摘要
目的 :研究克拉霉素胶囊在正常人体内的药动学与相对生物利用度。方法 :以藤黄八叠球菌 2 80 0 1为敏感菌株 ,采用微生物法测定 10名健康志愿受试者 po单剂量克拉霉素胶囊和进口片剂 (5 0 0mg)后血清中克拉霉素的浓度 ;以PKBP N1程序处理测定结果 ,计算药动学参数 ;用双单侧t检验法和配对t检验法对主要的药动学参数进行统计分析 ,评价二者的生物等效性。结果 :微生物法的最低检测浓度为 0 .0 5 μg·ml-1,线性范围 0 .0 5～ 4.0 0 μg·ml-1,回收率为 99.0 4%～ 10 1.48% ,RSD≤8.2 0 % ;克拉霉素在人体内的药动学行为均符合一级吸收的开放一室模型 ,二者的达峰时间分别为 (1.45± 0 .5 0 )h和 (1.5 5± 0 .44 )h ,峰浓度分别为 (2 .2 0± 0 .39) μg·ml-1和 (2 .15± 0 .33) μg·ml-1,血浓经时曲线下面积分别为 (17.6 0± 2 .85 ) μg·h·ml-1和 (17.74± 3.46 ) μg·h·ml-1。结论 :以克拉霉素进口片为参比 ,计算得克拉霉素胶囊的相对生物利用度为 10 1.6 4% ,二者生物等效。
OBJECTIVE:To study the pharmacokinetics and relative bioavailability of clarithromycin capsule.METHODS:A microbiological agar diffusion assay using Micrococcus luteus (ATCC 28001) was used as a bioassay for clarithromycin in serum following a single oral dose 500 mg of clarithromycin capsule and tablet respectively given to 10 healthy volunteers in an open randomized cross over test.The data obtained were fitted with PKBP N1 program.RESULTS:A linear relationship was obtained between the peak area ratio and the concentration of clarithromycin from 0.05 to 4.00 μg·ml -1 and the lowest limit of detection of clarithromycin in serum was 0.05 μg·ml -1 .Precisions were under 8.20%.The recoveries were 99.04%～101.48%.The one compartment open model with first order absorption was used to described the time course of serum concentrations of clarithromycin in human following administration of a single oral dose 500 mg as capsule and tablet.The results were t peak =(1.45±0.50) h and (1.55±0.44) h,c max =(2.20± 0.39 ) μg·ml -1 and (2.15±0.33) μg·ml -1 ,AUC=(17.60±2.85) μg·h·ml -1 and (17.74±3.46) μg·h·ml -1 .CONCLUSION:There were no significant differneces between their pharmacokinetic parameters.The tested capsule and the reference tablet is bioequivalent with F rel =101.64%.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2000年第4期254-257,共4页
Chinese Pharmaceutical Journal
