Improvement of Solubility and Dissolution of Rilpivirine Solid Dispersions by Solvent Evaporation Technique and Novel Carriers
DOI:
https://doi.org/10.37285/ijpsn.2018.11.4.5Abstract
Rilpivirine benzonitrile is a pharmaceutical drug used for the treatment of HIV infection it is characterized with poor solubility that limits its absorption and dissolution rate, which delays onset of action. In the present study, immediate release solid dispersion of antiretroviral Rilpivirine was formulated by solvent evaporation technique. Eighteen solid dispersions were prepared with 1:1:1, 1:2:1 and 1:3:1 ratios of drug: carrier: surfactant. There was significant improvement in the rate of drug release from all 18 solid dispersions and the formulation (SE12) comprising Rilpivirine: Kolliwax GMS II: SLS in 1:3:1 by solvent evaporation process has shown enhanced solubility about 30 folds and significant improvement in the rate of drug release. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Rilpivirine has been converted into an amorphous form from crystalline within the solid dispersion formulation. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of Rilpivirine.
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Keywords:
Rilpivirine, Solid dispersion, Solvent evaporation method, solubility, Kolliwax GMS II
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