论文部分内容阅读
目的以溴吡斯的明普通片为对照,通过多剂量口服给药后,评价溴吡斯的明缓释片在兔体内的药动学和生物利用度。方法 6只新西兰兔随机分成两组,采用自身交叉对照实验,多剂量口服溴吡斯的明缓释制片(90mg/次,2次/d)或普通片(60mg/次,3次/d)后,采用高效液相色谱法测定血浆中溴吡斯的明浓度。计算药动学参数和相对生物利用度。结果家兔体内血浆中药物浓度随时间的变化符合血管外给药二室模型。溴吡斯的明普通片与缓释片给药药动学参数如下:tmax分别为(2.00±0)h和(4.00±0)h;Cmax分别为(25.48±0.18)mg/L和(19.24±0.45)mg/L;AUC0-∞分别为(321.42±5.00)mg.h.L-1和(370.08±12.23)mg.h.L-1。与普通片相比,缓释片的相对生物利用度为119.15%。结论溴吡斯的明缓释片具有缓释动力学特征,与普通片生物等效。
OBJECTIVE To compare the pharmacokinetics and bioavailability of triptorelin tablets in rabbits after oral administration of multiple doses of triptolide. Methods Six New Zealand white rabbits were randomly divided into two groups. The self-controlled crossover study was conducted. The multi-dose oral administration of pyridostimuric acid (90mg / time, twice daily) or ordinary tablets (60mg / time, ), The plasma concentration of pyridostigmine was determined by high performance liquid chromatography. Pharmacokinetic parameters and relative bioavailability were calculated. Results The change of plasma concentration in rabbits with time was in accordance with the two-compartment model of extravascular administration. The pharmacokinetic parameters of triptorelin tablets and sustained release tablets were as follows: tmax was (2.00 ± 0) h and (4.00 ± 0) h respectively; Cmax was (25.48 ± 0.18) mg / L and ± 0.45) mg / L; AUC0-∞ were (321.42 ± 5.00) mg.hL-1 and (370.08 ± 12.23) mg.hL-1, respectively. The relative bioavailability of extended release tablets was 119.15% compared to tablets. Conclusion: The sustained release tablets of triptorelin tablets have sustained-release kinetic characteristics and are bioequivalent to common tablets.