Abstract

PREPARATION AND CHARACTERIZATION OF LORNOXICAM COCRYSTALS

Dasharath M. Patel*, Hardik R. Shah, Rahul J. Patel and Chhagan N. Patel

ABSTRACT

Objective: Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID) of oxicam class. According to BCS, Lornoxicam is classified as a low solubility and high permeability drug (class II). Therefore, it often shows dissolution rate-limited oral absorption and high variability in pharmacological effects. The purpose of this study was to prepare pharmaceutical co-crystals of Lornoxicam to enhance solubility and dissolution rate of Lornoxicam. Experimental Work: Co-crystals were prepared by three different methods: liquid assisted grinding, reaction co-crystallization and cooling crystallization by use of four different co-crystal formers which included saccharin, salicylic acid, tartaric acid and pyrogallol. The prepared co-crystals were evaluated for solubility, powder characterization, assay and in vitro dissolution study. The solid state property was characterized by differential scanning calorimetry (DSC), Fourier transfer infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD). Results and Discussion: The solubility and dissolution rate was significantly increased by preparation of co-crystal. Cocrystal prepared by liquid assisted grinding method using saccharin as co-crystal formers (stoichiometric ratio 1:1) and acetonitrile as a drop solvent gave maximum solubility and dissolution rate. The FTIR, DSC and PXRD studies of co-crystals confirmed the formation of co-crystals. Conclusion: From the study carried out it was concluded that stable co-crystals of Lornoxicam with increased solubility and improved in vitro dissolution of Lornoxicam can be successfully prepared. So, co-crystal is a one of the most promising method to improve the solubility and dissolution of drug having poor solubility.

Keywords: Co-crystals, Lornoxicam, Co-crystal former, Solubility, In vitro dissolution.