摘要
以羟丙基-β-环糊精(HP-β-CD)为载体,以无水乙醇为溶剂,采用溶剂法制备了依鲁替尼固体分散体,对其制备工艺进行了优化,并通过傅立叶变换红外光谱法(FTIR)、X-射线衍射法(XRD)、差示扫描量热法(DSC)、热重法(TG)和扫描电镜法(SEM)对依鲁替尼固体分散体进行了系统表征。结果表明,最佳制备工艺为:依鲁替尼与载体HP-β-CD的质量比1∶15、反应温度50℃、反应时间30 min,在此条件下,依鲁替尼固体分散体的溶出效果最佳,5 min时体外累积溶出度达到78.87%,远高于原料药依鲁替尼(9.12%);原料药依鲁替尼以无定形态均匀分布于载体HP-β-CD中。
Using hydroxypropyl-β-cyclodextrin(HP-β-CD)as a carrier and anhydrous ethanol as a solvent,we prepared Ibrutinib solid dispersion by a solvent method,and optimized the preparation process.Moreover,we characterized the Ibrutinib solid dispersion by Fourier transform infrared spectroscopy(FTIR),X-ray diffraction(XRD),differential scanning calorimetry(DSC),thermogravimetry(TG),and scanning electron microscopy(SEM).The results show that the optimal preparation process is determined as follows:the mass ratio of Ibrutinib to carrier HP-β-CD of 1∶15,the reaction temperature of 50℃,and the reaction time of 30 min.Under above conditions,the dissolution effect of Ibrutinib solid dispersion is the best,and the cumulative dissolution in vitro of Ibrutinib can reach 78.87%at 5 min,which is much higher than that of active pharmaceutical ingredient(API)Ibrutinib(9.12%).Ibrutinib is uniformly dispersed in carrier HP-β-CD with amorphous form.
作者
汪涛
冯菊红
张朵朵
陈雅婷
盛余豪
胡学雷
WANG Tao;FENG Juhong;ZHANG Duoduo;CHEN Yating;SHENG Yuhao;HU Xuelei(School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China;Key Laboratory of Green Chemical Engineering Process of Ministry of Education,Wuhan 430205,China)
出处
《化学与生物工程》
CAS
2023年第3期25-29,共5页
Chemistry & Bioengineering
基金
湖北省自然科学基金重点项目(2011CDA048)。
关键词
依鲁替尼
固体分散体
体外累积溶出度
溶剂法
Ibrutinib
solid dispersion
cumulative dissolution in vitro
solvent method
作者简介
汪涛(1998-),男,山东济宁人,硕士研究生,研究方向:药物合成及制剂,E-mail:2395507003@qq.com;通讯作者:冯菊红,博士,讲师,研究方向:有机合成与制药化学,E-mail:jhfeng@wit.edu.cn。
