睾酮放免测定法研究醋酸亮丙瑞林口服在大鼠体内的吸收

The testosterone release profiles in rats by oral administration of leuprolide

目的:建立亮丙瑞林口服给药剂量与睾酮释放间的量效关系。方法:对雄性大鼠分别灌胃给予0.005,0.05,0.5,1,5,10μg/kg,于0、1、2、4、8、12、24h取血0.5ml,血清用RIA测定睾酮含量。结果:大鼠灌胃给予亮丙瑞林游离药物1μg/kg为最大无效剂量。5μg/kg亮丙瑞林足以促进睾酮释放,再增加剂量时,睾酮浓度增加并不明显。结论:亮丙瑞林口服给药剂量与睾酮释放不成线性。

Objective： To establish the relationship between the oral administration dose of leuprolide and the release of testosterone in rats. Methods： Different doses （0.005, 0.05, 0.5, 1, 5, 10 μg/kg） were intragastrically given to male rats. Blood samples （0.5 ml） were taken at 0, 1, 2, 4, 8, 12, 24 h. The serum testosterone level was measured by RIA. Results： Oral administration of 1 μg/kg leuprolide was the maximum ineffective dose. Administration of 5 μg/kg was enough to promote testosterone release. Further increase in the dose did not promote more testosterone release. Conclusion： The oral administration dose of leuprolide is not linearly related to the testosterone release.