Thesis (M.Sc. in Pharm.)--Chulalongkorn University, 2001

Development and evaluation of ketoprofen transdermal patches were studied. Formulations were prepared using Eudragit (R) E 100 as a polymer (pressure-sensitive adhesive). The effects of drug loading, amount and type of plasticizer on drug released from transdermal patches were investigated. In vitro studies found that ketoprofen transdermal patches gave a slow and prolonged release. The formulations which gave satisfactorily ketoprofen release were those with ketoprofen and plasticizer to amount of Eudragit (R) E 100 used in formula in the proportion of 35 and 40, respectively. Plasticizer that gave appropriate release was found to be tributyl citrate, propylene glycol and glycerin with the amount of 5.27 mg/cm2, 5.19 mg/cm2 and 4.34 mg/cm2, respectively. Formulations containing each of these three plasticizers that gave the best release were subsequently selected for in vivo studies. In vivo studies were performed using nine white New Zealand rabbits. Each rabbit received three ketoprofen transdermal patches of the individual three formulation in a crossover design. Blood samples were collected at predetermined time intervals and quantitated using HPLC. It was clearly shown that ketoprofen could be released from the transdermal patch into systemic circulation. Pharmacokinetic studies of ketoprofen transdermal patches demonstrated that the pharmacokinetic parameters obtained (AUC0-24, AUMC0-24 and MRT) were statistically significant difference (P<0.05). It can be concluded that the amount of ketoprofen loaded, concentration of plasticizer, and type of plasticizer in the patches affected the ketoprofen release and pharmacokinetic of drug.