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The Thai Journal of Pharmaceutical Sciences

Article Title

A comprehensive review on pharmaceutical cocrystal - a subtle technique for solubility enhancement

Abstract

Solubility enhancement of active pharmaceutical ingredients is a challenging field in the pharmaceutical industry. Poorly soluble drugs lack oral bioavailability. Several methods and excipients are employed in the solubility improvement process. The physical and chemical properties of the developed compound play a key role in solubility enhancement. Crystal engineering is a novel strategy to alter the physicochemical properties of the molecule without causing significant changes in its structural integrity. Cocrystals are single-phase or homogeneous crystalline structures composed of two or more compounds bound noncovalently with the active pharmaceutical ingredient in a definite stoichiometric ratio. The cocrystallization technique is effective in improving the problems associated with solubility, bioavailability, permeability, stability, hygroscopicity, flowability, and process ability. This review represents the concept, characterization, and application of cocrystal in a systematic way. The review focuses on the requisite and mechanism of cocrystal formation, different preparation methods of cocrystals, and stages of screening. The growing interest in this technique has led the regulatory bodies to implement the guidelines and a brief on regulatory perspectives is discussed here. The cocrystallization method establishes the proof of concept of its potential in the pharmaceutical field through increasing number of patents and market approval.