纳米晶体药物制备技术的研究进展  

Research progress on preparation technology of nanocrystal drugs

作　　者：田阳 彭一凡 张志伟 张慧 高翔[1] TIAN Yang;PENG Yi-fan;ZHANG Zhi-wei;ZHANG Hui;GAO Xiang(China Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850)

机构地区：[1]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《药学学报》2021年第7期1902-1910,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81573357);国家新药关键技术研究开发计划(2018ZX09721003-007/2018ZX09J18107).

摘　　要：纳米晶体药物具有无需载体材料、易工业化和剂型多样化,且能显著提高难溶性药物的溶解度和生物利用度等优势,已经有多种药物上市。传统的纳米晶制备技术存在制备效率低和最小可实现粒径的工艺限制的问题。随着药物制剂制备技术的进步,纳米晶体药物的制备技术也在不断提升,不断涌现出新的制备技术。新技术的出现大大缩短了工艺时间,使制备更小粒径的纳米晶体药物成为可能。本文从“Top-down”技术、“Bottom-up”技术及组合技术三个方面对纳米晶体药物的制备技术,尤其是高重力控制沉淀法、微射流反应技术和多种组合技术等新型制备技术进行了综述,并对新型制备技术的发展进行了展望,以期为纳米制剂相关研究提供借鉴。Nanocrystal drugs have many advantages,such as no carrier materials,easy industrialization,diversified dosage forms,and can significantly improve the solubility and bioavailability of insoluble drugs,so many drugs have been on the market.The traditional nanocrystal preparation technology has the problems of low preparation efficiency and process limitation of the smallest achievable particle size.With the progress of pharmaceutical preparation technology,the preparation technology of nanocrystal drugs is constantly improving,and new preparation technologies are constantly emerging.The emergence of new technologies has greatly shortened the process time and makes it possible to prepare nanocrystal drugs with smaller particle diameters.In this paper,the preparation technologies of nanocrystal drugs,especially the new preparation technologies such as high gravity controlled precipitation,microfluidic reaction technology and various combination technologies,are reviewed from three aspects:"Top-down"technology,"Bottom-up"technology and combination technology.This article also prospects the development of new preparation technologies,hoping to provide reference for the related research of nanopreparations.

关 键 词：纳米晶体 难溶性药物 制备技术 溶解度 生物利用度 

分 类 号：R943[医药卫生—药剂学]