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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 the pharmacokinetics of volatile oil from Corylus heterophylla and its distribution in nasal cavity of rats through nasal administration, which will lay the foundation for the development and preparation of clinical medicine. Methods: After the essential oil of Cangai was given to the rabbits through nasal cavity, the concentration of eugenol, the main component of the volatile oil in Cangai, was detected by UPLC. The mobile phase was methanol (-1)% glacial acetic acid (45:55), the flow rate was 0.4 m L · min ~ (-1), detection wavelength 280 nm, injection volume 1μL. The experimental data were fitted using the DAS 3.0 software (non-compartmental model) and the pharmacokinetic parameters were calculated. The content of eugenol in rat brain, heart, liver, spleen, lung and kidney was measured by HPLC. The mobile phase was methanol - 1% glacial acetic acid (65:35). The detection wavelength was 280 nm. Results: The main pharmacokinetic parameters of volatile oil in Cangai were peak time (Tmax) (0.083 ± 0) h, peak drug concentration (Cmax) (1.150 ± 0.141) mg · L -1, The area under the curve (AUC0-∞) (0.376 ± 0.085) h · mg · L -1, mean retention time (MRT0-∞) (0.505 ± 0.039) h. After being absorbed by the nose of rats, the volatile oil of Cangai was quickly distributed to various tissues, of which the content was the highest in lung tissue, followed by the heart and brain tissue, with less distribution in liver, spleen and kidney. Conclusion: The pharmacokinetics of rabbits and the distribution of rat tissue showed that the volatile oil in Cavaia suffruticosa had shorter residence time in vivo after nasal absorption and had the tendency of brain targeting.