雾化吸入氨茶碱在犬体内的组织分布

Distribution of aminophylline after aerosol inhalation in beagles

目的:研究雾化吸入氨茶碱在犬体内的组织分布特点。方法:建立了采用HPLC法测定犬血清和组织中茶碱浓度的方法。比较雾化吸入和静脉滴注给药后的组织分布特点与血药浓度。结果:相对于静脉滴注途径,采用雾化吸入途径给予同剂量氨茶碱后0.25和0.5 h气管组织中的药物浓度显著升高(0.25 h,P<0.01;0.5 h,P<0.05),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24.52%。结论:雾化吸入给予氨茶碱能够在维持气管和支气管药物高浓度的同时显著降低药物在其他正常组织以及血清中的分布。氨茶碱改用雾化吸入途径给药治疗哮喘和阻塞性肺疾病具有明显的优势。

To investigate the tissue distribution and pharmacokinetics of aminophyl line after aerosol inhalation in beagles. METH ODS： HPLC was used to determine the concen tration of theophylline in different tissues and plasma of the beagles. The tissue distribution of theophylline after aerosol inhaling was compared to intravenous infusing aminophylline. Plasma concentrations at different time after aerosol in halation were compared with intravenous infu sion. RESULTS ： The theophylline concentrations in trachea after aerosol inhalation at 0.25 and 0.5 h were higher obviously than that of intrave nous infusion administration group （0.25 h, P~ 0.01; 0.5h, P%0.05）. At 0.25, 0.5, land2h, the theophylline concentrations in other tis sues were decreased obviously. The absolute bioavailability of aminophylline after aerosol in halation was 24.52%. CONCLUSION： After aerosol inhaling aminophylline, the theophylline is retained mostly in trachea. At the same time, the theophylline concentrations in other tissues are decreased obviously. The administration route of aerosol inhaling aminophylline can raise the therapeutic index and reduce adverse effects dramatically.