超临界流体技术制备辛伐他汀/PLLA-PEG缓释复合微球Preparation of Simvastatin/PLLA-PEG Sustained-Release Microspheres by Supercritical Fluid Technology
颜庭轩,王志祥,黄德春,宋杏芳
摘要(Abstract):
采用超临界流体(SCF)技术制备具有缓释效果的辛伐他汀/左旋聚乳酸(PLLA)-聚乙二醇(PEG)复合微球,以载药量和粒径为指标考察了结晶压力、结晶温度以及辅料浓度等操作参数对复合微球的影响。由单因素实验得到较优工艺条件为:结晶压力12 MPa,结晶温度45℃,PEG浓度6 mg?mL?1。在此工艺条件下制备得到的复合微球载药量为12.65%,粒径为6.24μm;通过红外(IR)、差示扫描量热法(DSC)以及扫描电镜(SEM)分析表明辛伐他汀可能与PLLA形成氢键结合,并以无定型形式复合于微球中;PEG均匀复合于微球骨架中。体外溶出实验表明辛伐他汀/PLLA-PEG缓释微球具有良好的缓释效果。实验结果表明,采用SCF技术可制备得到辛伐他汀/PLLA-PEG缓释微球,添加适量PEG可有效增加载药量,提高药物溶出速率。
关键词(KeyWords): 超临界流体技术;辛伐他汀;聚乙二醇;左旋聚乳酸;缓释
基金项目(Foundation): 江苏省自然科学基金资助项目(BK2012763)
作者(Author): 颜庭轩,王志祥,黄德春,宋杏芳
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