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目的研究溴吡斯的明缓释片与其普通片在兔体内的药代动力学与相对生物利用度。方法 6只新西兰兔随机分成2组,采用自身交叉对照实验,单剂量口服溴吡斯的明缓释片或普通片后,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。结果溴吡斯的明普通片与缓释片给药后,药动学参数如下:tmax分别为2 h和4 h;Cmax分别为(17.944±0.991)mg/L和(15.442±0.215)mg/L;AUC0-∞分别为(201.956±4.623)mg/(h.L)和(200.557±3.357)mg/(h.L);与普通片相比,缓释片的相对生物利用度为102.89%。结论溴吡斯的明缓释片有明显的缓释效果,与普通片生物等效。
OBJECTIVE To study the pharmacokinetics and relative bioavailability of triptorelin sustained-release tablets and its common tablets in rabbits. Methods Six New Zealand white rabbits were randomly divided into two groups. After self-controlled crossover test, single-dose oral administration of pyridostigmine or conventional tablets was used to determine the concentration of triptolide in plasma by HPLC. Kinetic parameters and relative bioavailability. Results The pharmacokinetic parameters of triptolide tablets and sustained-release tablets were as follows: tmax was 2 h and 4 h respectively; Cmax was (17.944 ± 0.991) mg / L and (15.442 ± 0.215) mg / L and AUC0-∞ were (201.956 ± 4.623) mg / (hL) and (200.557 ± 3.357) mg / (hL), respectively. The relative bioavailability of sustained-release tablets was 102.89% Conclusion Bromopylamine sustained release tablets have a sustained release effect, which is bioequivalent to ordinary tablets.