Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols
First Claim
1. A pharmaceutical composition for topical application having penetration-enhancing properties consisting essentially of:
- (a) a safe and effective amount of an active pharmaceutical agent contained in,(b) a penetration-enhancing vehicle exclusive of diols and N-cyclic solvents consisting essentially of;
(i) 1-95% by weight of one or more cell-envelope disordering compounds selected from the group consisting of oleic acid, oleyl alcohol, glycerol esters of oleic acid and mixtures thereof;
(ii) 5-75% by weight of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof; and
(iii) 0-45% by weight of an inert diluent.
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Accused Products
Abstract
Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents.
379 Citations
40 Claims
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1. A pharmaceutical composition for topical application having penetration-enhancing properties consisting essentially of:
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(a) a safe and effective amount of an active pharmaceutical agent contained in, (b) a penetration-enhancing vehicle exclusive of diols and N-cyclic solvents consisting essentially of; (i) 1-95% by weight of one or more cell-envelope disordering compounds selected from the group consisting of oleic acid, oleyl alcohol, glycerol esters of oleic acid and mixtures thereof; (ii) 5-75% by weight of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof; and (iii) 0-45% by weight of an inert diluent. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40)
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Specification
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- Resources
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Current AssigneeTheratech, Inc. (Dynatronics Corporation)
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Original AssigneeTheratech, Inc. (Dynatronics Corporation)
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InventorsChang, Yunik, Patel, Dinesh C.
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Primary Examiner(s)Terapane, John F.
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Assistant Examiner(s)Scalzo, Catherine S. K.
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Application NumberUS07/218,702Time in Patent Office419 DaysField of Search424/59, 514/946, 514/947, 514/69, 514/784, 514/785, 514/786, 514/772US Class Current514/784CPC Class CodesA61K 47/10 Alcohols; Phenols; Salts th...A61K 47/12 Carboxylic acids; Salts or ...A61K 47/14 Esters of carboxylic acids,...A61K 9/0014 Skin, i.e. galenical aspect...
