注射用阿奇霉素的生物利用度  

Bioavailability of azithromycin for injection

作　　者：徐晓梅[1] 林文红 金燕辛 钟震球 张伟明[1] 许卫关[1] 

机构地区：[1]广东省粤北人民医院药剂科,韶关512026 [2]广东省顺峰药业有限公司科研所,顺德528300 [3]广东省韶关市药品检验所生化室,韶关512026

出　　处：《中国临床药学杂志》2002年第1期38-40,共3页Chinese Journal of Clinical Pharmacy

摘　　要：目的 :研究注射用阿奇霉素的绝对生物利用度。方法 :采取静滴、肌注给药 ,以微生物检定法测定 12名健康志愿者血中阿奇霉素的浓度 ,经 3P87程序拟合 ,计算药物动力学参数。结果 :单剂量静滴及肌注阿奇霉素 5 0 0mg后血药浓度 时间曲线分别符合恒速静滴的二室模型和有滞后时间的一级吸收的二室模型。肌注滞后时间 (t1ag)为 (0 4 4 7± 0 0 2 8)h ,静滴和肌注达峰时间 (tmax)分别为 (1 12 5± 0 2 78)h和 (1 5 75± 0 4 6 4 )h ,峰浓度 (cmax)分别为 (3 5 2 4± 0 6 5 0 )mg·L-1和 (3 16 3± 0 887)mg·L-1。血药浓度 时间曲线下面积 (AUC0→∞)分别为 (2 1 4 71± 1 5 72 )mg·h·L-1及 (19 5 4 3± 2 75 7)mg·h·L-1,清除率 (CL)分别为 (2 3 5 86± 2 32 1)L·h-1及 (2 1 5 2 5± 6 4 5 2 )L·h-1,绝对生物利用度 (F0→∞)为 91 0 2 1%。结论AIM: To study the bioaviailability of azithromycin for injections. METHODS: 500 mg azithromycin were given to 12 healthy volunteers intravenously and intramuscularly in an open randomized crossover test. Azithramycin concentrations in plasma were determined by microbiological assay method. The pharmacokinetic parameters were obtained by using 3P87 program. RESULTS: The concentration time curves of intravenously and intramuscularly given azithromycin were conformed to two compartment model with constant rate infusion and two compartment model with first order absorption and lag time. The main pharmacokinetic parameters of intravenously and intramuscularly given azithromycin were as follows: t max were (1 125±0 278) h and (1 575±0 464) h, c max were (3 524±0 650) mg·L -1 and (3 163±0 887) mg·L -1 . The AUC 0→∞ were (21 471±1 572) mg·h·L -1 and (19 543±2 757) mg·h·L -1 , the clearance rate were (23 586±2 321) L·h -1 and (21 525±6 452) L·h -1 , respectively. The lag time was (0 447±0 028) h. The absolute bioavailability ( F 0→∞ ) was 91 021%. CONCLUSION: The azithromycin for injection has higher bioavailability.

关 键 词：阿奇霉素 生物利用度 药物动力学 微生物检定法 注射剂 

分 类 号：R969[医药卫生—药理学]