摘要
目的：考察20（S）-原人参二醇（PPD）聚乳酸微球的体外释放特征,初步评价微球中药物在大鼠体内药动学行为。方法：考察微球在体外长期和加速条件下的释药特性、释放相关性,进行方程拟合以阐述释药机制;初步评价单次注射给予普通药物溶液及微球后,药物在大鼠体内的药动学行为。结果：微球体外长期释放体现良好缓释效果,在0.5 h内无明显突释,当释放达到38 d时,微球的累积释放率达到83.6%;体外长期释放曲线符合Higuchi方程,药物释放以扩散机制为主;长期与加速释放的累积释放率经拟合相关性好;微球在大鼠体内给药后,能够缓慢释放药物长达11 d,与普通药物溶液静脉组相比,t1/2延长17.5倍,MRT延长22.8倍,体现了明显的体内缓释特性。结论：体内外释放实验数据均表明该微球具有良好的缓释效果。
Objective： To investigate the in vitro release characteristics of 20（ S）-protopanaxadiol polylactic acid microspheres and evaluate the pharmacokinetic properties of the microspheres in rats. Methods： The in vitro release performance and correlation characteristics of microspheres were investigated under long-term and accelerated conditions,with which the mechanism of drug-release was estimated by fitting equation. The effects of the single dose of injection and microspheres were respectively evaluated with pharmacokinetic behavior in rats. Results： The results of long-term release investigations of the microspheres showed good sustained-release effects,with no burst release within the first 0. 5 h. The cumulative release rate of the microspheres reached 83. 6%,while the release time reached 38 d. The in vitro long-term release curve was consistent with Higuchi equation,which indicated the release performance was related with diffusion mechanism. It also showed that the cumulative release rate of long-term and accelerated release was well-correlated. After drug single administration in rats,the drug sustained released within 11 days in vivo. Compared with the normal drug solution group,t1/2 was extended by 17. 5 times and MRT extended by 22. 8 times,which illustrated an obvious property of a sustained-release agent in vivo. Conclusion： Both in vitro and in vivo release performance showed that microspheres showed good sustained-releasing effects.
出处
《中华中医药学刊》
CAS
北大核心
2018年第3期609-612,共4页
Chinese Archives of Traditional Chinese Medicine
基金
国家自然科学基金项目(81303233)
