苯甲酸雌二醇羟丙基倍他环糊精包合工艺研究  

Study on the Inclusion Process of Estradiol Benzoate and Hydroxypropyl Betacyclodextrin

作　　者：黄孟秋 李同根 黄子健 周小琴 陈红英 Huang Mengqiu;Li Tonggen;Huang Zijian;Zhou Xiaoqin;Chen Hongying(Guangzhou Baiyunshan Mingxing Pharmaceutical Company Limited.,Guangzhou 510250,China)

机构地区：[1]广州白云山明兴制药有限公司,广东广州510250

出　　处：《广东化工》2022年第23期44-46,40,共4页Guangdong Chemical Industry

摘　　要：目的:以羟丙基-β-环糊精(HP-β-CD)为包合材料,对苯甲酸雌二醇进行包合,制备水溶性苯甲酸雌二醇注射液,完成包合工艺研究,以解决苯甲酸雌二醇水溶性差、油针制剂易带来不良反应的问题。方法:以苯甲酸雌二醇溶解度为评价指标衡量包合效果,研究HP-β-CD对苯甲酸雌二醇的包合作用,优化包合工艺,通过含量测定、DSC、扫描电镜等分析方法对包合体系进行评价。结果:优选得到最佳包合工艺,苯甲酸雌二醇:HP-β-CD包合体系的摩尔比m(HP-β-CD)∶m(苯甲酸雌二醇)-1∶1、超声频率40 KHz、超声功率400 W、包合时间1.5 h,制备得到的苯甲酸雌二醇注射液含量符合临床使用需求。结论:采用超声法制备苯甲酸雌二醇HP-β-CD包合体系工艺简单、产品质量稳定且重现性良好,包合后可显著改善其水溶性,为苯甲酸雌二醇更安全有效的临床应用提供了新思路。Objective: To prepare water-soluble estradiol benzoate injection by using hydroxypropyl-β-cyclodextrin(HP-β-CD) as the inclusion material, and to complete the inclusion process research in order to solve the problems of poor water-solubility of estradiol benzoate, and easy to bring adverse reactions as the oil injection formulation. Methods: Estradiol benzoate solubility was used as an evaluation index to measure the inclusion effect, to study the inclusion effect of HP-β-CD on estradiol benzoate, to optimize the inclusion process, and to evaluate the inclusion system by content determination, DSC, SEM and other analytical methods. The results: Estradiol benzoate: HP-β-CD inclusion system with molar ratio m(HP-β-CD)∶m(Estradiol benzoate)=1∶1, ultrasonic frequency 40 KHz,ultrasonic power 400 W, inclusion time 1.5 h. The content of the prepared Estradiol benzoate injection meets the clinical use requirements. Conclusion: The preparation of estradiol benzoate HP-β-CD inclusions by ultrasonication is simple, stable and reproducible, and the water solubility of estradiol benzoate can be significantly improved after inclusions, which provides a new idea for a safer and more effective clinical application of estradiol benzoate.

关 键 词：HP-β-CD 苯甲酸雌二醇 超声法 包合工艺 包合体系 

分 类 号：TQ[化学工程]