DESIGNING A FORMULATION SYSTEM TO ENHANCE AQUEOUS SOLUBILITY AND DISSOLUTION OF POORLY SOLUBLE DRUGAbstract
The main purpose of this investigation study is to enhance the solubility and dissolution rate of poorly water-soluble drug Fluconazole. Fluconazole was selected as the choice of drug as it belongs to BCS class II i.e., drugs having low solubility and high permeability, which hinders in-vivo efficacy of drugs giving poor pharmacokinetic profile and low absorption. Solid dispersions are formed to increase the dissolution rate of a drug and solubility, thereby improving its oral bioavailability. Fluconazole solid dispersions were prepared to enhance the solubility and dissolution rate using the Kneading method and Solvent Evaporation method. Solid dispersions were formulated using different carriers like PEG, PVP, Gelucire, etc. The batch containing PEG 4000 as a carrier by using the Solvent Evaporation method gave maximum drug content, and solubility was selected as the optimized batch for the formulation of an oral tablet. The optimized batch was subjected for Practical yield, Drug content, Saturation solubility, Infrared (I.R.) Spectroscopy, Differential Scanning Calorimetry (DSC), X-ray powder Diffractometry, and Scanning electron microscopy. Post and pre-compression parameters were also studied. FT-IR revealed no chemical incompatibility between drug and polymer. The dissolution rate study for the tablet containing Fluconazole solid dispersion was carried out for improvement of the dissolution rate. The formulation SE-Z1 showed maximum solubility and also an increase in dissolution rate as compared to the plain drug. The tablets of fluconazole solid dispersions were successfully prepared, and the formulation was found to be stable.
Z. Nasikkar * and N. Khutle
Department of Pharmaceutics, Dr. L. H. Hiranandani College of Pharmacy, Ulhasnagar, Maharashtra, India.
19 August 2019
23 April 2020
26 July 2020
01 August 2020