元胡止痛方两种有效组分固体分散体的制备与评价
Chinese Journal of Pharmaceuticals(2016)
Abstract
捅要:为提高元胡止痛方中2个有效组分延胡索乙素(1)和欧前胡素(2)的口服生物利用度,采用溶剂挥发法制备其固体分散体.优化结果表明,载体材料宜选用聚乙烯吡咯烷酮(PVP K30),药物(1∶2=1∶1)与PVP K30的比例为1∶1.差示扫描量热和X-射线衍射分析结果表明,1和2均以无定形状态存在于制剂中.与原料药相比,1和2的溶解度和溶出度均显著增加.大鼠药动学试验结果显示,与单独灌胃给予1和2原料药相比,固体分散体组大鼠血浆中1和2的AUC得到显著提高(P<0.05).以AUC0→t计算,1和2的相对生物利用度分别为155%和187%.可见,固体分散体可同时提高这2种有效成分的溶解度、溶出度和口服吸收.
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