吗啡缓释栓的研制及其体内外释药相关性研究

目的：制备吗啡缓释栓。经家兔直肠给药，考察缓释栓剂释药的体内外相关性。方法：以聚乙二醇为基质，添加阻滞剂卡波姆，氮酮为促渗透剂制备吗啡缓控释栓；采用自行设计的体外溶出装置进行体外筛选；以大白兔为动物模型进行体内筛选；采用3p87程序计算药代动力学参数。结果：制备的吗啡缓释栓的体外释药性能良好，缓释时限〉7h。当体外释药符合零级模式，且R^2〉0．9时，体内药物释放出现平台，显示了良好的体内外相关性；体内释药过程为二室模型，MRT=8．221h,Tpeak=2．857h，Cmax=12．944μg/ml，AUC=127．275（μg／ml）·h。结论：所制备的吗啡栓剂具有良好的缓释特征。

Study on sustained release suppositories of morphine and its pharmacokinetics in rabbits

Objective： To prepare sustained release suppositories of morphine and evaluate its characteristics between vitro release and vivo absorption. Methods： The drug release of morphine in vitro was studied with new scanning instrument made by our lab and the drug absorption in vivo that was performed in rabbits. The 3p87 program was used to calculate the pharmacokinetic parameters of morphine. Results： Drug release pattern in vitro was best described by zero-order kinetics and in vivo profile was demonstrated to fit two compartment model.The pharmacokinetics pharmerers were： MRT=8.221 h, Tpeak=2.857 h, Cmax=12.944 μg/ml, AUC=1273（μg/ml）·h, Conclusion： This preparation has the characteristic of sustained releasing.