Pharmacokinetics Evaluation of Capsaicin Submicron Emulsion Injection in Rabbits

LU Xiu-xia; TENG Xi-feng; LU Yu-mei; LIN Liang-min; LONG Xiao-ying

doi:10.11653/syfj2014060114

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Pharmacokinetics Evaluation of Capsaicin Submicron Emulsion Injection in Rabbits

更新时间：2024-01-04

- Pharmacokinetics Evaluation of Capsaicin Submicron Emulsion Injection in Rabbits
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 20, Issue 6, Pages: 114-117(2014)
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- DOI：10.11653/syfj2014060114
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- Published：2014
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LU Xiu-xia, TENG Xi-feng, LU Yu-mei, et al. Pharmacokinetics Evaluation of Capsaicin Submicron Emulsion Injection in Rabbits[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(6): 114-117.
DOI：

LU Xiu-xia, TENG Xi-feng, LU Yu-mei, et al. Pharmacokinetics Evaluation of Capsaicin Submicron Emulsion Injection in Rabbits[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(6): 114-117. DOI： 10.11653/syfj2014060114.

摘要

目的：考察并评价辣椒碱亚微乳注射剂在家兔体内的药动学行为。方法：采用HPLC测定家兔血浆中辣椒碱血药浓度，流动相甲醇-水-磷酸（68：32：0.1），检测波长281 nm。通过DASTM ver1.0药动学智能软件分析家兔耳缘静脉注射辣椒碱亚微乳及其水溶液的房室模型，计算药动学参数。结果：辣椒碱血药浓度在0.500~100 mg·L-1呈良好线性关系（r=0.999 7），萃取回收率96.10%~105.48%。家兔耳缘静脉注射辣椒碱亚微乳及其水溶液的药动学曲线均符合二室模型，消除半衰期分别为（48.501 3±4.011 9），（15.262 5±1.888 2）min，药时曲线下面积分别为（924.09±149.80），（555.36±57.46）mg·min·L-1。结论：建立的HPLC准确、灵敏，适用于辣椒碱血药浓度的测定。与辣椒碱水溶液相比，辣椒碱亚微乳能延长药物的体内半衰期，提高生物利用度。

Abstract

Objective: To evaluate pharmacokinetic characteristic of capsaicin submicron emulsion in rabbits. Method: HPLC was established to determine the concentration of capsaicin in rabbit plasma with mobile phase of methanol-water-phosphoric acid(68：32：0.1) and detection wavelength at 281 nm.compartment models were analyzed by DASTM ver1.0 software after rabbit ear vein administration of capsaicin submicron emulsion and its aqueous

then calculated pharmacokinetic parameters. Result: Linear correlation was satisfactory when the concentration of capsaicin in rabbit plasma was 0.500-100 mg·L-1(r=0.999 7)

extraction recovery was 96.10%-105.48%.Pharmacokinetics curve was both corresponded to two-compartment model after intravenous injection of capsaicin submicron emulsion and its aqueous

elimination half-life were (48.501 3±4.011 9) and (15.262 5±1.888 2) min

area under curve were (924.09±149.80) and (555.36±57.46) mg·min·L-1. Conclusion: Established HPLC was accurate

sensitive and satisfied with concentration determination of capsaicin in rabbit plasma.Compared with capsaicin solution

prolongation of elimination half-life and elevation of biological availability were all obtained after capsaicin was emulsified with submicron emulsion.

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