普朗尼克F68对地西泮在大鼠小肠吸收过程的影响  

Effect of Pluronic■ F68 on Intestinal Absorption of Diazepam in Rats

作　　者：马莉[1] 夏丽 王金萍[1] 聂晓静[1] 彭莉蓉[1] Ma Li;Xia Li;Wang Jinping;Nie Xiaojing;Peng Lirong(Department of Pharmacy,Xi'an Central Hospital,Xi'an 710003, China)

机构地区：[1]西安市中心医院药剂科,西安710003

出　　处：《中国药师》2019年第1期167-169,共3页China Pharmacist

基　　金：西安市卫生计生委医学科研计划项目(编号:J201702019)

摘　　要：目的:考察药用辅料普朗尼克F68对地西泮在大鼠小肠吸收过程的影响。方法:采用大鼠在体单向肠灌流模型,使用HPLC法测定肠灌流液中地西泮浓度。计算不含普朗尼克F68药物组及含不同浓度普朗尼克F68药物组、含P-糖蛋白抑制药物组(维拉帕米)地西泮的吸收速率常数Ka与药物渗透系数Peff。结果:1. 00μg·ml^(-1)、0. 50μg·ml^(-1)的普朗尼克F68及维拉帕米均显著影响地西泮的K_a、P_(eff),并且随着普朗尼克F68浓度的增加,地西泮的K_a、P_(eff)相应增加。30μg·ml^(-1)的普朗尼克F68对地西泮无显著性影响。结论:0. 50μg·ml^(-1)和1. 00μg·ml^(-1)的普朗尼克F68药物组及维拉帕米组均显著增加地西泮在大鼠小肠的吸收,可能与其抑制P-糖蛋白有关。Objective:To study the effect of Pluronic?F68 on the intestinal absorption of diazepam in rats.Methods:Using single-pass intestinal perfusion model,the concentration of diazepam was determined by HPLC.The drug absorption rate constant(Ka)and the effective intestinal permeability(Peff)in each intestinal section were calculated in rats with or without Pluronic?F68,or with P-gp inhibitor verapamil.Results:Pluronic?F68(1.00μg·ml^-1,0.05μg·ml^-1)and varapamil signifcantly increased the Kaand Peffof diazepam,the Kaand Peffof diazepam was increased significantly when the concentration of diazepam was increased.On the other hand,the Kaand Peffof 30μg·ml-1Pluronic?F68 group was not affected significantly.Conclusion:Pluronic?F68 at the doses of 0.50μg·ml^-1 and 1.00μg·ml^-1 and verapamil can promote the intestinal absorption of diazepam in rats,which may be due to the inhibition of P-glycoprotein activity.

关 键 词：普朗尼克F68 地西泮 在体单向肠灌流模型 肠吸收 

分 类 号：R945[医药卫生—微生物与生化药学]