聚合物对尼群地平无定形固体分散体结晶抑制作用的研究  

Studies on crystallization inhibition effects of polymers on nitrendipine amorphous solid dispersions

作　　者：李沫 徐万魁 曲建国 孙苓苓 LI Mo;XU Wankui;QU Jianguo;SUN Lingling(Liaoning Institute for Drug Control,Shenyang 110036,China)

机构地区：[1]辽宁省药品检验检测院,辽宁沈阳110036

出　　处：《沈阳药科大学学报》2024年第8期1067-1073,共7页Journal of Shenyang Pharmaceutical University

摘　　要：目的 评价不同聚合物对尼群地平(nitrendipine,NTD)无定形固体分散体(amorphous solid dispersion,ASD)的结晶抑制作用。方法 采用溶剂蒸发法,分别以PVP、PVP VA和Soluplus等3种聚合物为载体,制备90%载药量的尼群地平无定形固体分散体(NTD_(90%)-ASD)。以熔融淬冷法制备的无定形NTD药物为对照,采用偏光显微镜、差示扫描量热仪和粉末X-射线衍射仪对样品进行物相表征。再采用偏光显微镜,观察无定形NTD和NTD_(90%)-ASD的结晶过程,并计算结晶速率。结果 相较于无定形NTD,3种NTD_(90%)-ASD的结晶速率明显降低。结论 Soluplus对无定形NTD有明显的结晶抑制作用,PVP VA次之,PVP的结晶抑制作用较弱。Objective To prepare amorphous solid dispersion(ASD) with different polymer carriers by using nitrendipine(NTD) as a model drug,and to evaluate the crystallization inhibition effects of different polymers on NTD ASD.Methods Amorphous NTD was prepared by the melt quenching method and characterized by using the polarizing microscope,the differential scanning calorimeter and the powder X-ray diffractometer.Subsequently,nitrendipine amorphous solid dispersions at a drug loading of 90%(NTD_(90%)-ASD) were prepared by solvent evaporation with three different polymers(PVP,PVP VA and Soluplus),and the physical characterization of THE ASD system was carried out.The crystallization rates of neat amorphous NTD and NTD_(90%)-ASD were studied using a polarizing microscope.Finally,the crystallization rates of each system were calculated.Results The crystallization rate of ASD was significantly lower than that of the neat amorphous NTD.Conclusion Soluplus has the best crystallization inhibition effects on amorphous NTD,followed by PVP VA and PVP.

关 键 词：无定形固体分散体 结晶抑制 聚合物 尼群地平 

分 类 号：R917[医药卫生—药物分析学]