葛根素自微乳在大鼠体内药代动力学分析

陈顺尧; 雷凯君; 吴颖欣; 王汝上

doi:10.13422/j.cnki.syfjx.2014100106

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葛根素自微乳在大鼠体内药代动力学分析

药物代谢 | 更新时间：2024-01-04

- 葛根素自微乳在大鼠体内药代动力学分析
- Pharmacokinetics of Puerarin Self-microemulsions in Rats
- 中国实验方剂学杂志 2014年20卷第10期页码：106-108
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- DOI：10.13422/j.cnki.syfjx.2014100106
  中图分类号： R285
- 纸质出版日期：2014
- 稿件说明：
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陈顺尧, 雷凯君, 吴颖欣, 等. 葛根素自微乳在大鼠体内药代动力学分析[J]. 中国实验方剂学杂志, 2014,20(10):106-108.

CHEN Shun-yao, LEI Kai-jun, WU Ying-xin, et al. Pharmacokinetics of Puerarin Self-microemulsions in Rats[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(10): 106-108.
陈顺尧, 雷凯君, 吴颖欣, 等. 葛根素自微乳在大鼠体内药代动力学分析[J]. 中国实验方剂学杂志, 2014,20(10):106-108. DOI： 10.13422/j.cnki.syfjx.2014100106.

CHEN Shun-yao, LEI Kai-jun, WU Ying-xin, et al. Pharmacokinetics of Puerarin Self-microemulsions in Rats[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(10): 106-108. DOI： 10.13422/j.cnki.syfjx.2014100106.

摘要

目的：考察葛根素自微乳在大鼠体内的血药浓度经时过程，评价葛根素自微乳的药代动力学及相对生物利用度。方法：单剂量给予大鼠葛根素自微乳和葛根素混悬液，采用HPLC测定血浆中葛根素质量浓度，检测波长250 nm，流动相甲醇（A）-0.1%磷酸水溶液（B）梯度洗脱（0~30 min，20%~25%A；30~40 min，25%~40%A；40~50 min，40%A），运用DAS 2.1.1程序拟合药物浓度-时间曲线，计算药代动力学参数及生物利用度。结果：葛根素自微乳和混悬液的tmax分别为0.71，1.1 h，Cmax分别为2.052，1.120 mg·L-1，AUC0-24 h依次为2.901，2.013 mg·h·L-1，葛根素自微乳相对于混悬液的生物利用度144.11%。结论：与葛根素混悬液相比，葛根素自微乳能显著提高葛根素在大鼠体内的生物利用度。

Abstract

Objective: To estabolish a quantitative analysis method for pharmacokinetics and bioavailability of puerarin self-microemulsions in rats. Method: Puerarin self-microemulsions and suspensions were given by a single dose

HPLC was adopted to determine the concentration of puerarin in plasma with detection wavelength at 250 nm and mobile phase of methanol(A)-0.1% phosphoric acid solution(B) for gradient elution(0-30 min

20%-25%A;30-40 min

25%-40%A;40-50 min

40%A)

pharmacokinetics parameters and bioavailability was calculated by DAS 2.1.1 programs. Result: tmax of puerarin self-microemulsions and suspensions were 0.71

1.1 h

Cmax were 2.052

1.120 mg·L-1

AUC0-24 h were 2.901

2.013 mg·h·L-1

respectively.Relative bioavailability of puerarin self-microemulsions to suspensions was 144.11%. Conclusion: Compared with puerarin suspensions

puerarin self-microemulsion could significantly improve bioavailability in rats.

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