Formulation and evaluation of rivaroxaban solid dispersion for improved oral drug delivery
Keywords:
Rivaroxaban, Solid dispersion, Soluplus, Polyvinylpyrrolidone (PVP), Solubility enhancement, Direct compression, Superdisintegrants, DissolutionAbstract
Rivaroxaban is an oral direct factor Xa inhibitor used in the prevention and treatment of Deep Vein Thrombosis (DVT). Its poor aqueous solubility can limit dissolution and oral drug delivery. The present study aimed to enhance the solubility and dissolution of rivaroxaban by preparing solid dispersions using Soluplus and polyvinylpyrrolidone (PVP), followed by development of tablets containing the selected solid dispersion. Four solid-dispersion formulations (SD1–SD4) containing rivaroxaban with different concentrations of Soluplus and PVP were prepared by a solvent evaporation method using ethanol. The prepared dispersions were evaluated for solubility, and SD4 containing 15 mg rivaroxaban, 30 mg Soluplus and 30 mg PVP showed the highest drug solubility, with 3.342 mg dissolved in 20 mL and approximately 17-fold enhancement compared with the pure drug (0.192 mg/20 ml). SD4 was selected for tablet formulation. Four tablet formulations (F1–F4) were prepared by direct compression using crospovidone, croscarmellose sodium and sodium starch glycolate as superdisintegrants. The granule blends showed acceptable flow characteristics. All tablet formulations complied with the reported weight-variation and friability requirements and disintegrated within 30 min. At 60 min, the in-vitro drug release was 89.13%, 92.50%, 84.16% and 98.13% for F1, F2, F3 and F4, respectively. F4 showed the highest drug release. The findings indicate that solid dispersion using Soluplus and PVP improved rivaroxaban solubility, while incorporation of superdisintegrants supported rapid drug release from the tablet formulation.
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