黄体酮缓释栓的制备及药动学  

Study on the preparation of sustained-release suppository of progesterone and its pharmacokinetics in rabbits

作　　者：龙利红[1] 黄群[2] 侯淑贤[1] 代宗顺[1] 

机构地区：[1]华中科技大学同济医学院药理学系,湖北武汉430030 [2]武汉协和医院免疫室,湖北武汉430022

出　　处：《中国医院药学杂志》2006年第2期156-160,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研制黄体酮缓释栓,研究其家兔药动学。方法:采用正交设计法,以体外释放度为指标,优化黄体酮缓释栓的处方。体外释放度采用中国药典2000年版二部转篮法,体内血药浓度用磁性分离酶联免疫法和3P97程序计算药动学参数。结果:体外释放行为符合零级动力学;体内过程为二室模型,药动学参数为t1/2Ke=12.7h,tpeak=0.5h,Cm ax=48.8μg.L-1,AUC0-24h=385.1μg.L-1.h。结论:该制剂具有缓释特征。OBJECTIVE To study a sustained release suppository of progesterone in order to provide a new preparation of progesterone with prolonged effective time for clinic. METHODS The drug release of progesterone was determined in vitro according to Volume H of the Chiese Pharmacopoeia 2000. The blood concentration in vivo was determined by ELISA. The 3P97 program was used to calculate the pharmacokinetic parameters of progesterone. RESULTS The dissolution of progesterone was 92.43% within 12 h. The drug release pattern in vitro was best described by zero-order kinetics and in vivo profile was demonstrated to fit two compartment mod- el. The pharmacokinetic parameters were t1/2Ke=12.7h,tpeak=0.5h,Cmax=48.8μg·L^-1,AUC0.24h=385.1μg·L^-1·h, respective- ly. CONCLUSION This preparation has the characteristio of sustained releasing.

关 键 词：黄体酮 缓释栓 药动学 

分 类 号：R944[医药卫生—药剂学]