Abstract

PREPARATION AND CHARACTERIZATION OF IBUPROFEN COCRYSTALS BY USING SOLVENT DROP GRINDING METHOD

Zalte Amar Gangadhar, Darekar Avinash Bhaskar, Gondkar Sheetal Bhaskar, Saudagar Ravindranath Bhanudas

ABSTRACT

Ibuprofen is a non-steroidal anti-inflammatory BCS class II drug of low solubility and high permeability. Pharmaceutical cocrystals of Ibuprofen were prepared with cocrystal formers, such as benzoic acid, 3-aminobenzoic acid, and cinnamic acid, to improve drug solubility.Solvent drop grinding method was successful to make Ibuprofen cocrystals. All new crystalline forms were characterized by IR spectroscopy, differential scanning calorimetry, and X-ray diffraction to confirm their purity and homogeneity. Cocrystals with benzoic acid, 3-aminobenzoic acid and cinnamic acid showed a faster powder dissolution rate than the reference active pharmaceutical ingredient (API). Cocrystals of Ibuprofen with benzoic acid showed the highest solubility (7 times as compared with API) while cocrystals with Ibuprofen and 3-aminobenzoic acid and cinnamic acid showed comparably good solubility (3 times faster than the API) up to 60 min. The study showed cocrystals is an emerging trend to modify physicochemical properties of drug to enhance their pharmaceutical properties.

Keywords: Cocrystals, Cocrystallization, Ibuprofen, Grinding.