SOLUBILITY ENHANCEMENT OF RIVAROXABAN BY SOLID DISPERSION WITH POLYETHYLENE GLYCOL 4000

RUCHITA KUMARI PATRA; AJIT KUMAR ACHARYA; ANJAN KUMAR MAHAPATRA; PADALA NARASIMHA MURTHY

doi:10.22159/ijap.2023v15i2.46687

Authors

RUCHITA KUMARI PATRA Royal College of Pharmacy and Health Sciences, Berhampur-2, Odisha
AJIT KUMAR ACHARYA Royal College of Pharmacy and Health Sciences, Berhampur-2, Odisha
ANJAN KUMAR MAHAPATRA Royal College of Pharmacy and Health Sciences, Berhampur-2, Odisha
PADALA NARASIMHA MURTHY Royal College of Pharmacy and Health Sciences, Berhampur-2, Odisha https://orcid.org/0000-0001-9649-7848

DOI:

https://doi.org/10.22159/ijap.2023v15i2.46687

Keywords:

Solid dispersions, Dissolution rate, PEG 4000, Hydrophilic carriers, Physicochemical characterization

Abstract

Objective: The aim of the work was to enhance the dissolution rate of rivaroxaban by preparing its solid dispersions (SDs) using hydrophilic carrier PEG 4000.

Methods: The SDs of rivaroxaban with PEG 4000 were prepared at 1:1, 1:2 and 1:3 w/w ratios by physical mixing, melting and solvent evaporation techniques. The prepared solid dispersions were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC).

Results: Both the solubility and dissolution rate of the drug in these formulations were increased. The used hydrophilic carriers showed a more than two-fold increase in dissolution rate in their prepared solid dispersions by melting or solvent evaporation techniques. The pure drug rivaroxaban as the pure drug shows a dissolution rate of nearly 39 % after 60 m, whereas the solid dispersions by melting or solvent evaporation showed 90% of dissolution after 60 m. The FTIR spectroscopic and DCS thermal studies showed the compatibility of rivaroxaban and the absence of well-defined drug polymer interactions, though the shift in peaks was observed due to the formation of new bonds.

Conclusion: Formulation of solid dispersions of drug with hydrophilic carriers is a successful approach for solubility or dissolution rate enhancement of low soluble drug(s). In this work for solubility enhancement of rivaroxaban the hydrophilic carrier PEG 4000 showed significant solubility enhancement.

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