Pharmaceutical Cocrystals of Pain Relieving Drugs

Abstract

Cocrystallisation of two components into one crystal form can enhance the solid-state properties of drug compounds. Cocrystals are considered as the next generation modified-active pharmaceutical ingredients with improved physical-chemical, (aqueous solubility, dissolution, hygroscopicity, bioavailability, stability, increase of melting point, purity of an active pharmaceutical ingredients (API), intellectual property positions) and pharmacokinetic properties. Cocrystal formation may overcome dissolution problems of highly lipophilic APIs because the new crystalline lattice being formed often has very different dissolution properties compared to those of the crystals of the API alone. In this review article, pharmaceutical cocrystals of pain relieving drugs (NSAIDs, acetaminophen and opioids) are reported. The co-crystallization of active pharmaceutical ingredients (APIs) with non-toxic co-formers or other API as conformer has been shown to increase the solubility, stability, bioavailability of APIs, and improved tablet ability.

 Keywords: Pharmaceutical cocrystal, coformer, active pharmaceutical ingredient (API), drug, NSAIDs