雾化吸入羟基喜树碱在小鼠体内的药代动力学研究

Pharmacokinetic Study of Hydroxycamptothecin after Aerosol Inhalation in Mice

目的:研究雾化吸入羟基喜树碱(HCPT)在小鼠体内和肺中以及其他脏器中的药代动力学特征。方法:采用HPLC法测定不同时间点小鼠血浆和肺组织以及其他脏器组织中羟基喜树碱的内酯和盐型的浓度,并对雾化吸入给药后的血浆和各个脏器组织中的药物浓度数据进行药代动力学分析。结果:雾化吸入给药后,肺组织中的浓度远远高于血浆和其他器官组织,血浆和其他器官组织中药物浓度较低,并且在肺组织中,内酯型比例较高。结论:雾化吸入羟基喜树碱在肺癌中能达到靶器官中的高浓度和血浆中的低浓度,两者的药物动力学规律有所不同。

Objective： To investigate the pharmacokinetic characteristics of hydroxycamptothecin （HCFF） after inhalation in mice. Methods： HPLC was used to determine the concertrations of HCPT lactone and sah form at different time points in plasma, lung tissue and other organs. The drug concentration data of plasma and various organs and tissues were compared. Results： After inhalation, the drug concentrations in lung were much higher than those in plasma and other organs and tissues. A higher proportion of lactone from HCFF was found in the lung tissue. Conclusion： After aerosol inhalation, HCPT is retained mostly in the lung organ and rarely in plasma. Drug kinetics were different in plasma and lung organ.