国产头孢克洛临床药代动力学研究和相对生物利用度测定  

Pharmacokinetics and bioavailability of domestic cefaclor

作　　者：郭蓓宁[1] 张菁[1] 王磊[1] 张婴元[1] 

机构地区：[1]上海医科大学华山医院抗生素研究所,上海200040

出　　处：《中国新药杂志》2000年第7期466-467,共2页Chinese Journal of New Drugs

摘　　要：目的 :测定国产头孢克洛胶囊的药代动力学及相对生物利用度。方法 :8名受试者随机交叉空腹口服国产和进口头孢克洛 10 0 0mg ,用微生物方法测定药物浓度 ,计算药代动力学参数和国产品的相对生物利用度。 结果 :体内过程符合血管外二室模型 ,国产品Cmax 为 (2 0 .5 1± 3.48)mg/L ,Tmax 为 (0 .84± 0 .13)h ,t1/ 2 β为(1.0 7± 0 .38)h ,AUC为 (2 7.2 7± 2 .88)mg·h/L ,2 4h累积尿排出率为 (6 9.15± 6 .6 6 ) %。国产胶囊剂与进口胶囊剂比较的相对生物利用度为 10 8.43%。结论 :国产头孢克洛胶囊剂的生物利用度与进口胶囊剂相仿 。Objective:To determine the pharmacokinetics and relative availability of domestic cefaclor. Methods:The crossover study was conducted in 8 healthy, fast volunteers. They were treated randomly with domestic or imported cefaclor 1 000 mg and their serum and urine drug levels were measured by bioassay. RESULTS: The concentration time curves fitted to a two compartment model. The pharmacokinetic parameters of domestic cefaclor were: mean C max =(20.51±3.84) mg/L, T max =(0.84±0.13)h, t 1/2 β=(1.07±0.38)h, AUC=(27.27±2.88) mg·h/L. The cumulative excretion rate in urine within 24 h was (69.15±6.66)%. The relative bioavailability of domestic cefaclor was 108.43%. CONCLUSION: The domestic and the imported cefaclor are bioequivalent with similar bioavilability.

关 键 词：头孢克洛 药代动力学 生物利用度 药理 

分 类 号：R978.11[医药卫生—药品]