摘要
目的 探讨模拟失重条件下以血流量改变为生理基础的药代动力学变化。方法 选择庆大霉素作为模型药物，采用头低位（ － ２０°） 兔限制活动为模拟失重动物模型，观察模拟失重对兔庆大霉素药代动力学参数的影响。７ 只家兔在头低位７ ｄ 前后，分别静脉滴注了３ ｍｇ／ｋｇ 的庆大霉素，用 Ｔ Ｄｘ Ｆ Ｌｘ 测定了给药后４ ｈ 内的血药浓度。结果 庆大霉素的分布变慢，这表现在α值由头低位前的（０ ．１８３８ ±０ ．１０７６）ｍｉｎ － １ 降至头低位后的（０ ．０５９１ ±０ ．０３３４） ｍｉｎ － １ ，ｔ１／２α由（５ ．３０ ±３ ．５５） ｍｉｎ 延长为（１５ ．０４ ±７ ．４９）ｍｉｎ ， Ｋ１２ 由（０ ．１０２５ ±０ ．０７２１） ｍｉｎ － １ 降至（０ ．０１８１ ±０ ．０１６１） ｍｉｎ１ ，都有显著性差异； Ｖ（ Ｃ） 、 Ｖ（ Ｄ） 也有升高的趋势。庆大霉素清除率在模拟失重后也有所增加， Ｃ Ｌ（ Ｓ） 从（２ ．２ ±０ ．５）ｍｌ·ｍｉｎ１·ｋｇ１ 升至（２ ．７ ±０ ．３）ｍｌ·ｍｉｎ１·ｋｇ１ 。结论 模拟失重可改变药代动力学过程。
Objective To observe pharmacokinetic changes under simulated weightlessness in relevant to body flood flow changes. Method Gentamicin was selected as probe drug in the present study, and rabbits exposed to Head Down Tilt( HDT,-20°) immobilization were selected as simulated weightlessness animal model. Seven rabbits were treated inf. with 3 mg/kg of gentamicin sulfate pre HDT and 7 d after HDT. Gentamicin blood samples within 4 h after administration were analyzed by TDxFLx. Result The distribution of gentamicin postponed significantly: a significant decrease in α from (0.1838± 0.1076 )min -1 before HDT to (0.0591±0.0334)min -1 after HDT; a significant increase in t 1/2 α from (5.30±3.55)min to (15.04±7.49)min;a significant decrease in k 12 from (0.1025±0.0721)min -1 to (0.0181±0.0161)min -1 ,a increase trend in V (C) and V (D) . After HDT, CL (S) of gentamicin increased from (2.2±0.5)ml·min -1 ·kg -1 to (2.7±0.3)ml·min -1 ·kg -1 . Conclusion Simulated weightlessness might induce pharmacokinetic changes.
出处
《航天医学与医学工程》
CAS
CSCD
1999年第5期333-337,共5页
Space Medicine & Medical Engineering
关键词
失重模拟
药代动力学
庆大霉素
兔
weightlessness simulation
pharmacokinetics
gentamicin
rabbits Address reprint requests to:GUO Zhi feng.Institute of Space Medico-Engineering,Beijing 100094,China
