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目的 :研究阿奇霉素国产分散片与进口片剂人体相对生物利用度及药物动力学。方法 :12名健康受试者自身交叉单剂量口服阿奇霉素国产分散片和进口片剂各 5 0 0mg ,定时取血 ,用微生物法测定血药浓度。结果 :受试制剂国产阿奇霉素分散片与参比制剂进口片剂的血药浓度时间曲线基本一致 ,符合一级吸收二房室模型。国产分散片、进口片两种制剂的主要药动学参数分别为 :消除半衰期t1/ 2 β:(45 .2± 10 .3)h ,(45 .7± 9.2 )h ;Tmax:(1.3± 0 .6 )h ,(2 .0± 1.0 )h ;Cmax:(414.7± 12 3.8) μg·L-1,(35 2 .5± 92 .1) μg·L-1。药动学参数经配对t检验 ,P >0 .0 5 ,差异均无显著性。两种制剂的药时曲线下面积AUC0→tn平均值分别为 :国产分散片 (480 4.2± 95 7.6 ) μg·L-1·h-1,进口片剂 :(5 10 9.8± 10 10 .5 ) μg·L-1·h-1;国产分散片的相对生物利用度为 :F =(94.7± 13.4) %。结论 :统计学结果表明受试制剂国产阿奇霉素分散片与参比制剂生物等效。
Objective: To study the relative bioavailability and pharmacokinetics of azithromycin domestic dispersible tablets and imported tablets. Methods: Twelve healthy subjects were crossed with single doses of oral azithromycin oral tablets and imported tablets of 500 mg, blood was taken regularly, and the plasma concentration was determined by the microbiological method. Results: The time curve of the plasma concentration of the azithromycin dispersible tablets and reference tablets was basically consistent with that of the first-order absorption two-compartment model. The main pharmacokinetic parameters of domestic dispersible tablets and imported tablets were as follows: elimination half-life t1 / 2 β: (45.2 ± 10.3) h, (45.7 ± 9.2) h; Tmax: (1.3 ± 0 .6) h, (2.0 ± 1.0) h; Cmax: (414.7 ± 12 3.8) μg · L-1, (35 2 .5 ± 92.1) μg · L-1. Pharmacokinetic parameters by paired t test, P> 0. 05, the difference was not significant. The average area under the curve of AUC0 → tn of the two preparations were respectively: domestic dispersible tablets (480 4.2 ± 95 7.6) μg · L-1 · h-1, imported tablets: (5 10 9.8 ± 10 10 .5 ) μg · L-1 · h-1. The relative bioavailability of domestic dispersible tablets was: F = (94.7 ± 13.4)%. Conclusions: The statistical results show that the domestic preparation of azithromycin dispersible tablets and reference formulations bioequivalence.