伐昔洛韦缓释片体外释放速率与人体内吸收速率的相关性

Correlation between dissolution rate in vitro and absorption rate in vivo of valaciclovir sustained release tablets

目的:研究伐昔洛韦缓释片体外释放速率与人体内吸收速率的相关性。方法:以水为释放介质,测定伐昔洛韦缓释片的体外释放速率;采用Wagner-Nelson法计算单剂量口服缓释片后体内吸收分数,考察吸收相体内吸收与体外释放的相关性。结果:伐昔洛韦缓释片体内吸收分数(f_a)与体外释放速率(f_r)的关系为:f_a=2.11f_r -20.12,r=0.994 0(n=5)。结论:伐昔洛韦缓释片人体内外相关性良好(P<0.001)。

AIM： To explore the in vivo-in vitro correlation of valaciclovir sustained release tablets （VSRT） . METHODS： In vitro release rate of VSRT was studied by the Chp basket method using the following conditions： in 900 ml of water at （37.5 ± 0.5） ℃ at a rotation speed of 100 rpm. In vivo bioavailability was tested in twenty healthy male volunteers and the fractions absorbed were calculated by Wagner-nelson method. RESULTS： The relationship between the release fraction （fr） and the absorption fraction （fa） was： fa =2.11 fr - 20.12, r = 0.994 0 （n = 5） . CONCLUSION： There is a good correlationship of VSRT between dissolution rate in vitro and absorption rate in vivo.