아세클로페낙 연질캡슐(클란자 에스 연질캡슐)의 개발

Abstract

To develop an aceclofenac soft capsule, four preparations with various solubilizers were prepared and their dissolution test was carried out. Among four preparations tested, a preparation with ethanolamine was selected as a formula of aceclofenac soft capsule (Clanza STM), since it showed the fastest dissolution rate. Bioequivalence of aceclofenac tablet, AirtalTM (Dae-Woong Pharmaceutical Co., Ltd.) and aceclofenac soft capsule, Clanza STM (Korea United Pharmaceutical Co., Ltd.) was evaluated according to the guideline of KFDA. Fourteen normal male volunteers (age 20-25 years old) were divided into two groups and a randomized 2?´?2 cross-over study was employed. After oral administration of one tablet or capsule containing 100mg of aceclofenac, blood was taken at predetermined time intervals and the concentration of aceclofenac in plasma was determined with an HPLC method under UV detector. The pharmacokinetic parameters (Cmax, Tmax and AUCt) were calculated and ANOVA was utilized for the statistical analysis of parameters using logarithmetically transformed AUCt, Cmax and Tmax. The results showed that the differences in AUCt, Cmax and Tmax between Airtal tablet and Clanza soft capsule were 2.89%, 0.18% and 43.0%, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) (e.g. log(0.81)-log(1.23) and log(0.89)-log(1.14)) for AUCt and Cmax, respectively. Thus, the criteria of the KFDA guidelines for the equivalence was satisfied, indicating that Clanza STM soft capsule is bioequivalent to AirtalTM tablet.