Pharmacokinetics and Tissue Distribution of Cang'ai Volatile Oil by Nasal Absorption

HUANG Qiu-yan; XIONG Lei; KONG Shu-jun; WANG Hong-mei; WANG Hui; MA Yun-shu; CHEN Bo-jun

doi:10.13422/j.cnki.syfjx.2016230094

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Pharmacokinetics and Tissue Distribution of Cang'ai Volatile Oil by Nasal Absorption

更新时间：2024-01-04

- Pharmacokinetics and Tissue Distribution of Cang'ai Volatile Oil by Nasal Absorption
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 22, Issue 23, Pages: 94-97(2016)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2016230094
  CLC： R285.5
- Published：2016
- 稿件说明：
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HUANG Qiu-yan, XIONG Lei, KONG Shu-jun, et al. Pharmacokinetics and Tissue Distribution of Cang'ai Volatile Oil by Nasal Absorption[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 94-97.
DOI：

HUANG Qiu-yan, XIONG Lei, KONG Shu-jun, et al. Pharmacokinetics and Tissue Distribution of Cang'ai Volatile Oil by Nasal Absorption[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(23): 94-97. DOI： 10.13422/j.cnki.syfjx.2016230094.

摘要

目的：研究苍艾挥发油经家兔鼻腔给药的药动学及经大鼠鼻腔吸收的组织分布，为后期开发制备成临床用药奠定基础。方法：家兔经鼻腔给予苍艾挥发油后，经UPLC检测血浆中苍艾挥发油主成分丁香酚的浓度，流动相甲醇-1%冰乙酸（45：55），流速0.4 mL·min-1，检测波长280 nm，进样量1 μL。试验数据采用DAS 3.0软件（非房室模型）进行拟合并计算药动学参数。采用HPLC测定大鼠脑组织、心、肝、脾、肺、肾中丁香酚的含量，流动相甲醇-1%冰乙酸（65：35），检测波长280 nm。结果：苍艾挥发油在血液中主要的药动学参数为达峰时间（Tmax）（0.083±0）h，药峰浓度（Cmax）（1.150±0.141）mg·L-1，药-时曲线下面积（AUC0-∞）（0.376±0.085）h·mg·L-1，平均滞留时间（MRT0-∞）（0.505±0.039）h。苍艾挥发油经大鼠鼻吸收后，快速分布至各组织中，其中肺组织中含量最高，其次为心脏及脑组织，肝、脾、肾组织中的分布量较少。结论：家兔药动学及大鼠组织分布试验结果均表明苍艾挥发油经鼻吸收后体内滞留时间较短，具有脑靶向趋势。

Abstract

Objective: To study on pharmacokinetics in rabbits and tissue distribution in rats of Cang'ai volatile oil after nasal absorption. Method: After intranasal administration of Cang'ai volatile oil

the concent of eugenol in rabbit plasma was detected by UPLC

mobile phase was methanol-1% glacial acetic acid (45:55)

flow rate was 0.4 mL·min-1

the detection wavelength was 280 nm and sample volume was 1 μL.The data were fitted by DAS 3.0 software (non-compartment model) and pharmacokinetic parameters were calculated.The contents of eugenol in rats' brain

heart

liver

spleen

lung and kidney were determinated by HPLC after intranasal administration of Cang'ai volatile oil. Result: Primary pharmacokinetic parameters of Cang'ai volatile oil were as follows:Tmax of (0.083±0) h

Cmax of (1.150±0.141) mg·L-1

AUC0-∞ of (0.376±0.085) h·mg·L-1

MRT0-∞ of (0.505±0.039) h.Cang'ai volatile oil was rapidly distributed into all tissues after intranasal absorption

the content of eugenol in the lung was the highest

followed by the heart and brain

its distribution in liver

spleen and kidney was small. Conclusion: In vivo retention time of Cang'ai volatile oil is short with brain targeting trend.

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