粉防己碱温敏性缓释原位凝胶的大鼠体内药代动力学分析

高秀蓉; 许小红; 杨洋; 王凤玲; 张燕; 李泽民

doi:10.13422/j.cnki.syfjx.2016230098

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粉防己碱温敏性缓释原位凝胶的大鼠体内药代动力学分析

药物代谢 | 更新时间：2024-01-04

- 粉防己碱温敏性缓释原位凝胶的大鼠体内药代动力学分析
- Pharmacokinetic Analysis of Tetrandrine Sustained-release Thermosensitive Gel in Rats
- 中国实验方剂学杂志 2016年22卷第23期页码：98-102
- 作者机构：
- 作者简介：
- 基金信息：
  
  四川省教育厅自然科学基金项目（11ZB202）;成都医学院大学生创新性实验项目（CX201225）
- DOI：10.13422/j.cnki.syfjx.2016230098
  中图分类号： R285.5
- 纸质出版日期：2016
- 稿件说明：
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高秀蓉, 许小红, 杨洋, 等. 粉防己碱温敏性缓释原位凝胶的大鼠体内药代动力学分析[J]. 中国实验方剂学杂志, 2016,22(23):98-102.

GAO Xiu-rong, XU Xiao-hong, YANG Yang, et al. Pharmacokinetic Analysis of Tetrandrine Sustained-release Thermosensitive Gel in Rats[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 98-102.
高秀蓉, 许小红, 杨洋, 等. 粉防己碱温敏性缓释原位凝胶的大鼠体内药代动力学分析[J]. 中国实验方剂学杂志, 2016,22(23):98-102. DOI： 10.13422/j.cnki.syfjx.2016230098.

GAO Xiu-rong, XU Xiao-hong, YANG Yang, et al. Pharmacokinetic Analysis of Tetrandrine Sustained-release Thermosensitive Gel in Rats[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 98-102. DOI： 10.13422/j.cnki.syfjx.2016230098.

摘要

目的：采用LC-MS/MS测定静脉注射、灌胃粉防己碱原料药与皮下注射粉防己碱凝胶剂的血药浓度，计算粉防己碱凝胶剂的生物利用度。方法：建立血浆中粉防己碱含量的检测方法。通过颈静脉注射粉防己碱原料药、灌胃原料药、皮下注射凝胶剂后采血，采用LC-MS/MS检测大鼠血浆中药物浓度，流动相0.1%甲酸水溶液-乙腈梯度洗脱，流速0.4 mL·min-1；采用电喷雾电离，正离子检测模式，粉防己碱和蝙蝠葛碱（内标）的m/z分别为623.1~176.0，625.1~206.0。利用DAS 3.0软件计算药动学参数并绘制药-时曲线，计算口服和皮下注射方式的绝对生物利用度。结果：建立的LC-MS/MS精密度、稳定性良好（RSD均<11.0%），萃取回收率81.36%~97.14%。灌胃给予粉防己碱与皮下注射粉防己碱凝胶剂的绝对生物利用度分别为42.76%和85.44%。结论：粉防己碱凝胶剂的生物利用度较灌胃给予原料药大大提高，且具有缓释效果，具有一定的开发前景。

Abstract

Objective: LC-MS/MS was employed to determine blood concentration after intravenous

intragastric administration of tetrandrine powder and subcutaneous injection of tetrandrine gel

and calculated the bioavailability of tetrandrine gel. Method: Determination of tetrandrine in plasma was established.After intravenous

intragastric administration of tetrandrine powder and subcutaneous injection of tetrandrine gel

LC-MS/MS was adopted to determine blood concentration of tetrandrine

detection ion for tetrandrine was m/z 623.1-176.0

detection ion for dauricine (the internal standard) was m/z 625.1-206.0

DAS 3.0 software was used to calculate pharmacokinetic parameters and the absolute bioavailability. Result: This established LC-MS/MS had good stability and precision

extraction recovery was 81.36%-97.14%.Absolute bioavailabilities of intragastric administration of tetrandrine powder and subcutaneous injection of tetrandrine gel were 42.76% and 85.44%

respectively. Conclusion: The absolute bioavailability of tetrandrine gel is improved greatly by compared with intragastric administration of tetrandrine powder

tetrandrine gel has a sustained-release effect.

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