摘要
目的:制备复合载体齐墩果酸固体分散体,提高齐墩果酸的溶出度。方法:采用溶剂法,以聚乙烯吡咯烷酮(PVP VA64)和聚乙烯己内酰胺-聚乙酸乙烯酯-聚乙二醇接枝共聚物(Soluplus)为复合载体,制备齐墩果酸固体分散体,以累积溶出度为评价指标,考察不同载体比例,药物与载体比例,筛选最佳工艺。通过差式扫描量热法(DSC)、扫描电镜(SEM)、傅里叶红外光谱(FTIR)、粉末X射线衍射(XRPD)等技术手段对其表征,并考察其溶出度。结果:Soluplus和PVP VA64复合载体比例为3∶2,药物与载体比例为1∶7,制备固体分散体,在45 min时累积溶出度为92.43%,DSC、SEM、XRPD、FTIR等表征结果显示药物以无定形状态存在于固体分散体中,且药物与载体之间存在氢键相互作用。结论:Soluplus和PVP VA64作为复合载体材料,联合应用可显著提高齐墩果酸的体外溶出度。
OBJECTIVE To prepare oleanolic acid solid dispersion with composite carrier and improve the dissolution of oleanolic acid.METHODS Solid dispersion of oleanolic acid was prepared by solvent method with PVP VA64 and Soluplus graft copolymer as composite carrier.They were characterized by differential scanning calorimetry(DSC),scanning electron microscopy(SEM),Fourier transform infrared spectroscopy(FTIR),and powder X-ray diffraction(XRPD),and their dissolution was investigated.RESULTS The solid dispersion was prepared by Soluplus and PVP VA64 composite carrier in a ratio of 3∶2,the drug to carrier ratio of 1∶7,and the cumulative dissolution percentage in vitro was as high as 92.43%in 45 minutes.DSC,SEM,XRPD,FTIR and other characterization results showed that the drug existed in the solid dispersion in an amorphous state,and there was hydrogen bond interaction between drug and carrier.CONCLUSION As a composite carrier material,Soluplus and PVP VA64 can significantly improve the in vitro dissolution of oleanolic acid.
作者
武倩
常金花
薛禾菲
程佳慧
赵强
刘喜纲
WU Qian;CHANG Jin-hua;XUE He-fei;CHENG Jia-hui;ZHAO Qiang;LIU Xi-gang(Hebei Key Labo-ratory of Research and Development for Traditional Chinese Medicine,Institute of Chinese Materia Medica of Chengde Medical University,Hebei Chengde 067000,China)
出处
《中国医院药学杂志》
CAS
北大核心
2020年第4期385-390,共6页
Chinese Journal of Hospital Pharmacy
基金
河北省高等学校科学技术研究项目(编号:QN2018057),河北省高校重点学科建设项目(冀教高[2013]4)。
