Effects of Different Doses of Chuanxiong Rhizoma on Pharmacokinetics of Active Ingredients from Gastrodiae Rhizoma in Rats

WANG Qiang; SHEN Lan; MA Shi-yu; ZHAO Li-jie; ZHAO Meng-xian; FENG Yi

doi:10.13422/j.cnki.syfjx.2015020103

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Effects of Different Doses of Chuanxiong Rhizoma on Pharmacokinetics of Active Ingredients from Gastrodiae Rhizoma in Rats

更新时间：2024-01-04

- Effects of Different Doses of Chuanxiong Rhizoma on Pharmacokinetics of Active Ingredients from Gastrodiae Rhizoma in Rats
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 21, Issue 2, Pages: 103-109(2015)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2015020103
  CLC： R965
- Published：2015
- 稿件说明：
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WANG Qiang, SHEN Lan, MA Shi-yu, et al. Effects of Different Doses of Chuanxiong Rhizoma on Pharmacokinetics of Active Ingredients from Gastrodiae Rhizoma in Rats[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(2): 103-109.
DOI：

WANG Qiang, SHEN Lan, MA Shi-yu, et al. Effects of Different Doses of Chuanxiong Rhizoma on Pharmacokinetics of Active Ingredients from Gastrodiae Rhizoma in Rats[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(2): 103-109. DOI： 10.13422/j.cnki.syfjx.2015020103.

摘要

目的: 探讨不同剂量川芎对天麻素(GAS)及天麻苷元(HBA)在偏头痛大鼠体内药动学的影响。方法: 234只大鼠随机等分为3组

川芎-天麻配比分别为1:3(川芎、天麻剂量分别为0.163

0.484 g ·kg-1)

2:3(川芎、天麻剂量分别为0.326

0.484 g ·kg-1)

4:3(川芎、天麻剂量分别为0.652

0.484 g ·kg-1)

于给药后不同时间点采血和脑组织。采用HPLC测定GAS和HBA含量

血浆中天麻素、天麻苷元检测流动相乙腈-0.01%磷酸水(2:98)

柱温35 ℃;脑组织中天麻苷元检测流动相乙腈-水(3:97)

柱温30 ℃。利用DAS 2.0软件计算药动学参数。结果: GAS在3组大鼠血浆中的药时曲线下面积 [AUC(0-t)]分别为(1 984.41±89.91)

(1 708.74±108.96)

(1 862.76±82.11) mg ·L-1 ·min

平均滞留时间[MRT(0-t)]分别为(63.62±2.04)

(61.69±2.40)

(75.04±4.29) min

清除率(CL)分别为(0.034 3±0.002 4)

(0.039 9±0.002 3)

(0.031 6±0.003 2) L ·min-1 ·kg-1。HBA在3组大鼠的脑匀浆中AUC(0-t)分别为(72 891.70±12 075.24)

(64 201.77±5 921.88)

(97 046.82±11 002.49) μg ·L-1 ·min

MRT(0-t)分别为(82.15±15.34)

(68.33±11.22)

(96.68±8.87) min

CL分别为(0.395 5±0.072 8)

(0.450 7±0.049 2)

(0.301 2±0.036 7) L ·min-1 ·kg-1。结论: 川芎-天麻(4:3)时GAS及HBA在血、脑中生物利用度较高

滞留时间延长

消除速率减缓

这与古方中川芎-天麻药对的常用剂量相符

从药动学角度证明了古方用药的合理性和科学性。

Abstract

Objective: To investigate influence of different dose of Chuanxiong Rhizoma(LC) on pharmacokinetics of gastrodin(GAS) and gastrodigenin(HBA) from Gastrodiae Rhizoma(GE) in migraine model rats. Method: Rats were randomly divided into LC-GE(1: 3) group(doses of LC and GE extracts were 0.163

0.484 g · kg-1)

LC-GE(2:3) group(doses of LC and GE extracts were 0.326

0.484 g · kg-1) and LC-GE(4:3) group(doses of LC and GE extracts were 0.652

0.484 g · kg-1)

plasma and brain tissue was collected at different times after drug administration.Concentrations of GAS and HBA were determined by HPLC

a mixture of acetonitrile-0.01% phosphoric acid(2: 98) was employed as mobile phase for determination of GAS and HBA in rats plasma with temperature of column oven was maintained at 35 ℃.While mobile phase of acetonitrile-water(3: 97) was used for quantification of HBA in rats brain

column temperature was heated at 30 ℃.DAS 2.0 software was used to calculate pharmacokinetic parameters. Result: Area under curve[AUC(0-t)] of GAS in rats plasma from these three groups were (1 984.41±89.91)

(1 708.74±108.96)

(1 862.76±82.11) mg · L-1 · min

their mean residence time[MRT(0-t)] were (63.62±2.04)

(61.69±2.40)

(75.04±4.29) min

their clearance(CL) were (0.034 3±0.002 4)

(0.039 9±0.002 3)

(0.031 6±0.003 2) L · min-1 · kg-1

respectively.AUC(0-t) of HBA in rats brain from these three groups were (72 891.70±12 075.24)

(64 201.77±5 921.88)

(97 046.82±11 002.49) μg · L-1 · min

their MRT(0-t) were (82.15±15.34)

(68.33±11.22)

(96.68±8.87) min

their CL were (0.395 5±0.072 8)

(0.450 7±0.049 2)

(0.301 2±0.036 7) L · min-1 · kg-1

respectively. Conclusion: These findings demonstrate LC-GE(4: 3) group(equivalent to crude herbs ratio of 4: 1) can enhance bioavailability

prolong MRT and reduce elimination speed of GAS in plasma as well as HBA in brain by comparing with other compatibility groups

which is consistent with usual dose in ancient prescriptions.This study demonstrates compatibility connotation at a right dose-ratio of LC and GE through angle of pharmacokinetics.

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