摘要
为了改善舒尼替尼的溶解度进而提高其生物利用度,采用溶剂蒸发法制备了舒尼替尼固体分散体,通过体外溶出实验对制备工艺进行了优化,通过FTIR、XRD、SEM和DSC对固体分散体进行了表征,并对舒尼替尼固体分散体胶囊剂的处方和制备工艺进行了研究。结果表明,在舒尼替尼与载体γ-环糊精的质量比为1∶5、反应温度为60℃、反应时间为60 min的最佳条件下制备的舒尼替尼固体分散体的溶出效果最佳,体外累积溶出度可达到82.88%;舒尼替尼以无定型态分散于载体γ-环糊精中,加快了药物的溶出速度;以舒尼替尼固体分散体为原料制备的胶囊剂的体外累积溶出度较市售胶囊剂有显著提高。
In order to improve the solubility of Sunitinib and thereby enhance its bioavailability,we prepared Sunitinib solid dispersion by a solvent evaporation method.Moreover,we optimized the preparation process of Sunitinib solid dispersion through in vitro dissolution experiments,and characterized Sunitinib solid dispersion by FTIR,XRD,SEM,and DSC.Furthermore,we studied the formulation and preparation process of Sunitinib solid dispersion capsule.The results indicate that Sunitinib solid dispersion with the best dissolution effect is prepared under the optimal conditions as follows:the mass ratio of Sunitinib andγ-cyclodextrin is 1∶5,the reaction temperature is 60℃,and the reaction time is 60 min,and the in vitro cumulative dissolution can reach 82.88%.Sunitinib is dispersed in an amorphous state on the carrierγ-cyclodextrin,the dissolution speed of drugs is accelerated.The in vitro cumulative dissolution of the capsule prepared from Sunitinib solid dispersion is significantly higher than that of the commercial capsule.
作者
陈雅婷
冯菊红
汪诗雨
周洁
刘云
沈宇寒
胡学雷
CHEN Yating;FENG Juhong;WANG Shiyu;ZHOU Jie;LIU Yun;SHEN Yuhan;HU Xuelei(School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430074,China;Key Laboratory for Green Chemical Process of Ministry of Education,Wuhan 430074,China)
出处
《化学与生物工程》
CAS
2023年第6期28-34,共7页
Chemistry & Bioengineering
基金
湖北省自然科学基金重点项目(2011CDA048)。
关键词
舒尼替尼
固体分散体
溶剂蒸发法
胶囊剂
体外累积溶出度
Sunitinib
solid dispersion
solvent evaporation method
capsule
in vitro cumulative dissolution
