醒脑静口服给药后栀子苷在比格犬体内的药代动力学及生物利用度

[Pharmacokinetics and bioavailabilities of geniposide in Beagle dogs after oral administration Xingnaojing].

作者信息

Tian Xiufeng, Li Pengyue, Wang Hongjie, Bian Baolin, Du Shouying, Yang Jian

机构信息

Beijing University of Chinese Medicine, Beiing 100102, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2012 Aug;37(16):2461-4.

PMID:23234150

Abstract

OBJECTIVE

To establish a method for determination of geniposide in Beagle dogs plasma by high performance liquid chromatography (HPLC), and study the pharmacokinetics and bioavailability of geniposide in Beagle dogs after oral administration Xingnaojing.

METHOD

To determine the geniposide in Beagle dogs plasma by HPLC after oral administration or intravenous injection Xingnaojing, and the pharmacokinetic parameters were calculated by the software of Kinetica.

RESULT

The good linearity range of geniposide was 1.24 - 158.88 mg x L(-1). The main pharmacokinetic parameters after oral administration was as follows: Cmax (11.8 +/- 0.6) mg x L(-1), Tmax (52.0 +/- 4.5) min, AUC(1280.8 +/- 172.0) mg x min x L(-1), MRT(118.7 +/- 25.4) min, and these parameters after intravenous injection was follows: Cmax 107.4 +/- 6.3) mg x L(-1), AUC(7930.1 +/- 670.0) mg x min x L(-1), MRT(92.4 +/- 5.1) min. The bioavailability of geniposide in Beagle dogs after oral administration Xingnaojing was (6.46 +/- 0.87)%.

CONCLUSION

The HPLC method had good applicability. The extract recovery, method recovery, intra-day precision and inter-day precision of the method were all met the requirements. The stability in conditions of room temperature and freeze-thaw cycle was good. The results indicated that the oral administration bioavailability of geniposide was in low degree.

摘要

目的

建立高效液相色谱法（HPLC）测定比格犬血浆中栀子苷的含量，并研究比格犬口服醒脑静后栀子苷的药代动力学及生物利用度。

方法

比格犬口服或静脉注射醒脑静后，采用HPLC法测定血浆中栀子苷的含量，并用Kinetica软件计算药代动力学参数。

结果

栀子苷的线性范围为1.24～158.88mg·L⁻¹。口服给药后的主要药代动力学参数如下：Cmax为（11.8±0.6）mg·L⁻¹，Tmax为（52.0±4.5）min，AUC为（1280.8±172.0）mg·min·L⁻¹，MRT为（118.7±25.4）min；静脉注射后的这些参数如下：Cmax为（107.4±6.3）mg·L⁻¹，AUC为（7930.1±670.0）mg·min·L⁻¹，MRT为（92.4±5.1）min。比格犬口服醒脑静后栀子苷的生物利用度为（6.46±0.87）%。