Pharmacokinetic Analysis of New Calcium Sensitizer of M6 in Rat Plasma by Single Intravenous

FAN Hong-hao; DENG Le-jun; ZHU Jin-hui; LI Jian; WAN Hua-yin; LI Wei-da; ZHAO Jian-hua; LI Ru-bing

doi:10.13422/j.cnki.syfjx.2015230083

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Pharmacokinetic Analysis of New Calcium Sensitizer of M6 in Rat Plasma by Single Intravenous

更新时间：2024-01-04

- Pharmacokinetic Analysis of New Calcium Sensitizer of M6 in Rat Plasma by Single Intravenous
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 21, Issue 23, Pages: 83-86(2015)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2015230083
  CLC： R965
- Published：2015
- 稿件说明：
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FAN Hong-hao, DENG Le-jun, ZHU Jin-hui, et al. Pharmacokinetic Analysis of New Calcium Sensitizer of M6 in Rat Plasma by Single Intravenous[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(23): 83-86.
DOI：

FAN Hong-hao, DENG Le-jun, ZHU Jin-hui, et al. Pharmacokinetic Analysis of New Calcium Sensitizer of M6 in Rat Plasma by Single Intravenous[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(23): 83-86. DOI： 10.13422/j.cnki.syfjx.2015230083.

摘要

目的:探究新型钙离子增敏剂M6在大鼠血浆中的药代动力学特点

建立快速、简便的检测大鼠血浆中M6血药浓度的高效液相色谱法(HPLC)。方法:采用颈静脉抽血法

考察大鼠尾静脉注射M6后于1

30 min和1

8 h的血药浓度变化

采用HPLC测定血药浓度

流动相1%乙酸水溶液-乙腈(85:15)

检测波长280 nm

绘制血药浓度-时间曲线

通过PKSolver数据处理软件计算M6药代动力学参数。结果:M6检测的线性范围3.125~200 mg·L-1

最低定量限0.6 mg·L-1

日内、日间精确度和稳定性试验的RSD均<10%

方法回收率均>85%。M6在大鼠体内的主要药代动力学参数为达峰时间(tmax)1 min

最大血药浓度(Cmax)6.67 mg·L-1

半衰期(t1/2)21.36 min

平均滞留时间(MRT)30.83 min;药-时曲线出现了双峰现象。结论:M6的t1/2较原型药物PPTA延长

具有代谢时间延长的特点

有望开发M6的新药物。建立的HPLC灵敏、快速、准确

可用于大鼠血浆中M6质量浓度的测定。

Abstract

Objective: To explore pharmacokinetic characteristics of the new calcium sensitizer-M6 in rat plasma

and establish a fast

convenient and effective HPLC for determination of M6 in rat plasma. Method: Jugular vein haemospasia was adopted

M6 was injected by tail vein in rats

plasma concentration was determined by HPLC after 1

30 min and 1

8 h

mobile phase of 1% acetic acid solution-acetonitrile (85:15)

detection wavelength was set at 280 nm.Plasma concentration-time curve was drawn

and pharmacokinetic parameters were calculated by PKSolover software. Result: Linear range of M6 was 3.125-200 mg·L-1

the limit of quantitation was 0.6 mg·L-1

the intra-day

inter-day precision and stabilization were less than 10%

recovery of method was more than 85%.These main pharmacokinetic parameters of M6 were as followed:tmax of 1 min

Cmax of 6.67 mg·L-1

t1/2 of 21.36 min

MRT of 30.83 min

concentration-time curve showed double peaks. Conclusion: Results suggest that t1/2 of M6 is longer than t1/2 of its prototype drug-PPTA.This HPLC is sensitive

rapid and accurate

it can be empolyed to determine concentration of M6 in rat plasma.

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