药用辅料对无定形固体分散体中药物过饱和的影响  

Effects of pharmaceutical excipients on drug supersaturation in amorphous solid dispersions

作　　者：王会建 王衍飞 苏伟 付强[1,2] WANG Huijian;WANG Yanfei;SU Wei;FU Qiang(Wuya College of Innovation,Shenyang Pharmaceutical University,Shenyang 110016;Joint International Research Laboratory of Intelligent Drug Delivery Systems,Ministry of Education,Shenyang 110016,China)

机构地区：[1]沈阳药科大学无涯创新学院,沈阳110016 [2]智能药物递送系统设计与评价国际合作交流实验室,沈阳110016

出　　处：《中国药科大学学报》2024年第6期725-733,共9页Journal of China Pharmaceutical University

基　　金：辽宁省“兴辽英才计划”青年拔尖人才项目(XLYC2203044);辽宁省教育厅重点研究项目(JYTZD2023142);沈阳药科大学优秀青年提升计划(YQ202113)。

摘　　要：采用无定形固体分散体(amorphous solid dispersion,ASD)技术,可以将晶态的难溶药转变为高能量的无定形态,在胃肠道内形成具有动力学优势的药物过饱和溶液,有效提高其口服生物利用度。作为ASD的重要组成部分,药用辅料在很大程度上影响药物过饱和。因此,总结各类药用辅料对药物过饱和溶液的影响并明确其机制,对ASD的研发具有重要意义。本文综述了聚合物、小分子辅料以及多孔材料对ASD溶解后所形成药物过饱和溶液的影响,重点介绍了各类药用辅料对药物过饱和溶液的作用机制,为ASD处方中药用辅料的合理选择提供了理论指导。Using the amorphous solid dispersion(ASD)technology,poorly water-soluble drugs can be formulated into high-energy amorphous forms.After oral administration,a kinetic supersaturated solution is formed in the gastrointestinal tract,and oral bioavailability is thus effectively improved.As important components of ASDs,pharmaceutical excipients affect the supersaturation of ASDs.Therefore,it is significant to clarify the effects of various types of pharmaceutical excipients on the supersaturated solutions for the development of ASDs.This paper reviews the effects of polymers,small-molecule excipients,and porous materials on the supersaturated solutions formed after dissoptlution of ASD with an emphasis on the mechanisms of various types of pharmaceutical excipients on the supersaturated solutions,providing theoretical guidance for the rational selection of medicinal excipients in the development of ASDs.

关 键 词：药用辅料 无定形固体分散体 药物过饱和溶液 

分 类 号：R943[医药卫生—药剂学]