<p>The present work attempts to enhance the solubility of the poorly soluble compound, nebivolol hydrochloride by gelatin and cyclodextrin in different concentrations. Kneading and solvent evaporation techniques were employed for cyclodextrin whereas hot-melt extrusion and grinding were executed for gelatin. Amongst all the solid dispersions prepared, significant improvement of solubility was observed for the mixture of nebivolol hydrochloride and gelatin prepared using the hot-melt extrusion technique. Solubility behavior can be explained by increased wettability driven by entrapment of nebivolol hydrochloride in molten gelatin. Solid dispersions were characterized by solubility measurement, dissolution profile, nebivolol hydrochloride content, FTIR, DSC, and XRD analysis, etc. A promising solid inclusion complex was formulated into a tablet dosage form. A pre-formulation study performed includes but is not limited to a nebivolol hydrochlo-ride-excipient compatibility study, physical characterizations, etc. An optimized tablet dosage form was formulated using a direct compression method. An International Council for Harmonisation -guided stability study was conducted with accelerated and real-time conditions.</p>

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Gelatin-Induced Solubility Enhancement of a Poorly Soluble Drug: Nebivolol Hydrochloride

  • Tauseef Shaikh,
  • S. Sasikumar

摘要

The present work attempts to enhance the solubility of the poorly soluble compound, nebivolol hydrochloride by gelatin and cyclodextrin in different concentrations. Kneading and solvent evaporation techniques were employed for cyclodextrin whereas hot-melt extrusion and grinding were executed for gelatin. Amongst all the solid dispersions prepared, significant improvement of solubility was observed for the mixture of nebivolol hydrochloride and gelatin prepared using the hot-melt extrusion technique. Solubility behavior can be explained by increased wettability driven by entrapment of nebivolol hydrochloride in molten gelatin. Solid dispersions were characterized by solubility measurement, dissolution profile, nebivolol hydrochloride content, FTIR, DSC, and XRD analysis, etc. A promising solid inclusion complex was formulated into a tablet dosage form. A pre-formulation study performed includes but is not limited to a nebivolol hydrochlo-ride-excipient compatibility study, physical characterizations, etc. An optimized tablet dosage form was formulated using a direct compression method. An International Council for Harmonisation -guided stability study was conducted with accelerated and real-time conditions.