Abstract

CO-CRYSTALLIZATION: A NEW TREND IN ACTIVE PHARMACEUTICAL INGREDIENTS

Sarang R. Masodkar*, Shrikant D. Pande and Sandeep C. Atram

ABSTRACT

Co-crystallization is an effective crystal engineering approach for modifying the crystal structure and properties of drugs. Majority of drugs marketed world-wide is administered by oral route. Nearly 40% of the new molecular entities coming from discovery were never brought to the market because of biopharmaceutical issues like low solubility, low dissolution rate, low permeability and first-pass metabolism. Pharmaceutical co-crystals are nonionic supramolecular complexes and can be used to altered physical property issues such as solubility, stability and bioavailability in pharmaceutical development without affecting chemical composition of API. Co-crystal comprising of API and desired stoichiometric acceptable co-crystal that can be made by various types of interaction like hydrogen bounding, π-stacking and Vander wall forces. Co-crystallization can improve physiochemical properties like solubility, dissolution rate, chemical stability and melting point. Co-crystals are attractive to pharmaceutical scientists because they can significantly diversify the number of crystal forms that exist for a particular active pharmaceutical ingredient (API), and they can lead to improvements in physical properties of clinical relevance. The article gives a brief review on the co-crystallization, their method of synthesis, its importance as an alternative over salt formation, Characterization and applications.

Keywords: Co-crystallization, Selection of Co-former, Method of Co-crystal Formation, Evaluation of Co-crystals.