[醒脑静微乳剂及mPEG2000-PLA修饰醒脑静微乳剂给药小鼠后栀子苷的药代动力学研究]

[Study on pharmacokinetics of geniposide in mice administrated by xingnaojing microemulsion and mPEG2000-PLA modified xingnaojing microemulsion].

作者信息

Wen Ran, Chen Xiao-Lan, Li Hui-Yun, Guo Qing-Li, Lu Yang, Du Shou-Ying

出版信息

Zhongguo Zhong Yao Za Zhi. 2014 Mar;39(6):1111-4.

Abstract

An HPLC method for the determination of geniposide concentration in mouse plasma was developed and the pharmacokinetics after intranasal administration of Xingnaojing microemulsion (XNJ-M) and mPEG2000-PLA modified Xingnaojing microemulsion (XNJ-MM) were investigated. Eighty mice were treated by XNJ-M and XNJ-MM nasally. The plasma samples were collected at different times and the drug in samples was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica. The pharmacokinetic parameters of geniposide of XNJ-M were C(max) (4.36 +/- 2.69) mg x L(-1), t(max) 1 min, MRT (29.73 +/- 4.54) min, AUC (53.63 +/- 14.03) mg x L(-1) x min. The pharmacokinetic parameters of geniposide of XNJ-MM were C(max) (9.75 +/- 4.14) mg x L(-1), t(max) 1 min, MRT(22.34 +/- 2.90) min, AUC (131.87 +/- 40.13) mg x L(-1) x min. Geniposide can be absorbed into blood in a higher degree after intranasal administration with XNJ-MM compared to XNJ-M, which maybe caused by its less irritating and more absorption.

摘要

建立了一种测定小鼠血浆中栀子苷浓度的高效液相色谱法，并研究了醒脑静微乳（XNJ-M）和mPEG2000-PLA修饰醒脑静微乳（XNJ-MM）鼻腔给药后的药代动力学。80只小鼠分别经XNJ-M和XNJ-MM鼻腔给药。在不同时间采集血浆样本，采用高效液相色谱法检测样本中的药物。通过Kinetica软件计算药代动力学参数。XNJ-M中栀子苷的药代动力学参数为C(max)（4.36±2.69）mg·L(-1)，t(max) 1分钟，MRT（29.73±4.54）分钟，AUC（53.63±14.03）mg·L(-1)·分钟。XNJ-MM中栀子苷的药代动力学参数为C(max)（9.75±4.14）mg·L(-1)，t(max) 1分钟，MRT(22.34±2.90)分钟，AUC（131.87±40.13）mg·L(-1)·分钟。与XNJ-M相比，XNJ-MM鼻腔给药后栀子苷能更高程度地吸收入血，这可能是由于其刺激性较小且吸收性更强所致。