雾化吸入羟基喜树碱在兔体内的组织分布

目的研究雾化吸入羟基喜树碱在兔体内的组织分布特点。方法建立了采用RP-HPLC法测定兔血浆和组织中羟基喜树碱浓度的方法。比较雾化吸入和静脉注射给药后的组织分布特点与血药浓度。结果相对于静脉注射途径，采用雾化吸入途径给予同剂量羟基喜树碱后0.5,1和2 h肺中的药物浓度分别提高了13.52,27.81和20.82倍，而药物在其他组织中的分布几乎都显著降低。雾化吸入给药后的绝对生物利用度为7.38%。结论雾化吸入给予羟基喜树碱能够在维持肺内药物高浓度的同时显著降低药物在其他正常组织以及血浆中的分布。羟基喜树碱改用雾化吸入途径给药治疗肺癌具有明显的优势。

Distribution of hydroxycamptothecin after aerosol inhalation in rabbits

Aim To investigate the tissue distribution and pharmacokinetics of hydroxycamptothecin ( HCPT) after aerosol inhalation in rabbits. Methods RP-HPLC was used to determine the concentration of HCPT in different tissues and plasma of rabbits. The tissue distribution of HCPT after aerosol inhalation or iv administration was compared. The plasma concentrations at different time after aerosol inhalation were compared with iv injection. Results The HCPT concentrations in lung after aerosol inhalation at 0. 5, 1 and 2 h were 13. 52, 27. 81 and 20. 82 times higher than that of iv administration group, respectively. At the same time, concentrations in other tissues were decreased obviously. The absolute bioavailability of HCPT after aerosol inhalation was 7. 38% . Conclusion After aerosol inhalation, HCPT is retained mostly in lung. So this administration route can raise the therapeutic index and reduce adverse effects.