ENHANCEMENT OF PERCUTANEOUS-ABSORPTION OF KETOPROFEN - EFFECT OF VEHICLES AND ADHESIVE MATRIX

The effects of various vehicles on percutaneous absorption of ketoprof en in a solution formulation and in a pressure-sensitive adhesive (PSA ) matrix were evaluated. The permeation rate of ketoprofen across hair less mouse skin was evaluated using a flow-through diffusion cell syst em at 37 degrees C. The solubility of ketoprofen was determined using the equilibrium solubility method. Among tested vehicles, octanol, eth anol, and propylene glycol (PG)/oleyl alcohol (OA) mixture showed the highest flux of 30 mu g/cm(2) per h from 5 mg/ml solution. However, it was not possible to demonstrate any correlation between the solubilit y of ketoprofen and its permeation rate, indicating change in the barr ier property of the skin and/or carrier mechanism by vehicles used. Wh en the effects of various vehicles on the percutaneous absorption of k etoprofen from acrylic PSA matrix were evaluated, oleic acid showed a slightly higher flux of 2 mu g/cm(2) per h than all other solvents tes ted. As the concentration of ketoprofen in acrylic PSA matrix increase d from 6.3 to 16.7%, the permeation rate also increased almost linearl y. The permeation rate of ketoprofen from polyisobutylene (PIB)-type P SA matrix was more than three times higher than that from acrylic PSA matrix. (C) 1998 Elsevier Science B.V. All rights reserved.