ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF NEBIVOLOL BY SOLID DISPERSION TECHNIQUE
Keywords:Nebivolol, Solid dispersion, Fusion method, Solvent evaporation method
Objective: Solubility is greater challenges for formulation which can be explain by different technological approaches during the pharmaceutical product development and to improve water solubility and drug release respectively.
Methods: The solid dispersions of nebivolol were prepared in ratio 1:1, 1:3, 1:5 and 1:7 by fusion and solvent evaporation method using PEG 6000 and PVP K30 as carriers to enhance solubility of compound.
Results: All the solid dispersions were evaluated for drug content, phase solubility, in vitro dissolution study. Deferential Scanning Calorimetric (DSC) and Fourier Transformer Infra Red (FTIR) showed no chemical interaction between the drug and its carriers. Solubility of PEG 6000 and PVP K30 indicates a linear relationship (AL type of curve) in the investigated polymer concentration range. The Gibb's free energy showed declined trend with increase in the carrier concentrations. The uniformly of drug content was found in all solid dispersions. The drug release obtained from different drug-carrier concentration level fitted to different kinetic model and it was found that solid dispersions exhibited fickian diffusional characteristics and best fitted to higuchi model. A PVP K30 solid dispersion (1:7 ratio) prepared by solvent evaporation method showed faster dissolution rate (94.38 %) in 30 min among studied solid dispersions..
Conclusion: The overall results showed that process of nebivolol transfer from water to carrier solution is more favorable at higher level of PVP K30. The solid dispersion of drug: PVP K 30 (1:7 ratio) prepared by solvent evaporation method was found to be optimum in term of solubility and dissolution rate. Hence, we can concluded that solubility of nebivolol can be enhanced using this carrier ratio.
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