萘哌地尔缓释片犬体内外相关性的研究

The Study of the In Vivo-In Vitro Correlation of the Naftopidil Sustained-release Tablet in Dog

对萘哌地尔(NAF)缓释片体外释放和家犬体内吸收之间的相关性进行研究。以人工胃液为介质,测定萘哌地尔缓释片的体外释放度(X),同时测定家犬单剂顿服100 m g萘哌地尔普通片/缓释片后的血药浓度,分别采用W-N法和逆卷积法计算萘哌地尔缓释片在家犬体内不同时间的吸收分数(F)/体内吸收量(A);以F或A对相应时间点的X进行线性回归,回归方程分别为:F=2.1533X-27.636,r=0.9927;A=2.3452X-25.474,r=0.9938。两种方法均表明NAF缓释片的体外释放与家犬的体内吸收之间相关性良好。

We studied the correlation of sustained-release tablet of naftopidil between the in vitro release and the in vivo absorption in the dog. The release rate （X） of naftopidil sustained-release tablet in artificial gastric fluid was determined and the naftopidil concertration in plasma was determined after a single oral dose of 100 mg naftopidil （tablet or sustained-release tablet） in the dog. The absorbed fraction （F） and in vivo absorption rate （A） of the NAF sustained-release tablet in the dog at different time were calculated by W-N method and deconvolution method,respectively. Then the regression equations beteween F or A and X of the corresponding time point were obtained：F=2. 1533X-27. 636（r=0. 9927）and A=2. 3452X-25. 474（r=0. 9938）. W-N method and deconvolution method both indicated that the correlation between the in vitro release and the in vivo absorption in the dog of the NAF sustained-release tablet was good.