司丙红霉素胶囊的药物动力学  

Pharmacokinetics of erythromycin stinoprate capsule

作　　者：王黎青[1] 胡哲益[1] 余奇[1] 郭歆[1] 熊静[1] 黄志壮[1] 程泽能[1] 

机构地区：[1]中南大学药学院生物药剂学教研室,长沙410014

出　　处：《中南大学学报（医学版）》2005年第2期197-201,共5页Journal of Central South University ：Medical Science

摘　　要：目的:研究司丙红霉素胶囊的药物动力学,为该药进行临床研究提供依据。方法:采用随机、开放试验设计, 30名健康受试者(男女各半),随机分为3组,每组男女各5人。各组分别单剂量口服试验制剂250, 500和750mg。采用HPLC MS法测定给药后不同时间丙酸红霉素和红霉素碱的血药浓度。结果: 30例健康志愿者,全部完成试验,未发生药物不良反应。用3P87软件进行模型分析和参数计算,高、中、低3个剂量组均符合单室模型。口服司丙红霉素胶囊后,丙酸红霉素药物动力学参数为:低剂量组Ka为( 2. 007±1. 281 ) /h,tmax(实测值)为(1. 9±0. 6)h,Cmax为(437. 0±295. 0)μg/L,AUC0-14为(1840. 2±1476. 87 )μg·h/L,Ke为( 0. 329±0. 119 ) /h,T1 /2为(2. 45±0. 9)h;中剂量组Ka为(1. 451±0. 380) /h,tmax(实测值)为(1. 7±0. 3)h,Cmax为(923. 1±217. 5 )μg/L,AUC0-14为(4542. 4±1579. 4 )μg·h/L,Ke为( 0. 237±0. 057 ) /h,T1 /2为( 3. 1±1. 1 )h;高剂量组Ka为(2. 076±1. 559) /h,tmax(实测值)为(1. 7±0. 3)h,Cmax为(1336. 5±366. 0)μg/L,AUC0-14为(7481. 5±2496. 2 )μg·h/L,Ke为(0. 266±0. 051) /h,T1 /2为(2. 7±0. 5 )h。红霉素碱的药物动力学参数为:低剂量Ka为( 1. 410±0. 626) /h,tmax(实测值)为(1. 8?Objective To determine the pharmacokinetics of erythromycin stinoprate capsules and to provide guidance for clinical research. Methods Thirty healthy volunteers (15 men and 15 women) were divided into 3 groups randomly, each including 5 men and 5 women. Single oral doses of 250, 500 and 750 mg were given to each volunteer. The concentrations of erythromycin propionate and erythromycin base in the plasma were determined by HPLC-MS. Results All 30 volunteers completed the experiment without adverse reactions. Using 3P87 we analyzed the model and calculated the pharmacokinetic parameters. Three dose groups taking high, middle and low dose were all single compartment model. The pharmacokinetic parameters of erythromycin propionate after taking erythromycin stinoprate capsules were as follows: Low dose group: Ka (2.007±1.281)/h,t max (actual value)(1.9±0.6) h,C max (437.0±295.0) μg/L,AUC 0-14 (trapezoid area) (1840.2±1476.87) μg·h/L,Ke (0.329±0.119)/h,T 1/2 (2.45±0.9) h. Middle dose group: Ka (1.451±0.380)/h, t max (1.7±0.3) h, C max (923.1± 217.5) μg/L,AUC 0-14 (4542.4±1579.4) μg·h/L,Ke (0.237±0.057)/h,T 1/2 (3.1±1.1) h; High dose group: Ka (2.076±1.559)/h,t max (1.7±0.3) h,C max (1336.5±366.0) μg/L,AUC 0-14 (7481.5±2496.2) μg·h/L,Ke (0.266±0.051)/h,T 1/2 (2.7±0.5) h. The pharmacokinetic parameters of erythromycin were as follows: Low dose group: Ka (1.410±0.626)/h, t max (1.8± 0.5) h, C max (197.5±227.6) μg/L, AUC 0-14 (766.4±981.0) μg·h/L,Ke (0.519±0.240)/h, T 1/2 (1.6±0.8) h. Middle dose group: Ka (1.900±1.049)/h,t max (1.6±0.2) h,C max ( 488.3±216.7) μg/L,AUC 0-14 ( 488.3±216.7) μg/L,Ke (0.329±0.057)/h,T 1/2 ( 2.2±0.4) h; High dose group: Ka (1.934±0.794)/h,t max (1.7±0.3) h,C max ( 749.3±387.2) μg/L,AUC 0-14 (3820.1±1966.4) μg·h/L,Ke (0.373±0.174)/h,T 1/2 ( 2.2±0.7) h. AUC of both erythromycin propionat

关 键 词：司丙红霉素 胶囊 药物动力学参数 HPLC-MS法 药物不良反应 性别差异 健康受试者 单剂量口服 健康志愿者 半衰期 临床研究 试验设计 试验制剂 血药浓度 不同时间 参数计算 模型分析 单室模型 线性关系 活性成分 体内代谢 

分 类 号：R969.2[医药卫生—药理学]