Preparation and in vitro Evaluation of Apixaban Solid Dispersions by Fusion Method

Poor solubility of drugs (including Apixaban) is one of the major challenges in pharmaceutical formulation, as more than 40% of new drugs are practically poorly or non-water-soluble. For a drug absorption, it must be soluble at the absorption site.

In this study, solid dispersions of Apixaban were prepared by a Fusion Method, by using different excipients such as Glycerol Monostearate (GMS), Stearic Acid (SA), and Poloxamer 188 (PXM188) and 407 (PXM407).

The aim was to improve the solubility of poorly water-soluble Apixaban. Solid dispersion technology is considered as a promising and practical control of drug release.

The physiochemical properties of the resulting formulations were evaluated in terms of production yield, drug content, in-vitro dissolution studies by using USP apparatus I (rotating basket), drug-excipient interactions by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC).

Solid dispersions of Apixaban, prepared by fusion method with different polymers, demonstrated good yield, high drug content, increase in the dissolution rate of Apixaban compared with the pure drug. Moreover, FTIR and DSC analyses indicated minimal interactions between Apixaban and the previous excipients.