替比培南匹酯在犬体内的相对生物利用度研究  

Relative Bioavailability of Tebipenem pivoxil Tablets in Dogs

作　　者：罗玉莹 周艺佳 崔佳丽 张培培 赵高琼 梅晶 刘红斌 王京昆 LUO Yuying;ZHOU Yijia;CUI Jiali;ZHANG Peipei;ZHAO Gaoqiong;MEI Jing;LIU Hongbin;WANG Jingkun(Dali University,Dali Yunnan 671000,China;Yunnan Institute of Materia Medica;Yunnan Province Company Key Laboratory for Traditional Chinese Medicine and Ethnic Drug of New Drug;School of Pharmacy,Kunming Health Vocational College)

机构地区：[1]大理大学,云南大理671000 [2]云南省药物研究所 [3]云南省中药和民族药新药创制企业重点实验室 [4]昆明卫生职业学院药学院

出　　处：《质量安全与检验检测》2021年第2期83-87,共5页QUALITY SAFETY INSPECTION AND TESTING

摘　　要：为研究禁食与进食2种条件下替比培南匹酯片(受试制剂)与替比培南匹酯颗粒(参比制剂)在Beagle犬体内的相对生物利用度,本文采用自身双交叉实验设计,8只犬分别在进食和禁食条件下单剂量口服替比培南匹酯颗粒及替比培南匹酯片。采用高效液相色谱法-串联质谱法(HPLC-MS/MS)测定给药后血浆中替比培南的浓度,计算药动学参数及相对生物利用度。结果显示受试制剂与参比制剂的主要药动学参数为:禁食状态下tmax为(1.29±0.38)和(0.94±0.28)h;cmax为(4269±1847)和(3031±1115)ng·ml^(-1);AUC(0-t)为(6893±2942)和(4628±1780)ng·h·ml^(-1);AUC(0-∞)为(6939±2948)和(4653±1777)ng·h·ml^(-1)。受试制剂替比培南匹酯片的相对生物利用度为149%。进食状态下tmax为(1.44±0.68)和(1.19±0.37)h;cmax为(3834±1321)和(2009±1179)ng·ml^(-1);AUC(0-t)为(5655±1351)和(2881±1484)ng·h·ml^(-1);AUC(0-∞)为(5757±1370)和(2940±1473)ng·h·ml^(-1)。受试制剂替比培南匹酯片的相对生物利用度为196%。可见替比培南匹酯片与替比培南匹酯颗粒在禁食与进食给药条件下二者相对利用度不一致。To study the relative bioavailability of tebipenem pivoxil tablets and tebipenem pivoxil granules in Beagle dogs under two conditions of fasting and feeding.Eight beagles were given single doses of tebipenem pivoxil granules and tebipenem pivoxil tablets respectively under feeding and fasting conditions in a self-designed double-cross experiment.The plasma tibipenem concentration was determined by HPLC-MS/MS,and calculate pharmacokinetic parameters and relative bioavailability.The main pharmacokinetic parameters were as follows:In a state of fasting,tmax was(1.29±0.38)and(0.94±0.28)h;cmax was(4269±1847)and(3031±1115)ng·ml^(-1);AUC(0-t)was(6893±2942)and(4628±1780)ng·h·ml^(-1);AUC(0-∞)is(6939±2948)and(4653±1777)ng·h·ml^(-1).The relative bioavailability of tebipenem pivoxil tablets was 196%.In the state of eating,tmax was(1.44±0.68)and(1.19±0.37)h;cmax was(3834±1321)and(2009±1179)ng·ml^(-1);AUC(0-t)was(5655±1351)and(2881±1484)ng·h·ml^(-1);AUC(0-∞)is(5757±1370)and(2940±1473)ng·h·ml^(-1).The relative bioavailability of tebipenem pivoxil tablets was 196%.The relative bioavailability of tebipenem pivoxil tablets and tebipenem pivoxil granules were not consistent under the conditions of fasting and feeding.

关 键 词：高效液相色谱法-串联质谱法 犬血浆 替比培南 药代动力学 相对生物利用度 

分 类 号：R799.81[医药卫生—临床医学]