Abstract

SOLUBILITY ENHANCEMENT OF POORLY SOLUBLE DRUG BY USING COCRYSTAL TECHNIQUE AND ITS PRELIMINARY INVESTIGATIONS

Dr. R. Senthil Prabhu*, Dr. A. Abdul Hasan Sathali and K. S. Shanmugarajesh

ABSTRACT

Ursodeoxycholicacid acid is classified as a BCS class II drug, characterized by low solubility and high permeability, and it is commonly prescribed for cholestatic liver diseases. In order to enhance its pharmaceutical properties, crystal engineering techniques were employed to create innovative cocrystals of ursodeoxycholicacid acid with compounds recognized as safe for consumption (GRAS molecules). One notable instance involved the synthesis of a cocrystal of ursodeoxycholicacid acid and the GRAS molecule Nicotinamide, with a stoichiometric ratio of 1:1. The method employed for the preparation of these cocrystals was solvent evaporation. A comprehensive characterization process was undertaken to validate the integrity and formation of the newly prepared crystalline structures. Techniques such as Powder X-ray diffraction, Differential Scanning Calorimetry, and FT-IR spectroscopy were utilized. Powder X-ray diffraction analysis furnished insights into the intricate hydrogen bonding and interactions between the ursodeoxycholicacid acid and the coformer. Differential Scanning Calorimetry, on the other hand, revealed alterations in thermal behavior, serving as a key indicator of cocrystal formation. Furthermore, the physicochemical attributes of these cocrystals were meticulously evaluated. Solubility and dissolution rate measurements were conducted, revealing that the cocrystals exhibited accelerated dissolution kinetics. Impressively, the equilibrium solubility of these cocrystals surpassed that of the parent drug, signifying a substantial improvement in its aqueous solubility profile.

Keywords: Ursodeoxycholicacid, BCS class II drug, Crystal engineering, Cocrystals, Solvent evaporation, Aqueous solubility enhancement.