Formulation, Characterization, and Optimization of Fast-Dissolve Tablets Containing Celecoxib Solid Dispersion

Abstract

Celecoxib is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of the present investigation was to increase the solubility and dissolution rate of celecoxib by preparing a solid dispersion with polyvinyl pyrrolidone K30 (PVP-K30) using a solvent-evaporation method. The dissolution profiles of developed formulations in distilled water containing 1% SLS were studied. Drug–polymer interactions were investigated using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). For the preparation of celecoxib fast-dissolve tablets, a 1:2 solid dispersion with PVP-K30 was used with croscarmellose sodium as a superdisintegrant and Pearlitol 200SD (pearlitol) as a pore-forming agent. A 3 2 full-factorial design was employed to study the effect of independent variables, the amounts of croscarmellose sodium (X1) and pearlitol (X2), on dependent variables, disintegration time, percentage friability, wettability, and percentage of drug released after 20 min (Q20). The results show that a dispersion of the drug in polymer considerably enhanced the dissolution rate. The drug-to-carrier ratio is the controlling factor for dissolution improvement. FTIR spectra show no chemical incompatibility between the drug and PVP-K30. FTIR and DSC data indicate that celecoxib was in the amorphous form, which explains the faster dissolution rate of the drug from its solid dispersions. Concerning the optimization study, multiple regression analysis reveals that an optimum concentration of croscarmellose sodium and a higher percentage of pearlitol are required for obtaining rapidly disintegrating tablets.