Penetration enhancement with binary system of oleic acid, oleins

Details Penetration enhancement with binary system of oleic acid, oleins Penetration enhancement with binary system of oleic acid, oleins

1988-07-13

1989-09-05

Terapane, John F.

Drug, bio-affecting and body treating compositions

Designated organic nonactive ingredient containing other...

Carboxylic acid or salt thereof

514947, 514772, 514785, 514786, A01N 6100, A61K 3100

Patent

active

048639702

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.

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Drug Delivery Systems, R. L. Juliano, "Characteristics and Biomedical Applications", 1980, p. 159.
Jane Stotts and W. Jeanne Ely, "Induction of Human Skin Sensitization to Ethanol", 1977, pp. 69:219-222.
William Brown et al., "Comparative Ultrastructure & Cytochemistry of Epidermal Responses to Tape Stripping, Ethanol & Vitamin A Acid in Hairless Mice", 1979, 73:203-206.

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