头孢丙烯分散片的人体药动学和生物等效性  

Study on Pharmacokinetics and Bioequivalence of Cefprozil Dispersible Tablets in Healthy Volunteers

作　　者：马昌[1] 刘心霞[1] 袁世英[1] 邱湘君[2] 王静[1] 顾世芬[1] 陈汇[1] 

机构地区：[1]华中科技大学同济医学院临床药理研究所,武汉430030 [2]河南科技大学医学院药理系

出　　处：《中国药师》2011年第12期1746-1748,共3页China Pharmacist

摘　　要：目的:建立高效液相色谱并同时测定人血浆中的顺式和反式头孢丙烯,对头孢丙烯分散片进行人体药物动力学和生物等效性研究。方法:将20名男性健康志愿者随机分两组进行两制剂双周期随机交叉试验,单次口服头孢丙烯分散片受试制剂或参比制剂500 mg,清洗期为7 d。用HPLC法测定血浆中头孢丙烯浓度,计算其药动学参数。结果:血浆中杂质不干扰样品的测定,标准曲线范围为0.10～20.0μg·ml^(-1),线性关系良好(r=0.999 7),最低定量限为0.10μg·ml^(-1);受试制剂和参比制剂中头孢丙烯的AUC_(0～t)分别为(30.26±4.65)μg·h·ml^(-1)和(31.29±5.42)μg·h·ml^(-1),AUC_(0～∞)分别为(30.73±4.75)μg·h·ml^(-1)和(31.78±5.62)μg.h·ml^(-1),C_(max)分别为(9.39±1.29)μg·ml^(-1)和(9.30±1.63)μg·ml^(-1),t_(max)分别为(1.53±0.49)h和(1.70±0.25)h,t_(1/2)分别为(1.52±0.20)h和(1.49±0.20)h,受试制剂的相对生物利用度为:(97.9±13.9)%。结论:分析方法操作简便,结果准确可靠。统计分析表明,两制剂具有生物等效性。Objective： To determine cefprozil in human plasma by HPLC method in order to evaluate the pharmacokinetics and bioequivalence of cefprozil dispersible tablets in healthy volunteers. Method： 20 healthy male volunteers were randomly divided into two groups for single dose, double period randomized cross-over trial, and the group was given 500mg test and reference tablets, respectively with wash-out period of 7 days. The drug concentrations in plasma samples were analyzed by HPLC, and the pharmacokinetic parameters were calculated. Result： Standard curve range was within 0. 10 -20. 0 μg·ml-1 with a good linear relationship （r = 0：999 7 ）, and the lower limit of quantification was 0. 10 μg·ml-1. For the cefprozil in the test and reference preparation,AUC0-t was （30. 26±4. 65） μg·h·ml-1 and （31.29 ±5.42） μg·h·ml-1,AUC0-∞ was （30.73±4. 75） μg·h·ml-1 and （31.78 ±5.62） μg·h·ml-1 ,Cmax was （9.39 ± 1.29） μg·ml-1 and （9. 30 ± 1.63 ） μg·ml-1, tmax was （ 1.53 ± 0. 49） h and （ 1.70 ± 0. 25 ） h and t1/2 was （ 1.52 ± 0. 20） h and （ 1.49 ± 0. 20） h, respectivley. The relative bioavailability of the test tablets was （97.9 ± 13.9 ） %. Conclusion： The analysis method is simple, accurate and reliable. Statistical analysis shows that the two preparations are bioequivalent.

关 键 词：头孢丙烯 生物等效性 高效液相色谱法:分散片 

分 类 号：R969.1[医药卫生—药理学]