国产罗红霉素胶囊剂的药代动力学及相对生物利用度测定

The pharmacokinetics and relative bioavailability of domestic roxithromycin

目的 :研究健康志愿者单剂口服罗红霉素胶囊剂后药代动力学及其与进口品种比较的相对生物利用度。方法 :10例受试者分别交叉空腹口服单剂国产罗红霉素胶囊剂和进口罗红霉素片剂各 30 0mg ,留取 72h内血、尿标本 ,以微生物琼脂弥散法测定其血、尿药物浓度 ,以 3P87程序计算药代动力学参数。结果 :受试者口服国产罗红霉素胶囊剂后体内过程符合血管外二室模型 ,其血药峰浓度 (Cmax)为 (10 .2 6± 2 .75 )mg·L-1,达峰时间 (Tmax)为(1.15± 0 .5 3)h ,药时曲线下面积 (AUC)为 (136 .5 1± 38.0 6 )mg·h·L-1,血清半衰期 (t1/ 2 β)为 (13.49± 2 .49)h ,72h累积尿排出率为 (10 .2 8± 3 .6 7) % ,国产罗红霉素胶囊剂与进口片剂的主要药代动力学参数以及 72h累积尿排出率均无统计学差异 (P >0 .0 5 )。以进口片剂AUC为对照 ,国产胶囊剂的相对生物利用度为 (10 3.76± 2 1.2 5 ) %。结论 :国产罗红霉素体内过程与进口罗红霉素相仿 ,两种制剂生物利用度相近 ,具生物等效性。

Objective:To study the relative bioavailability of domestic roxithromycin capsule.Methods:10 fast healthy volunteers were crossoverly treated with a single dose of 300mg domestic roxithromycin capsule or a single dose of 300mg imported roxithromycin tablet.The samples of serum and urine were collected within 72h after dosing and the serum and urine drug levels were determined by microbiological method.And the pharmacokinetic parameters were calculated with 3P87 program.Results:The pharmacokinetics of roxithromycin was fitted to two compartment model.The parameters obtained for domestic product were: C max =(10.26±2.75)mg·L -1 , T max =(1.15±0.53)h, AUC =(136.51±38.06)mg·h·L -1 , t 1/2 β=(13.49±2.49)h.The urinary accumulated excretion rate within 72h was (10.28± 3.67)%. Among these parameters there was no statistically significant difference between the two products.The relative bioavailability for domestic product was (103.76±21.25)%.Conclusion:The pharmacokinetic profile of the domestic and imported products was similar and so did the bioavailability.