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目的:研究国产含利福平两药复方制剂的药效学和药物动力学,评价其抗结核作用及产品质量。方法:采用试管二倍稀释法测定最低抑菌浓度,以半数动物存活时间为指标比较药物对实验性结核病的疗效。高效液相色谱法测定健康志愿者口服同剂量国产复方制剂中的利福平及利福平胶囊的血药浓度,求出其中利福平的主要药动学参数及相对生物利用度,并用双单侧t检验分析生物等效性。结果:复方制剂各成分对结核分枝杆菌的MIC均低于单独应用时各自的MIC;对小鼠试验性结核病均显著优于两者相应剂量单独应用的效果,与国外相应产品rifinah(卫非宁)比较未见显著性差异;复方制剂中的利福平与利福平胶囊的主要药动学参数t_(1/2),C_(max),AUC,t_(max)未见显著性差异,相对生物利用度生物等效性检验合格。结论:两药复合剂的抗结核作用具有协同作用;国产与进口片剂的药效学未见显著性差异;国产片中的利福平生物利用度合格。
Objective: To study the pharmacodynamics and pharmacokinetics of domestic rifampicin-containing compound preparations and evaluate the anti-TB effect and product quality. Methods: The minimum inhibitory concentration (MIC) was determined by in vitro double dilution method. The effect of drugs on experimental tuberculosis was compared with half of animal survival time as an index. The plasma concentrations of rifampicin and rifampicin capsules were determined by high performance liquid chromatography (HPLC). The main pharmacokinetic parameters and the relative bioavailability of rifampicin were obtained by using double- One-sided t-test analysis of bioequivalence. Results: The MICs of each component of Mycobacterium tuberculosis were lower than those of MICs alone. The experimental tuberculosis in mice was significantly better than that of the corresponding single dose of both, which was in good agreement with that of rifinah Ning) there was no significant difference between the two groups. The main pharmacokinetic parameters of rifampicin and rifampicin in compound preparations were as follows: t_ (1/2), C_ (max), AUC, t_ (max) , The relative bioavailability of bioequivalence test pass. Conclusion: The antituberculous effect of the two agents has a synergistic effect. There is no significant difference between the pharmacodynamics of domestic and imported tablets. The bioavailability of rifampin in domestic tablets is qualified.