In vitro diffusion studies for the studies for the assessment and optimization of drug release from various ketoprofen dermatological formulations.

摘要

Ketoprofen is a potent Non-Steroidal Anti --Inflammatory agent, widely used for symptomatic treatment of inflammatory syndromes such as rheumatoid arthritis, osteoarthritis and acute gouty arthritis. Unfortunately due to its poor solubility and hydrophobic nature several clinical failures have been demonstrated.;Orally administered Ketoprofen has been associated with systemic adverse events and in particular gastrointestinal disorders. Topical application of Ketoprofen is locally effective and at the same time reduces the risk of systemic adverse events.;This study was conducted to screen vehicles and various dermatological formulations. To develop an optimum topical dosage form of Ketoprofen. Formulations were developed using gels and emulsions based systems with an optimal pH. In-Vitro drug release studies were carried out using cellulose membrane and human cadaver skin. The general rank order of drug release from these samples was observed to be HPMC Gel base > Anionic emulsion base > Non Ionic emulsion base. In addition, the effects of various penetration enhancers including Propylene Glycol, Diethylene Glycol mono ethyl ether at 5%, 10% and 15% levels and urea at 2.5%, 5% and 7.5% levels were evaluated. In most cases addition of addition of additives had a little or no effects n enhancing the drug release from the bases.;Furthermore, to assess the in-vitro drug release / permeation of the drug formulation exhibiting optimum drug release was evaluated using human cadaver skin as barrier. Here, as expected the drug release was significantly reduced compared to data observed with cellulose membrane. Though the amount of drug release from the barrier was less, the drug release pattern was similar.