摘要
目的:通过对健康志愿者连续服用国产红霉素环酯片剂后的药代动力学研究,探讨国产红霉素环11,12-碳酸酯片剂在人体内的药代动力学特征。方法:12名健康男性志愿者多剂量口服国产红霉素环11,12-碳酸酯片剂500mg,12h一次,共服8d,用微生物法测定血清、尿液中药物浓度和排泄量,检测菌为藤黄八叠菌（CMCCB 28001）。结果:受试者血药浓度-时间数据用ssd软件处理,所获得的药代动力学参数如下:t1/2为10.14±3.36h;tmax为4.33±0.62h;Cmax为2.09±0.48mg·L-1;Cssmin为1.36±0.43mg·L-1;波动百分率DF％为48.11％±14.78％;AUCssmin为19.53±5.60mg·h·L-1;清除率CL为27.59±7.73L·h-1;表观分布容积V为391.56±151.09L;72h的尿累积排出百分率为35.70％±15.79％。结论:本品多剂量给药后,血药浓度高且波动小,口服吸收量大,药物不良反应小,有利于细菌感染的治疗。
OBJECTIVE: To explore the pharmacokinetic characteristics of erythromycin cyclic 11,12-carbonate tablets in healthy volunteers. METHODS:12 male healthy volunteers were given to a multi dose of 500mg erythromycin cyclic 11,12-carbonate tablets. After administration of erythromycin cyclic 11,12-carbonate tablets, the serum level and excretion amount in urine, at different time, were determined by bacillus subtilis (CMCCB 28001) as test strain. The data were analyzed by ssd program. RESULTS: It was found that the serum concentration-time curve of the preparetion was fitted into a one-compartment model. The pharmacokinetic parameters calculated were the follows: t1/2 was 10.14±3.36h;tmax was 4.33±0.62h; Cmax was 2.093±0.478mg.L-1;C was 1.355±0.433 mg.h.L-1;DF% was 48.11±14.78%;AuCssmin was 19.53 ± 5.60mg.h.L-1;Clearance was 27.59 ± 7.73L.h-1; Apparent volume of distribution was 391.56 ± 151.09L; Accumulative excretion rate in urine throughout 0-72h period was 35.70% ± 15.79%. CONCLUSION: Compared with other erythromycins, erythromycin cyclic 11,12-carbonate was distributed more widely, excreted more slowly and it accumulative rate in urine was bigger. This is benificial to the treatment of bacterial infections.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第4期281-284,共4页
The Chinese Journal of Clinical Pharmacology
