Advanced methodologies for cocrystal synthesis

被引:179
作者
Douroumis, Dennis [1 ]
Ross, Steven A. [1 ]
Nokhodchi, Ali [2 ,3 ,4 ]
机构
[1] Univ Greenwich, Sch Sci, Fac Engn & Sci, Chatham ME4 4TB, Kent, England
[2] Univ of Sussex, Sch Life Sci, Pharmaceut Res Lab, Arundel Bldg, Brighton BN1 9QG, E Sussex, England
[3] Tabriz Univ Med Sci, Drug Appl Res Ctr, Tabriz, Iran
[4] Tabriz Univ Med Sci, Fac Pharm, Tabriz, Iran
关键词
Cocrystals; Mechanochemical grinding; Hot melt extrusion; Spray; -; drying; Antisolvent; Freeze; Microfluidics; Ultrasound; Scale-up; Continuous; PHARMACEUTICAL CO-CRYSTALS; HOT-MELT EXTRUSION; INDOMETHACIN-SACCHARIN COCRYSTALS; TWIN-SCREW EXTRUSION; SOLID-STATE; SCALE-UP; ACID COCRYSTALS; STRUCTURAL-CHARACTERIZATION; ASSISTED COCRYSTALLIZATION; PHYSICOCHEMICAL PROPERTIES;
D O I
10.1016/j.addr.2017.07.008
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Pharmaceutical cocrystals are multicomponent systems composed of two or more molecules and held together by H-bonding. Currently, cocrystals provide exciting opportunities in the pharmaceutical industry for the development and manufacturing of new medicines by improving poor physical properties of Active Pharmaceutical Ingredients (APIs) such as processability, solubility, stability and bioavailability. According to the recent reclassification, cocrystals are considered as drug polymorph rather a new API which has a significant impact on drug development, regulatory submissions and intellectual property protection. This review summarizes recent trends and advances in synthesis, manufacturing and scale - up of cocrystals. The operational principles of several cocrystals manufacturing technologies are discussed including their advantages and disadvantages in terms of crystal quality, purity stability, throughput and limitations in large scale production. (C) 2017 Elsevier B.V. All rights reserved.
引用
收藏
页码:178 / 195
页数:18
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