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目的:评价国产与进口环孢素胶囊的生物等效性。方法:采用随机交叉自身对照试验设计,19名健康男性志愿受试者先后单剂口服国产与进口环孢素胶囊300 mg,用HPLC法测定全血中环孢素A的浓度,以DAS1.0生物等效性评价程序处理经时血药浓度数据。结果:国产与进口环孢素A的AUC0-t分别为9045.86±1119.30μg·h·L-1和8532.17±1140.83μg·h·L-1;AUC0-∞分别为10249.03±1607.78μg·h·L-1和9373.26±1742.89μg·h·L-1;Cmax分别为1692.69±330.06μg.L-1和1645.88±292.37μg.L-1;Tmax分别为1.45±0.50h和1.33±0.43h;T1/2分别为22.20±7.81h和19.43±4.19h。以进口制剂为参比,国产环孢素胶囊的相对生物利用度为108.42±20.20%。等效性检验显示两制剂生物等效。结论:国产与进口环孢素胶囊在健康人体具有生物等效性。
Objective: To evaluate the bioequivalence of domestic and imported cyclosporin capsules. Methods: A randomized crossover self-controlled trial was designed. Nineteen healthy male volunteers were given a single oral dose of 300 mg of domestic and imported cyclosporine capsules. The concentration of cyclosporin A in whole blood was determined by HPLC. The Equivalence Evaluation program processes the temporal blood concentration data. Results: The AUC0-t of domestic and imported cyclosporin A were 9045.86 ± 1119.30μg · h · L-1 and 8532.17 ± 1140.83μg · h · L-1, respectively; the AUC0-∞ were 10249.03 ± 1607.78μg · h · L -1 and 9373.26 ± 1742.89μg · h · L-1, respectively; Cmax were 1692.69 ± 330.06μg.L-1 and 1645.88 ± 292.37μg.L-1 respectively; Tmax was 1.45 ± 0.50h and 1.33 ± 0.43h respectively; 2 were 22.20 ± 7.81h and 19.43 ± 4.19h respectively. The relative bioavailability of domestic cyclosporine capsules was 108.42 ± 20.20% with imported preparations as reference. Equivalence tests showed that both formulations were bioequivalent. Conclusion: Domestic and imported cyclosporine capsules are bioequivalent in healthy human.