C514S560000, C514S725000
Reexamination Certificate
active
06300377
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to compositions comprising coenzyme Q (ubiquinone) in liquid form which provides enhanced bioavailability and may be presented in dietary supplement, cosmetic or pharmaceutical dosage form (preferably oral dosage form), including hard or soft gelatin capsules for oral administration.
BACKGROUND OF THE INVENTION
Coenzyme Q (ubiquinone), a dietary supplement, is a vitamin-like substance which is used to treat congestive heart failure and other cardiac problems, including heart ailments and diseases such as congestive heart failure, as well as a number of other conditions including high blood pressure, mitochochondrial disorders, including mitochondrial encephalomyopathy, anoxia, lactic acidosis, strokelike symptoms, neurodegenerative diseases, Kearns-Sayre syndrome and Alper's disease, among others. Coenzyme Q is the best known of a group of lipophilic quinones which have the capacity to transfer reducing equivalents or electrons within a lipid phase of cellular membranes. Reduced benzoquinones in general are effective reductants for oxygen or lipid radicals. Early studies showed that reduced coenzyme Q is an effective antioxidant. See, Mellors and Tappel, 1996
, J. Biol. Chem
., 241: 4353-4356. Reduced coenzyme Q now appears to function as part of a complex chain of antioxidant activity.
An important role of coenzyme Q can be in reduction of radicals of &agr;-tocopherol and ascorbate formed when these antioxidants are oxidized by oxygen or carboxyl radicals. There are no enzymes for direct reduction of tocopheryl radical or external ascorbate radical, but there are enzymes in all membranes which can reduce coenzyme Q and the reduced coenzyme Q can reduce the tocopheryl or ascorbate radicals to restore tocopherol or ascorbate. Without the support of enzymes to reduce coenzyme Q, the reduced coenzyme Q would not be a very effective antioxidant because the semiquinone formed by interaction with lipid or oxygen radicals is readily autooxidized with formation of a superoxide radical.
OBJECTS OF THE INVENTION
It is therefore an object of the present invention to provide a liquid form of coenzyme Q (ubiquinone) which can be administered with high bioavailability.
It is an additional object of the invention to provide a method for enhancing the bioavailability of coenzyme Q to patients by administering effective amounts of coenzyme Q in a liquid form which exhibits high bioavailability.
It is still another object of the present invention to provide coenzyme Q in liquid form which provides enhanced bioavailability and may be presented in dietary supplement, cosmetic or pharmaceutical dosage forms oral or topical administration.
These and/or other objects of the invention may be readily gleaned from a description of the invention which follows.
SUMMARY OF THE INVENTION
The present invention relates to a composition in cosmetic, dietary supplement or pharmaceutical dosage form of coenzyme Q which can be administered in high bioavailability form topically or as an oral dosage form. The compositions according to the present invention comprise an effective amount of coenzyme Q ranging from about 0.05% to about 15%, more preferably about 0.5% to about 10%, more preferably about 1.0% to about 7.5% by weight of the composition in combination with a polysorbate surfactant such as a Tween™ surfactant, most preferably, polysorbate 80, and amount of a vegetable oil or triglyceride, in further combination with an effective amount of a mono-, di or tri substituted glyceryl ester, preferably a C
1
-C
6
glyceryl triester, even more preferably a C
1
-C
4
glyceryl triester, or mixtures of these esters. In certain compositions according to the present invention, a component such as a phospholipid (e.g., hydroxylated lecithin) may be added to increase the solubility of the composition. In addition, in preferred embodiments according to the present invention, tocopherols (including vitamin E and vitamin E esters (such as vitamin E acetate, among others) or other vitamin additive, including other bioactive agents (lipophilic and non-lipophilic), are combined with ubiquinone as active agent. In addition, in certain embodiments, water may be optionally added, in an amount ranging from about 0.01% to about 10% by weight of the final formulation. Compositions according to the present invention preferably avoid the inclusion of a polyhydric alcohol solvent, such as propylene glycol or glycerine.
In addition to the above components, compositions according to the present invention may optionally comprise flavorings, preservatives and coloring agents in relatively minor amounts (i.e., in amounts which do not substantially impact the ability of the other components to work together to form a liquid dosage form). Compositions according to the present invention are preferably solvent free.
DETAILED DESCRIPTION OF THE INVENTION
The term “coenzyme Q” or “ubiquinone” is used throughout the present specification to describe a group of lipid soluble benzoquinones involved in electron transport in mitochondrial preparations, i.e., in the oxidation of succinate or reduced nicotine adenine dinucleotide (NADH) via the cytochrome system. According to the existing dual system of nomenclature, the compounds can be described as: coenzyme Q
N
, where n is 1-12 or ubiquinone (x) in which x designates the total number of carbon atoms in the side chain and can be any multiple of 5. Differences in properties are due to to the difference in the chain length. The preferred ubiquinone for use in the present invention is coenzyme Q
10
.
The amount of ubiquinone which is included in compositions according to the present invention ranges from about 0.05% to about 15% (preferably, no more than about 10.0% by weight and even more preferably no more than about 7.5% by weight of the final liquid composition).
The term “surfactant” or “emulsifier” is used interchangeably to describe additives to compositions according to the present invention. Surfactants for use in the present invention are solubilizers which are used to promote the solubility of the ubiquinone. These are to be used in combination with a triglyceride or vegetable oil and a short chain glyceryl ester, preferably a glyceryl triester. Polysorbate surfactants (Tween™) are clearly preferred. The amount of surfactant used in the present invention ranges from about 0.1% to about 50% by weight, more preferably about 1.5% to about 40%, preferably about 10% to about 35% by weight. Surfactants for use in the present invention are pharmaceutically acceptable and include, for example, the polysorbate surfactants as primary surfactants, and in certain embodiments, minor amounts of secondary surfactants such as the Span™ surfactants. Surfactants which exist in the liquid state at temperatures at or less than formulation temperature (generally, about 80° C. or less, more preferably about 50-65°) are preferred because they can also function as co-solvents or co-solubilizers in the present compositions. The preferred surfactant for use in the present invention is polysorbate 80 (Tween™80) surfactant.
In the present invention, the use of polysorbate (Tween™) 80 surfactant is preferred, with a mixture of Tween™ surfactants or Tween™ and Span™ surfactants, representing an alternative embodiment.
The Tween™ or polysorbate type surfactants are oleate esters of sorbitol and its anhydrides copolymerized with a number of moles of ethylene oxide per mole of sorbitol and sorbitol anhydride. The Tween™ surfactants are soluble or well dispersible in water. Preferred Tween™ surfactants include a sorbitan mono-9-octadecenoate poly(oxy-1,2-etheandiyl) derivative otherwise known as Tween™ 80 or Polysorbate 80.
The sum of w,x,y and z is 20 and R=C
17
H
33
CO
The Span™ surfactants, which may be optionally included in the present compositions of the present invention as secondary surfactants (the polysorbate surfactants are the preferred primary surfactants), are partial esters of common fatty acids, such as lauric acid, palmitic acid, stearic aci
LandOfFree
Coenzyme Q products exhibiting high dissolution qualities does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Coenzyme Q products exhibiting high dissolution qualities, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Coenzyme Q products exhibiting high dissolution qualities will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2605978