鸢尾苷元胃内漂浮缓释片兔体内药动学及其体内外相关性研究  

In vivo pharmacokinetics of tectorigenin floating sustained-release tablets in rabbits and evaluation of in vitro-in vivo correlation

作　　者：王金凤[1] 王芳[1] 杨翠燕[1] 王国玉[1] 魏颖[1] 赵楠[1] 赵庆兰[1] 

机构地区：[1]中国人民解放军第二○八医院,吉林长春130062

出　　处：《中草药》2017年第2期266-271,共6页Chinese Traditional and Herbal Drugs

基　　金：吉林省科技发展计划项目(20140204040YY)

摘　　要：目的评价鸢尾苷元胃内漂浮缓释片(TFSRT)的体外释药特性、兔体内药动学及其体内外相关性。方法以人工胃液为介质,HPLC法考察TFSRT的体外释放特性。以6只日本大耳白兔自身交叉对照,单剂量ig给予TFSRT和鸢尾苷元悬浮液各200 mg,HPLC法测定血浆鸢尾苷元质量浓度,并用PKsolver 2.0药动学软件进行数据处理。结果 TFSRT体外10 h累积释放度大于70%。兔体内药动学表明TFSRT和鸢尾苷元悬浮液均符合单室模型特征,药动学参数:tmax分别为(2.809±0.371)、(0.442±0.138)h,Cmax分别为(6.317±1.337)、(9.662±2.759)μg/m L,AUC0~t分别为(74.156±10.420)、(57.059±13.309)μg?h/m L,两者比较均有显著性差异(P<0.05、0.01)。TFSRT相对鸢尾苷元悬浮液的生物利用度为(134.63±27.94)%。结论 TFSRT达到了缓慢释药、显著提高生物利用度的设计目的;其体内吸收与体外释药具有良好的相关性(r=0.987 9),表明可以采用体外释放度来控制其制剂质量。Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of tectorigenin floating sustained-release tablets（TFSRT）. Methods The release characteristics of TFSRT in vitro was detected with HPLC in the artificial gastric fluid. Six Japanese Giant Ear Rabbits as self crossover control, which were given TFSRT and suspension liquid（200 mg）. The concentration of tectorigenin in plasma was determined with HPLC and the data were processed with PKsolver 2.0 software. Results The cumulative release rate of TFSRT in vitro was over 70% in 10 h. The pharmacokinetics in rabbits showed that TFSRT and tectorigenin suspension liquid conformed to the single compartment model and the pharmacokinetic parameters were obtained： tmax：（2.809 ± 0.371） and（0.442 ± 0.138） h, Cmax：（6.317 ± 1.337） and（9.662 ± 2.759） μg/m L, AUC0—t：（74.156 ± 10.420） and（57.059 ± 13.309） μg？h/m L. The relative bioavailability of TFSRT was（134.63 ± 27.94）%, so there was significant difference between them. Conclusion TFSRT can release slowly, so it increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro is fine（r = 0.987 9）, so the release rate in vitro can control the quality of TFSRT.

关 键 词：鸢尾苷元 胃内漂浮缓释片 释放度 药动学 体内外相关性 体外释药特性 HPLC 单室模型 生物利用度 

分 类 号：R286.02[医药卫生—中药学]