Solubility study of meloxicam in pure solvent systems

DAVÍN, VIRGINIA; FILIPPA, MAURICIO; GASULL, ESTELA; PERALTA, CECILIA

Rosario

Congreso; IV Reunión Internacional de Ciencias Farmacéuticas; 2016

Meloxicam (4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide) is a nonsteroidal antiinflammatory drug (NSAID), having very low water solubility [1]. It is further known that the solubility behavior of drugs is useful to establish the physicochemical parameters that have a more significant contribution to the process of solubilization. The experimental solubility of Meloxicam at 298 K in 15 solvents with different characteristics was determined. Data were adjusted using a multiple linear regression analysis (MLRA) of variables linearly related to free energy (LSER), to obtain a multiparameter equation describing the solubilization process: where XYZ0 is a constant that depends on solute, energyfc is the energy for the formation of the cavity where solute is located and energyint sto-ste is the sum of all forms of interaction of the solute with the solvent. The term energyfc is related to solvent: H is the Hildebrand?s solubility parameter, that represents the self-cohesiveness of the solvent, and the sum includes all modes of solute-solvent interaction: the donation (α) and acceptance (β) of hydrogen bonds and the polarizability (π) of solvents [2]. The statistical analysis was performed with IBM SPSS Statistics v 19 program. We have obtained the relation: r = 0,775 σ = 0,041As can be seen, the dissolution process is hampered significantly by the intrinsic properties of Meloxicam. The positive values of β and H indicate that solubility increases with increase in the value of these parameter, while α and  have a negative effect.This study provides valuable information on what are the factors that influence the solubility of an active pharmaceutical, which would improve the solubilization of drug in the transport process.[1] M. Farid, D.A. El-Setouhy, M.A. El-Nabarawi, T. El-Bayomi. J. Drug Deliv. Sci. Tec. 24, (2014), 645-652.[2] M.J Kamlet, J.L.M. Abboud, M.H. Abraham, R.W Taft. J. Org. Chem. 48, (1983), 2877-2887.