岩白菜素包合物渗透泵片的Beagle犬体内药动学研究  

Pharmacokinetics of bergenin inclusion complex osmotic pump tablets in Beagle dogs

作　　者：吴敏[1] 谢佳[2] 曾建[1] 刘洪[2] 李德银[1] 

机构地区：[1]成都医学院药学院,成都610081 [2]四川省天然药物研究所,成都610041

出　　处：《中国新药杂志》2013年第4期465-468,494,共5页Chinese Journal of New Drugs

基　　金：成都医学院2009年科研基金(CYZ09-011)

摘　　要：目的:研究岩白菜素包合物渗透泵片在Beagle犬体内的药动学,对体外释放和体内吸收的相关性做出评价,确认其处方设计的合理性。方法:按照《中华人民共和国药典》附录中转篮法测定体外释放度,以岩白菜素普通片为对照,采用HPLC-DAD测定犬血浆中岩白菜素浓度。采用Loo-Riegelman法计算药物体内吸收百分率。结果:体外释放度数据(R)与相应各时间点的体内药物吸收百分率(F)回归方程为:F=0.88R+4.262(r=0.923 0,P<0.01)。结论:岩白菜素包合物渗透泵片体内吸收和体外释放相关性良好,与普通片相比可有效促进药物的体内吸收。Objective： To investigate the pharmacokinetics of bergenin inclusion complex osmotic pump tablets in beagle dogs, and its in vitro-in vivo correlation and rationality of formulation design. Methods： The in vitro release was tested according to Pharmacopoeia of the People＇s Republic of China, Method 1 of Appendices XC. The HPLC-DAD methods were developed and validated for bergenin assay in plasma samples using bergenin conventional tablets as reference preparation, and the in vivo pharmacokinetics was studied by Loo-Riegelman method. Results： The linear regressive equation was established between the absorption percentage in vivo and the accumulated release percentage in vitro of bergenin as F = 0.88R ＋ 4. 262 （r = 0. 923 0, P 〈 0.01 ）. Conclusion ： There is a significant correlation between the in vivo absorption and the in vitro release of bergenin inclusion complex osmotic pump tablets, and it can effectively promote drug absorption in vivo compared with the conventional tablets.

关 键 词：岩白菜素 渗透泵片 Loo-Riegelman法 体内外相关性 

分 类 号：R969.1[医药卫生—药理学]