Evaluation of fenofibrate formulations without sodium lauryl sulfate with enhanced in-vitro dissolution profile.

摘要

Fenofibrate is one of the most widely prescribed anti-hyperlipidemic drugs, which exhibit poor solubility profiles in the gastro-intestinal fluids. Consequently, incomplete and variable bioavailability patterns are documented with the use of this drug.;Fenofibrate is a lipophilic compound with no solubility in water. Having no ionizable group in its molecule, its solubility is not influenced by the change of pH in the dissolution medium. Therefore, most of its formulations include strong anionic surfactants to enhance its in-vitro and in-vivo solubility for absorption.;This study was undertaken to develop the various solid dispersions of compositions using single and multiple carriers to enhance its in-vitro solubility profile. The carriers selected included polyethylene glycol-8000, polyvinylchloride k-30, sodium deoxycholate, sodium cholate and tripalmitin. Solid dispersion formulations were prepared via solvent evaporation method.;Among the formulations evaluated, the sample containing Fenofibrate/PEG-8000/Sodium deoxycholate at the weight ratio of 1:2:1 exhibited desirable dissolution of the drug. After 2 hours, almost 100% of the drug was dissolved, in comparison to 63% dissolution of pure fenofibrate powder or 69% commercial product, fenofibrate 67mg.;Physical characterization studies were performed on the selected formulation using FTIR (Fourier Transform Infra Red), XRD (X-Ray Diffraction) and DSC (Differential Scanning Calorimetric) analyses were conducted. The studies indicated that there are no physicochemical interactions within the formulation ingredients.;This study revealed that solid dispersion formulation with enhanced dissolution rate may optimize the drug solubility in the gastrointestinal fluid, and therefore minimize its bioavailability variations in human.