Designanddevelopmentofmeltsolidificationof meloxicam for enhancement of solubility and dissolution

Abstract

The objective of the present study wasto prepare an amorphous system of BCS Class2 drug meloxicam(MLX)to improve its solubility and dissolution byusingthe melt solidification techniques. About 40% of new chemical entities do not reach to market due to its poor aqueous solubility. Melt solidification technique is an important process to control the transition from liquid into solid phase to obtain product in an amorphous form. During the process of heating, some solid gets melted and if quench cooled, instead of crystallizing gets converted to amorphous solid form appearing as that of glass,whichimprovedissolution and bioavailabilityof drugs.Physical mixtures of MLX were prepared by melt solidification technique using polymer(soluplus). The solubility and dissolution studies for the meloxicam and batches were conducted in a phosphate buffer (pH 6.8). The fourier transforminfrared(FTIR)spectrophotometry,X-raydiffractionmicroscopy(XDM) andDifferentialscanning calorimetry(DSC) studies were conducted to evaluated pure drug and optimized batch(MS7). Saturation solubility and % drug release showed the improvesolubility and dissolution, resultssuggest that optimized batch (MS7)containing drug and polymer in proportion of 1:4 (MLX:soluplus) was a successful enhancing the solubility and dissolution of MLX. The % crystallinity of MLXin amorphous sample was 18.60%,which indicates significant decrease in crystallinity of MLXin an amorphous system. The best fit model of optimized batch (MS7) waszero order model, showing the %drug release 96.83% and R20.9904. The present investigation, successfully enhancement solubility and dissolution of MLXbyusingmelt solidification technique.