摘要
目的研究2种国产头孢丙烯片(头孢类抗生素)在健康人体内的药代动力学过程,并评价这2种制剂的生物等效性。方法20例健康成年男性受试者随机分组,自身对照,单次口服头孢丙烯片1 g后,用高效液相色谱法测定头孢丙烯顺式及反式异构体的血浆浓度,用非房室模型法计算各主要药代动力学参数,并进行方差分析和生物等效性评价。结果顺式异构体:参比制剂与受试制剂的tm ax分别为(2.4±1.0),(2.3±0.8)h;Cm ax分别为(15.4±3.5),(14.8±2.8)μg.mL-1;t1/2分别为(1.4±0.1),(1.4±0.1)h;MRT分别为(3.4±0.6),(3.4±0.6)h;AUC0-t分别为(61.2±10.6),(60.3±11.4)μg.h.mL-1;AUC0-∞分别为(64.7±11.2),(64.5±11.7)μg.h.mL-1;受试制剂相对于参比制剂的生物利用度为(99.3±14.5)%。反式异构体:参比制剂与受试制剂的tm ax分别为(2.4±0.9),(2.4±0.9)h;Cm ax分别为(1.6±0.3),(1.5±0.3)μg.mL-1;t1/2分别为(1.2±0.2),(1.5±0.6)h;MRT分别为(3.2±0.7),(3.2±0.7)h;AUC0-t分别为(6.1±1.4),(5.6±1.3)μg.h.mL-1;AUC0-∞分别为(6.1±1.4),(5.6±1.3)μg.h.mL-1;受试制剂相对于参比制剂的生物利用度为(94.0±17.5)%。结论受试制剂与参比制剂具有生物等效性。
Objective To study the pharmacokinetics and bioequivalence of two demostic cefprozil tablets. Methods Twenty healthy volunteers were randomized into two groups, whose plasma concentrations of cis and trans isomers of eefprozil were determined at different time after single oral dose of 1 g cefprozil tablets by own control by HPLC method. The pharmacokinetie parameters were computed and which were experienced variance analysis. Results Cis eefprozil： the main pharmacokinetic parameters of reference and trial eefprozil tablets were as follows： tmax were （2.4±1.0）,（2.3 ±0.8） h;Cmax were （15.4 ±3.5）,（14.8 ±2.8） μg · mL^-1;t1/2 were （1.4±0.1）,（1.4±0.1） h;MRT were （3.4±0.6）,（3.4±0.6） h;AUC0-1 were （61.2±10.6）,（60.3± 11.4） μg ·h· mL^-1;AUC0-∞ were （64.7±11.2）,（64.5±11.7） μg · h · mL^-1, respectively. Trans cefprozil： the relative bioavailability of the trial preparation was （99.3 ± 14.5 ） %. Trans eefprozil ： the main pharmaeokinetic parameters of reference and trial eefprozil tablets were as follows ： tmax were （ 2. 4 ± 0. 9 ）, （ 2. 4±0. 9 ） h ; Cmax were （ 1.6 ± 0. 3 ）, （ 1. 5± 0. 3 ） μg · mL^-1 ; t1/2 were （ 1.2± 0.2）,（1.5±0.6） h;MRT were （3.2±0.7）,（3.2±0.7） h;AUC0-1 were （6.1 ±1.4）,（5.6 ±1.3） μg · h· mL^-1; AUC0-∞ were （6. 1± 1.4）, （5.6 ± 1.3）μg ·h· mL^-1, respectively. The relative bioavailahility of the trial preparation was （94. 0 ± 17.5 ）%. Conclusion The results shows that the trial preparation and the reference preparation of cefprozil were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2010年第1期23-27,共5页
The Chinese Journal of Clinical Pharmacology
