PREPARATION AND EVALUATION OF MELOXICAM SOLID DISPERSIONS BY SOLVENT EVAPORATION METHOD

Abstract

Meloxicam (Class ΙΙ drug according to Biopharmaceutical Classification System) is a highly potent non-steroidal anti-inflammatory drug of the enolic acid  class of oxicam derivatives. The low solubility of Meloxicam in water and biological fluids results into its poor bioavailability. The aim of this study is to improve the solubility of Meloxicam, and hence bioavailability, by using solid dispersion technique. Nine physical mixtures of Meloxicam (PMMs) were  prepared in three different proportions of MEL-to-carrier (PEG 4000, PEG 6000, and poloxamer 407). Solid dispersions of MEL (SDMs) were prepared by  solvent evaporation method using the polymers mentioned above. Solubility studies for both PMMs and SDMs were conducted in a phosphate buffer (pH 6.8).  The prepared SDM formulations were subjected for percentage of practical yield and drug content analysis. Fourier Transform Infra-Red (FT-IR) spectrophotometric and Differential Scanning Calorimetric (DSC) studies were also conducted to evaluate both PMMs and SDMs. Among all the prepared  formulas the ratio of 1:5 MEL-to- poloxamer 407 was considered the best, which showed significant enhancement (p < 0.05) of the drug solubility for both  PMM-9 and SDM-9. Good results were also observed concerning the drug content analysis and percent of practical yield for SDM-9. FT-IR studies confirmed the compatibility between MEL and poloxamer 407 for both PMM-9 and SDM-9. Moreover, according to DSC studies, there was a perfect change of MEL crystallinity to the amorphous state. Overall, results suggest that SDM-9 containing poloxamer 407 (Pluronic®F-127) as a carrier in a proportion of 1:5 drug: carrier was a successful resolution for the limited solubility of MEL.