摘要
目的:研究注射用兰索拉唑钠在犬体内的立体选择性药动学。方法:6只Beagle犬静脉注射兰索拉唑钠,于给药前及给药后5,15,30,45 min及1,1.5,2,2.5,3,4,6 h自犬后肢静脉取血约3 ml制备血浆。采用HPLC法的两种色谱条件对其中的药物含量进行测定。结果:犬静脉注射兰索拉唑钠后,兰索拉唑钠左旋体与右旋体的主要药动学参数为:半衰期(t1/2):(0.434±0.101),(0.524±0.128)h;清除速率常数(Ke):(1.695±0.516),(1.402±0.397)L·h^-1;表观分布容积(Vd):(0.244±0.042),(0.284±0.048)L·kg^-1;清除率(CL):(0.404±0.093),(0.390±0.094)L·h^-1·kg^-1;AUC0~6h:(1.836±0.435),(1.909±0.440)mg·L^-1·h。结论:兰索拉唑钠在Beagle犬体内代谢迅速,兰索拉唑中左旋体及右旋体AUC0~6h的比值是0.96,未发现左旋体与右旋体之间存在明显的相互转化。
Objective: To study the stereoselective pharmacokinetics of lansoprazole sodium for injection in dogs. Methods:Six beagle dogs were intravenously injected with lansoprazole sodium,and blood was taken from the canine hind limb vein before the administration and 5,15,30,45 min and 1,1.5,2,2.5,3,4 and 6 h after the administration to prepare 3 ml plasma samples. The drug content was determined by HPLC using two chromatographic conditions. Results: After the intravenous injection of lansoprazole sodium in dogs, the main pharmacokinetic parameters of L-and R-lansoprazole sodium were as follows:t1/2 were( 0.434 ± 0.101) and( 0.524 ± 0.128) h;Kewere( 1.695 ± 0.516) and( 1.402 ± 0.397) L·h^-1;Vdwere( 0.244 ± 0.042)and( 0.284 ± 0.048) L·kg^-1;CL were( 0.404 ± 0.093) and( 0.390 ± 0.094) L·h^-1·kg^-1;AUC0 ~ 6 hwere( 1.836 ± 0.435) and( 1.909 ± 0.440) mg·h·L^-1. Conclusion: Lansoprazole sodium is rapidly metabolized in beagle dogs. The AUC0 ~ 6 hratio of L-and R-lansoprazole sodium is 0.96. No obvious mutual transformation between L-and R-lansoprazole sodium is found.
作者
郑晓霞
何小华
黄艳妮
程艳玲
Zheng Xiaoxia;He Xiaohua;Huang Yanni;Cheng Yanling(Shandong Academy of Pharmaceutical Science,Shandong Key Laboratory of Chemical Drugs,Jinan 250101,China)
出处
《中国药师》
CAS
2020年第8期1665-1668,共4页
China Pharmacist
关键词
兰索拉唑钠
对映异构体
手性流动相
构型转化
药动学
Lansoprazole sodium
Enantiomers
Chiral mobile phase
Inversion of configuration
Pharmacokinetics
