阿奇霉素片在健康人体的相对生物利用度和药代动力学

Relative bioavailability and pharmacokinetics of azithromycin tablet in healthy volunteers

目的研究阿奇霉素片(大环内酯类抗生素)在健康人体的相对生物利用度及药代动力学。方法19名健康受试者自身交叉单剂量口服阿奇霉素片受试制剂和参比药物各500mg后,用微生物法测定用药后不同时间血药浓度。结果2制剂的血药浓度-时间曲线基本一致,符合二房室模型,受试制剂和参比药物的药代动力学参数:t1/2β分别为(34.61±7.42),(31.16±5.28)h;tmax分别为(2.60±0.21),(2.55±0.16)h;Cmax分别为(557.15±129.57),(548.34±137.46)μg·L-1;AUC0-tn分别为(8.45±2.29),(8.66±2.34)h·mg·L-1;受试制剂的相对生物利用度为(99.35±19.77)%。结论受试制剂与参比药物生物等效。

Objective To study the pharmacokinetics and relative bioavailability of azithromycin tablets in healthy volunteers. Methods The serum concentrations of azithromycin of two formulations were determined by microbiological assay in 19 healthy male volunteers after a single oral dose of 500 mg of azithromycin in a randomized, crossover study. The serum samples were collected at various peroids after oral administration. Results Both concentration time curves of test and reference formulations were fitted to the two compartment open modle. The main pharmacokinetic parameters were as followings： t1/2β were （34.61± 7.42 ） h and （31.16 ±5.28） h;tmax were （2.60 ±0.21 ） h and（ 2.55 ±0.16） h; Cmax were （557.15 ±129.57） μg · L^-1 and （548.34 ±137.46） μg · L^-1; AUC0-tn（8.45±2.29） h · μg· L^-1 and（8.66 ±2.34） h ·mg· L^-1. The relative bioavailability of tested to reference tablets was （99.35 ± 19.77 ） %. Conclusion The two formulations are bioequivalent .