Advanced methodologies for cocrystal synthesis

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 A...

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Bibliographic Details
Published in:Advanced drug delivery reviews 2017-08, Vol.117, p.178-195
Main Authors: Douroumis, Dennis, Ross, Steven A., Nokhodchi, Ali
Format: Article
Language:English
Subjects:
Antisolvent
Chemistry, Pharmaceutical - methods
Cocrystals
Continuous
Crystallization
Freeze – drying
Hot melt extrusion
Mechanochemical grinding
Microfluidics
Pharmaceutical Preparations - chemistry
Scale-up
Spray – drying
Ultrasound
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Summary: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. [Display omitted]
ISSN:0169-409X
1872-8294
DOI:10.1016/j.addr.2017.07.008