Abstract
Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.
Highlights
The solubility/dissolution behavior of a drug is the key factor influencing its oral bioavailability, being the rate-limiting step for absorption of drugs from the gastrointestinal tract
The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers Polyethylene glycol (PEG) 6000 and PVP K30
The results revealed that the percentage yield was high in 1:4 ratio solid dispersion prepared by solvent evaporation method than compared to the fusion method
Summary
The solubility/dissolution behavior of a drug is the key factor influencing its oral bioavailability, being the rate-limiting step for absorption of drugs from the gastrointestinal tract. Dissolution and solubility are two important parameters which alter oral bioavailability of any drug; efforts should be done to improve the solubility and dissolution rate is essential. Characteristics of the drugs can be altered by converting them into salt forms, size reduction, and by adding surfactants [3]. Based on the solubility of the drug and its gastrointestinal permeability, they become the fundamental parameters for rate controlling and extent of drug absorption inside the body. The Biopharmaceutics Classification System correlates the in vitro drug dissolution and in vivo bioavailability
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