Journal
ACTA PHARMACEUTICA SINICA B
Volume 11, Issue 8, Pages 2537-2564Publisher
INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
DOI: 10.1016/j.apsb.2021.03.030
Keywords
Pharmaceutical cocrystals; Cocrystal engineering; Physicochemical properties; Solid dosage forms; Crystallization
Categories
Funding
- National Natural Science Foundation of China [81872813]
- Outstanding Youth Fund of Jiangsu Province of China [BK20190029]
- Natural Science Foundation of Jiangsu Province [BK 20200576]
- Fundamental Research Funds for the Central Universities [2632020PY04]
- Program of State Key Laboratory of Natural Medicines-China Pharmaceutical University [SKLNMZZ202031]
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Pharmaceutical cocrystals are multicomponent systems where at least one component is an active pharmaceutical ingredient. Cocrystallization with a coformer is a promising approach to enhance pharmaceutical performance. This review provides a comprehensive overview of pharmaceutical cocrystals, their preparation methods, properties, and applications, offering guidance for more efficient design and manufacturing.
Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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