Chi S C, Jun H W
Department of Pharmaceutics, University of Georgia, Athens 30602.
J Pharm Sci. 1990 Nov;79(11):974-7. doi: 10.1002/jps.2600791106.
The anti-inflammatory activity of a 1% ketoprofen gel containing 20% Pluronic F-127 was evaluated using the carrageenan-induced rat paw edema method. The activity of the gel was compared with that of other topical nonsteroidal anti-inflammatory drug (NSAID) preparations. The Pluronic gel formulation was significantly more effective against edema formation than other ketoprofen gels used. The 1% ketoprofen gel in the Pluronic base inhibited 53% of the carrageenan-induced edema formation as compared with 38% inhibition obtained with a 3% ketoprofen gel in a Carbopol-based formulation. The topical ED50 of the 1% ketoprofen gel was 2.2 mg/kg whereas the oral ED50 of ketoprofen in a suspension was 6.1 mg/kg, indicating that the relative equiponderal availability of the topical gel was nearly three times that of the oral suspension. The application of 50 mg of the 1% ketoprofen gel on the rat hind paw at various time intervals from 0 to 24 h prior to the carrageenan injection significantly inhibited edema formation in all groups of dosed rats. A significant correlation was found between the percent inhibition of rat paw edema and the log dose of ketoprofen injected subplantarly for the dose range between 0.1 and 10 micrograms/paw.
采用角叉菜胶诱导的大鼠足爪水肿法,评估了含20%普朗尼克F - 127的1%酮洛芬凝胶的抗炎活性。将该凝胶的活性与其他局部用非甾体抗炎药(NSAID)制剂的活性进行了比较。与所用的其他酮洛芬凝胶相比,普朗尼克凝胶制剂在抑制水肿形成方面显著更有效。与基于卡波姆的制剂中3%酮洛芬凝胶产生38%的抑制作用相比,普朗尼克基质中的1%酮洛芬凝胶抑制了53%的角叉菜胶诱导的水肿形成。1%酮洛芬凝胶的局部半数有效剂量(ED50)为2.2mg/kg,而酮洛芬混悬液的口服ED50为6.1mg/kg,这表明局部凝胶的相对等效可用性几乎是口服混悬液的三倍。在注射角叉菜胶前0至24小时的不同时间间隔,在大鼠后足爪上涂抹50mg的1%酮洛芬凝胶,在所有给药组大鼠中均显著抑制了水肿形成。在0.1至10微克/爪的剂量范围内,发现大鼠足爪水肿抑制百分比与足底注射酮洛芬的对数剂量之间存在显著相关性。