阿奇霉素颗粒剂的健康人体药物动力学和相对生物利用度

Relative bioavailability and pharmacokinetics of azithromycin in healthy volunteers

目的 :研究阿奇霉素颗粒剂的健康人体相对生物利用度及生物等效性。方法 :8名健康受试者单剂量交叉口服阿奇霉素颗粒剂和胶囊 10 0 0mg后 ,采用微生物法测定用药后不同时间血清和尿中药物质量浓度。结果 :二者体内过程符合二房室模型 ,AUC分别为 (16 .6 9± 3.2 0 )mg·h·L-1和 (16 .95± 3.0 9)mg·h·L-1,Cmax为 (1.77±0 .42 )mg·L-1和 (1.78± 0 .6 3)mg·L-1,Tmax为 (1.88± 0 .6 4)h和 (1.88± 0 .35 )h ,2种制剂药物动力学参数及 192h尿中总排泄率差异均无显著性 (P >0 .0 5 )。阿奇霉素颗粒剂的相对生物利用度为 (10 1.97± 10 .46 ) %。结论

Aim: To study the pharmacokinetics and relative bioavailability of azithromycin in healthy volunteers. Methods: The serum concentraions of azithromycin of two formulations were determined in 8 healthy male volunteers after an oral dose of 1000 mg azithromycin granules or capsules in crossways. The serum and urine samples were collected at various periods after oral administration. The serum and urine concentrations of azithromycin were determined by microbiological method. Results: The concentration time curves of azithromycin granules and capsules were fitted to the two compartment open model. The C max values were (1.77±0.42)mg/L and (1.78±0.63) mg/L,the T\- max values were (1.88±0.64) h and (1.88±0.35) h and the AUC were (16.69±3.20) mg·h·L -1 and (16.95±3.09) mg·h·L -1 , respectively. The relative bioavailability of granules to capsules were (101.97±10.46)%. Conclusion: It is suggested that the 2 formulations are bioequivalent.