【摘要】 目的研究聚乙二醇6000对间尼索地平溶解度和体外溶出度的影响,为间尼索地平剂型的选择提供参考。方法以聚乙二醇(PEG)6000为载体,采用溶剂-熔融法制备间尼索地平固体分散体。应用差示扫描量热分析法(DSC)、X射线粉末衍射光谱(XRD)对固体分散体进行鉴定,紫外分光光度法测定固体分散体的溶解度和体外溶出度。结果固体分散体的DSC、XRD图谱与原料药及其物理混合物均不同,不同比例的间尼索地平-聚乙二醇固体分散体的溶解度及体外溶出度均高于原料药,2 h的溶出百分率:原料药26.80%,固体分散体(1∶3,1∶5,1∶7)分别为35.31%,38.71%,41.48%,比例相同的固体分散体的溶出率高于其物理混合物。结论间尼索地平与聚乙二醇6000形成了低共熔物,聚乙二醇6000作为间尼索地平的载体,可加速其体外溶出。更多还原

【Abstract】 Objective To investigate the influences of polyethylene glycol 6000 on the solubility and in vitro dissolution of m-nisoldipine,which could provide guidance for chosing formulations of m-nisoldipine. Methods Solid dispersions of mnisoldipine were prepared by solvent-melting method with polyethylene glycol 6000 matrix. DSC and XRD spectroscopy were applied to identify the solid dispersions. The solubility and in vitro dissolution were detected by UV spectroscopy. Results The DSC and XRD map were different from the crude drug and their physical mixtures. The dissolution rates( 1∶ 3,1∶ 5,1∶ 7) were faster( 35. 31%,38. 71%,41. 48%) than that of the crude drug( 26. 80%),and the dissolution rates of the solid dispersions in the same ratio were higher than the physical mixtures. Conclusion DSC analysis indicated that eutectic compounds were produced by the m-nisoldipine and polyethylene glycol,in which polyethylene glycol6000 acts as a carrier. The solubility and in vitro dissolution of m-nisoldipine can be increased.更多还原