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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 in vitro release of tectoridin floating sustained-release tablets (TFSRT), pharmacokinetics in vivo and in vitro and in vivo in rabbits. Methods The artificial gastric juice was used as medium and the in vitro release characteristics of TFSRT were investigated by HPLC. Six Japanese white rabbits were crossed with each other. A single dose of TFSRT and 200 mg of tectorigenin suspension were respectively administered. The plasma concentration of tectorigenin was determined by HPLC. Data were analyzed by PKsolver 2.0 pharmacokinetic software. Results The cumulative release of TFSRT in 10 h was more than 70%. The pharmacokinetics in rabbits showed that the TFSRT and the tectorigenin suspension all fit the single-compartment model. The pharmacokinetic parameters tmax were (2.809 ± 0.371), (0.442 ± 0.138) h and (Cmax) were 6.317 ± 1.337, (9.662 ± 2.759) μg / m L and AUC0 ~ t were (74.156 ± 10.420) and (57.059 ± 13.309) μg? H / m L, respectively. There was significant difference between the two groups (P <0.05,0.01). The bioavailability of TFSRT was (134.63 ± 27.94)% relative to the tectorigenin suspension. Conclusion TFSRT achieves the goal of slow release and significantly improves the bioavailability. Its absorption in vivo has a good correlation with in vitro release (r = 0.987 9), indicating that in vitro release can be used to control the quality of its preparation.