摘要
氟比洛芬(FLU)是一种经典芳基丙酸类非甾体抗炎药,具有消炎、镇痛和解热作用。但氟比洛芬水溶性低,导致其口服吸收不完全。本文目的是期望通过制备药物共晶来调节氟比洛芬的水溶性。本研究采用溶剂缓慢挥发法和溶剂辅助研磨法成功制备了3种摩尔比为2:1的氟比洛芬共晶(包括氟比洛芬-4,4’-联吡啶(BIP)共晶、氟比洛芬-1,2-二(4-吡啶基)乙烯(BPE)共晶和氟比洛芬-吩嗪(PHEN)共晶),并对其晶体结构、Hirshfeld表面分析、理化性质和溶解度进行了研究。结果表明,药物共晶可以提高氟比洛芬的热稳定性和溶解度,并进一步探讨了改善氟比洛芬溶解度差异的原因。
Flurbiprofen(abbreviated as FLU) is a classical aromatic propionic acid non-steroidal anti-inflammatory drug with inflammatory,analgesic and antipyretic effects.However,the low water solubility of flurbiprofen leads to its incomplete oral absorption.The aim of this paper is to expect to regulate the aqueous solubility of flurbiprofen by preparing drug cocrystals.In this study,three flurbiprofen cocrystals with a molar ratio of 2:1(including flurbiprofen-4,4’-bipyridine(abbreviated as FLU-BIP) cocrystal,flurb iprofen-1,2-di(4-pyr idyl) ethylene(abbreviated as FLUBPE) cocrystal and flurbiprofen-phenoxazine(abbreviated as FLU-PHEN) cocrystal) were successfully prepared by solvent slow evaporation method,and their crystal structures,Hirshfeld surface analysis,physicochemical properties and solubility were investigated.The results showed that drug cocrystals could improve the thermal stability and solubility of flurbiprofen,and the reasons for improving the difference in solubility of flurbiprofen were further investigated.
作者
高蕾
覃有英
李莹洁
玉雨灵
张宪瑞
Gao Lei;Qin Youying;Li Yingjie;Yu Yuling;Zhang Xianrui(School of Food Science and Pharmaceutical Engineering,Wuzhou University,Guangxi,543000)
出处
《当代化工研究》
2023年第3期185-187,共3页
Modern Chemical Research
基金
广西科技基地和人才专项“利用超分子合成子改善芳基丙酸类非甾类抗炎药的水溶性”(项目编号:桂科AD20159051)
广西高校中青年教师科研基础能力提升项目“沙芬酰胺药物固态化学研究”(项目编号:2020KY17020)
大学生创新创业训练计划项目“基于吡啶和吡嗪配体基团设计合成氟比洛芬共晶”(项目编号:202211354010)。
关键词
氟比洛芬
共晶
晶体结构
理化性质
溶解度
flurbiprofen
cocrystal
crystal structure
physicochemical property
solubility
