摘要
以羟丙基-β-环糊精(HP-β-CD)为包合材料,制备阿司匹林包合物,以解决阿司匹林水溶性差、易水解的问题,并减轻其口服给药对胃肠道的刺激性。以阿司匹林包合率为评价指标衡量包合效果,筛选包合物的制备方法,优化包合工艺,通过TLC、DSC等分析方法对包合物进行评价。结果表明,制备阿司匹林HP-β-CD包合物的最佳方法为超声法,最佳工艺为m(HP-β-CD)∶m(阿司匹林)=3∶1、包合温度40℃、超声频率40 KHz、输入功率200 W、包合2.0 h,所得包合物对阿司匹林的包合率为52.85%;TLC、DSC等检测方法显示阿司匹林能够被充分包埋于HP-β-CD空腔内,且二者相容性良好。采用超声法所制备的羟丙基-β-环糊精包合物工艺简单、稳定且包合率较高,包合可改善其水溶性及稳定性,为阿司匹林更广泛的临床应用提供了新思路。
Using the hydroxypropyl-β-cyclodextrin(HP-β-CD)as material to inclusion aspirin to improve its water solubility and stability,and reduce the irritation of oral administration to gastrointestinal tract.Using the HP-β-CD as inclusion material,aspirin inclusion rate as evaluation index,the preparation method of inclusion screened and its process optimized by single factor test.The inclusion complex was evaluated by the TLC and DSC analysis.The ultrasonic method is the best preparation method,when the ratio of aspirin and HP-β-CD was 1∶3,temperature at 40℃,and when the ultrasonic frequency was 40 KHz and the input power was 200 W,the inclusion rate for HP-β-CD inclusion complex of aspirin was 52.85%after 2.0 hours.The TLC and DSC analysis indicated that the formation of complex,and showed that aspirin can be fully embedded in the cavity of HP-β-CD,and the compatibility is good.The developed inclusion process of HP-β-CD inclusion complex of aspirin is simple,stable and reliable,with a high inclusion rate,good solubility and high stability,which provides a new idea for wider clinical application of aspirin.
作者
赵宁
李伟泽
付丽娜
施晶晶
张湛睿
ZHAO Ning;LI Weize;FU Lina;SHI Jingjing;ZHANG Zhanrui(Xi′an Medical University,School of Pharmacy,Xi′an 710021,China)
出处
《化工科技》
CAS
2021年第6期11-15,共5页
Science & Technology in Chemical Industry
基金
国家自然科学-青年基金项目(82004075)
陕西省教育厅自然科学基金项目(19JK0759)
陕西省科技厅项目(2020JM-610)
陕西高校青年创新团队建设项目(陕教[2019]90号)
西安医学院国家自然科学基金培育项目(2017GJFY10)
西安医学院药学省级重点学科建设项目(2016YXXK07,2016YXXK20)。
关键词
HP-β-CD
包合物
阿司匹林
Hydroxypropyl-β-cyclodextrin
Inclusion complex
Aspirin
