氢化泼尼松-羟基丁酸酯-羟基戊酸酯共聚物纳米粒制备与性质  

PREPARATION AND CHARACTERIZATION OF PREDNISOLONE-POLY (HYDROXYBUTYRATE-CO-HYDROXYVALERATE) NANOPARTICLES

作　　者：陈建海[1] Shagufta M Davis SS 

机构地区：[1]第一军医大学南方医院药学部,广东广州510515 [2]Department of Pharmaceutical Science

出　　处：《药学学报》2002年第6期473-476,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目 ( 39970 2 2 3)

摘　　要：目的　用新型生物可降解材料羟基丁酸酯 羟基戊酸酯共聚物 (PHBV)为载体 ,以氢化泼尼松(prednisolone ,PNS)为模型药制备PNS PHBV纳米粒 (NP)。方法　用超声乳化法制备PNS PNBV纳米粒 ,激光粒度分析仪测试NP的粒径及其分布以及粒子表面的Zeta电位。结果　NP的粒径为 5 0～ 2 5 0nm。随着药 载比增加 ,NP的载药量也增大 ,但包封率与Zeta电位却明显下降 ;体外释药曲线表现出明显两相释药特征 ,伴随着不同程度突释效应 ,粒径越小突释效应越大 ,体外释药最长达 3 2h。结论　PNS PNBV纳米粒制备工艺稳定 。AIM To optimize the preparation of sustained release prednisolone poly(hydroxybutyrate co hydroxyvalerate) (PNS PHBV) nanospheres (NP) using the novel biodegradable materials PHBV as the carriers and PNS as a model drug. METHODS PNS PHBV nanospheres were prepared by ultrasonic emulsion technique. The diameter, its distribution and Zeta potential on the surface of particles were measured by means of Zetasizer. RESULTS The diameter of NP is in the range of 50～250 nm. The drug loading of NP increases but incorporation efficiency and Zeta potential dramatically decrease with increasing ratio of the feeding quantities of drug to those of carriers. The drug release behavior in vitro appeared to have biphasic characteristics with initial burst effect. The more burst effect, the less the diameters of nanoparticles. The longest release time was up to 32 h. CONCLUSION The technology of preparation is reasonable and PNS PHBV nanoparticle showed significant sustained release.

关 键 词：羟基丁酸酯-羟基戊酸酯 共聚物 氢化泼尼松 缓释作用 纳米粒 制备工艺 超声乳化法 

分 类 号：TQ460.6[化学工程—制药化工] TB38[一般工业技术—材料科学与工程]