药学学报, 2021, 56(9): 2513-2521
引用本文:
王洪亮, 董武军, 陈蕾, 叶军, 王艳宝, 刘玉玲. 叔丁醇在生物医药领域的主要应用及研究进展[J]. 药学学报, 2021, 56(9): 2513-2521.
WANG Hong-liang, DONG Wu-jun, CHEN Lei, YE Jun, WANG Yan-bao, LIU Yu-ling. Tert-butanol application and related research progress in biomedicine[J]. Acta Pharmaceutica Sinica, 2021, 56(9): 2513-2521.

叔丁醇在生物医药领域的主要应用及研究进展
王洪亮1, 董武军2, 陈蕾3, 叶军1, 王艳宝1, 刘玉玲1*
1. 中国医学科学院、北京协和医学院药物研究所, 药物传输技术及新型制剂北京市重点实验室, 北京 100050;
2. 国家食品药品监督管理总局药品审评中心, 北京 100038;
3. 国家药典委员会, 北京 100061
摘要:
叔丁醇是一种广泛应用于医药化工领域的有机溶剂,具有高结晶温度和高蒸汽压的特点,在冻干过程中易于升华而去除。本文介绍了叔丁醇作为难溶性药物冻干制剂中的助溶剂、多孔结构制剂的冻干溶媒和冰晶生长引导剂等方面的重要作用。另外,也概括了其在纳米制剂、包合物和气凝胶等方面的主要应用,并分析了叔丁醇的国内外质量标准现状、在制剂中的残留和检测方法,以及其安全性的法规要求。通过对已有研究的综述与总结,对当前研究的不足和未来的方向也进行了探讨。
关键词:    叔丁醇      药物制剂      难溶性药物      冻干      安全性     
Tert-butanol application and related research progress in biomedicine
WANG Hong-liang1, DONG Wu-jun2, CHEN Lei3, YE Jun1, WANG Yan-bao1, LIU Yu-ling1*
1. Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences&Peking Union Medical College, Beijing 100050, China;
2. Center for Drug Evaluation, National Medical Products Administration, Beijing 100038, China;
3. Chinese Pharmacopoeia Commission, Beijing 100061, China
Abstract:
Tert-butanol is an organic solvent, widely used in the medical field and chemical industry. It could be characterized by high crystallization temperature and vapor pressure. It could be easily sublimed and removed during the freeze-drying process. This review mainly describes the use of tert-butanol in the lyophilized formulations of poorly soluble drugs, the lyophilization solvent of porous structure productions, and as an ice crystal growth guider. In addition, the application of tert-butanol in nano drugs and aerogels has also been reviewed, as well as the current research progress in its quality and safety.
Key words:    tert-butanol    pharmaceutical preparation    poorly water-soluble drug    freeze drying    safety   
收稿日期: 2021-05-24
DOI: 10.16438/j.0513-4870.2021-0785
基金项目: “十三五”国家科技重大专项(2018ZX09711001-002-005).
通讯作者: 刘玉玲,Tel:86-10-83160332,E-mail:ylliu@imm.ac.cn
Email: ylliu@imm.ac.cn
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