苍艾挥发油经鼻吸收的药代动力学及组织分布  

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

作　　者：黄秋艳[1] 熊磊[1] 孔淑君 汪红梅[1] 王辉[1] 马云淑[1] 陈柏君[1] 

机构地区：[1]云南中医学院,昆明650500

出　　处：《中国实验方剂学杂志》2016年第23期94-97,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金地区基金项目(81160534;81560740)

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 m L·min^(-1),检测波长280 nm,进样量1μL。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。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 m L·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： Tmaxof（ 0. 083 ± 0） h,Cmaxof（ 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.

关 键 词：苍艾挥发油 鼻腔给药 药物代谢 组织分布 丁香酚 丹皮酚 

分 类 号：R969.1[医药卫生—药理学] R284.1[医药卫生—药学]