ABSTRACT
Pharmaceutical cocrystals are still gaining the interest of the researchers due to their potential to alter physicochemical, mechanical, and pharmacokinetic properties of active pharmaceutical ingredients without negotiating therapeutic action. The diverse new applications of cocrystals, like taste masking, reduced toxicity, patenting opportunities, commercial potential, etc. act as driving force to the rising interest of the pharmaceutical industries. Initially, cocrystals from the view of regulatory authorities, design strategies, cocrystal preparation in brief with special emphasis on scalable and solvent-free hot melt extrusion method, and practical guide to characterization have been provided. The special focus has been given to the biopharmaceutical attributes of the cocrystal. Finally, challenges before and after cocrystal preparation are presented in this review along with some commercial examples of the cocrystals.
Subject(s)
Pharmaceutical Preparations , Crystallization , Solvents/chemistryABSTRACT
BACKGROUND: Pharmaceutical cocrystal is an emerging approach to tailor physicochemical and mechanical properties of drug substances. Cocrystals are composed of API and pharmaceutically acceptable coformer. It is used to address the solubility, dissolution, mechanical properties and stability of drugs. METHODS: This review discusses introduction to cocrystal, preparation, and characterization, what USFDA says on cocrystal and role of Hansen solubility parameter to predict cocrystal. The effect of cocrystal on drug properties, dependence of cocrystal solubility on pH, concept of drug-drug cocrystal, and aerosil 200 as novel cocrystal former and impact of cocrystal on drug pharmacokinetic has also been presented in this review along with highly selected examples of cocrystals. Finally, how cocrystal offers an opportunity for patents is also delineated. RESULTS: Pharmaceutical cocrystals have ability to tailor physichochemical and mechanical properties of drug substances. It also provides opportunity for patentable invention. Therapeutic efficacy of drugs may be improved via drug-drug cocrystal. CONCLUSION: The pharmaceutical cocrystals are not fully explored and have potential for future development. Successful drug delivery can be achieved through cocrystallization. Pharmaceutical industry will be beneficial through successful cocrystallization of drug substances.