An Overview of Pharmaceutical Co-Crystal

Abstract

Pharmaceutical co-crystals are nonionic supramolecular complexes and supramolecular chemistry. Pharmaceutical co-crystal consists of active pharmaceutical ingredients and coformers. Pharmaceutical co-crystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity. Co-crystals can be constructed through several types of interaction, including hydrogen bonding, pi-stacking, and vander Waals forces. Pharmaceutical co-crystals could play a major role in the future of API formulation. Pharmaceutical co-crystal can be improvement future aspect problems related physicochemical properties of API

Pharmaceutical Cocrystals: An Emerging Approach to Modulate Physicochemical Properties of Active Pharmaceutical Ingredients

“…The melting point of a compound is used to classify it and determine its purity. 19 It is also particularly useful because of its relationships with aqueous solubility and vapour pressure. 30 Many drugs have low melting points, which allows them to exist in a liquid state at ambient temperature.…”

“…14 It was found that the molecules that form cocrystals tend to be similar in terms of their polarity and molecular shape. 19 The Molecular Complementarity tool is especially beneficial when target molecules lack common hydrogen bonding groups. Karki and colleagues used this method to screen coformers for Artemisinin that lacked common hydrogen bonding functionalities.…”

Co-Crystallization of Plant-Derived Antimalarial Drugs: An Alternate Technique for Improved Physicochemical Qualities and Antimalarial Drug Synergy

“…Co-crystals are solid compounds that show promise in drug development, particularly in terms of improving physicochemical properties such as drug solubility. Generally, co-crystals are formed due to the interactions between (1) active pharmaceutical ingredients (APIs) and (2) co-crystals forming agents (normally solid under ambient conditions) [24,25]. Normally, H-bond holds the two components of co-crystals, and this is facilitated by functional groups of APIs, e.g., carboxylic acid functional group.…”

Two Novel Co-Crystals of Naproxen: Comparison of Stability, Solubility and Intermolecular Interaction

“…In recent years, the formation of co-crystals has been an effective method to modulate the properties of active pharmaceutical ingredients (APIs) [ 7 , 8 ]. By selecting appropriate co-crystal formers (CCFs) to form non-covalent interactions, such as hydrogen bonding, van der Waals forces, and π-π stacking, co-crystals have the advantage of improving physicochemical properties while keeping their molecular structure unchanged [ 9 , 10 ]. However, intermolecular interactions and crystal packing are utilized at the supramolecular level to create modifications [ 11 ].…”

“…In this work, S-naproxen was used in this study. The co-crystal screening method was used in this study [ 10 ]; from a supramolecular perspective, naproxen has an effective functional group (carboxyl group) to form intermolecular hydrogen bonds due to the carboxyl group can act as both hydrogen bond acceptors and hydrogen bond donors. Various CCFs with free carboxylic, hydroxyl or amine groups were selected as potential CCFs [ 24 , 25 ], and finally we successfully obtained two co-crystals of NPX with caprolactam (azepan-2-one, CPL) and oxymatrine ((4R,7aS,13aR,13bR)-10-oxododecahydro-1H,5H-dipyrido [2,1-f:3′,2′,1′-ij] [1,6]naphthyridine 4(41H)-oxide, OMT); moreover, CPL belongs to cyclic imide and OMT belongs to quinoxaline alkaloids.…”