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目的:研究自制的硝苯啶缓释微球在兔体内的药物动力学及生物利用度。方法:以瑞士产硝苯啶缓释片为参比对照品,以组间对照方式,给予新西兰兔单剂量口服10mg缓释微球和对照品。用毛细管气相色谱法测定血浆中药物浓度。结果:硝苯啶缓释微球相对于缓释片的生物利用度为99.7%,两种制剂的达峰时间、达峰浓度和体内驻留时间等参数均无显著性差异(P>0.05)。微球的体内吸收百分率与体外溶出百分率呈显著相关性(P<0.01)。结论:自制的硝苯啶缓释微球具有较好的生物利用度和缓释作用,与进口缓释片剂具有生物等价性。
Objective: To study the pharmacokinetics and bioavailability of self-made nifedipine microspheres in rabbits. Methods: The nifedipine sustained-release tablets made in Switzerland were taken as reference substance, and 10mg sustained-release microspheres and reference substance were given orally to single-dose New Zealand rabbits in a controlled manner. Determination of plasma drug concentration by capillary gas chromatography. Results: The bioavailability of nifedipine microspheres was 99.7% compared with that of sustained-release tablets. There was no significant difference in peak time, peak concentration and in vivo residence time between the two preparations (P> 0.05). The percentage of in vivo absorption of microspheres was significantly correlated with the percentage of in vitro dissolution (P <0.01). CONCLUSION: Self-made nifedipine sustained-release microspheres have good bioavailability and sustained-release properties and are bioequivalent to imported sustained-release tablets.