초록 ▼

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, containe

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.

대표청구항 ▼

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

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.