Biopharmaceutical Studies on Solid Dispersions of Nalidixic Acid in Modified Starches

Chowdary, K. P. R.; Rao, P. Venkateswara

doi:10.3109/03639049409041965

Cited by 6 publications

(1 citation statement)

References 9 publications

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“…23) Hence, the faster dissolution of KET-NIC solid dispersions is ascribed to the solubilizing effect of the carrier (nicotinamide). In addition, other factors, such as particle size reduction, absence of aggregation and agglomeration between hydrophobic drug particles, good wettablity, and dispersibility of the dispersed drug 24) might have also contributed to the observed increase in the solubility of KET from SDs.…”

Section: Discussionmentioning

confidence: 99%

Physicochemical Characterization and Dissolution Study of Solid Dispersions of Ketoconazole with Nicotinamide

Aggarwal¹,

Jain²

2011

Chem. Pharm. Bull.

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Purpose: The aim of the present study was to improve the solubility and dissolution rate of a poorly watersoluble drug ketoconazole using solid dispersion technique. Methods: Solid dispersions of ketoconazole were prepared in ratios of 90 : 10, 70 : 30, 50 : 50, 30 : 70 and 10 : 90 by the melting method using nicotinamide as carrier. These solid dispersions were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and Fourier transform infrared (FT-IR) spectroscopy to ascertain if there were any physicochemical interactions between drug and carrier that could affect dissolution. Solubility and dissolution studies were conducted with pure ketoconazole, physical mixtures and solid dispersions. Results: Solubility studies indicated that nicotinamide increased significantly the solubility of ketoconazole in water. The Gibbs free energy (D DG°t r ) values were negative indicating the spontaneous nature of ketoconazole solubilization, and it decreased with increase in concentration of the carrier, demonstrating that the reaction became more favorable as the concentration of the carrier increased. The cumulative release of ketoconazole within 120 min from solid dispersion at a drug-tonicotinamide ratio of 10 : 90 (w/w) was 6 times higher than the pure drug in phosphate buffer of pH 6.8. Conclusion: Solid state characterization indicated that there is no interaction between ketoconazole and nicotinamide in the solid state. In contrast to the very slow dissolution rate of pure ketoconazole, the dispersion of the drug in nicotinamide considerably enhanced the dissolution rate. The drug dissolution rate was highest at a drug-tonicotinamide ratio of 10 : 90 (w/w).

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Section: Discussionmentioning

confidence: 99%