Evaluation of Selected Surface Active Agents in the Dissolution of Griseofulvin Granules Prepared by Hot Melt Granulation

Abstract

Introduction Poor aqueous solubility presents a major formulation challenge for many active pharmaceutical ingredients. The use of surface-active agents is a common strategy to address poor drug solubility. Griseofulvin has previously been studied as a model of poorly soluble drugs, shown to posses improved solubility in the presence of surfactants. This study seeks to evaluate the effect of selected surface-active agents on the dissolution of griseofulvin granules prepared by melt granulation. Methodology Griseofulvin granules were prepared by melt granulation technology. The molten binder mimicked the granulating liquid and no additional liquid added. Polyethylene glycol 4000 was incorporated as the melt binder. The surfactants studied were Gelatin, Tween 80 and Sodium lauryl sulphate (SLS), at concentrations of 0.5%, 1% and 2% w/w. Dissolution was performed and sampling done at 5, 10, 20, 30 and 45 min. The griseofulvin released was quantified using Ultraviolet spectrophotometry and its assay in all formulations performed in accordance to the British Pharmacopoeia (2019) specifications. Griseofulvin tablets from Universal Corporation Ltd in the market were subjected to dissolution; sampling was done at 45 minutes. Results and Discussion Formulations containing SLS recorded the highest drug release of 96.7% at a concentration of 2% w/w whereas Tween 80 recorded its highest release of 79.9% at a concentration of 2% w/w. Gelatin formulations recorded the lowest release at all time points. The control formulation that did not have any surfactant had insignificant release at all time points confirming that the surfactants played a critical role in enhancing the dissolution. In all the formulations containing