Gelucire 44/14 based immediate release formulations for poorly water-soluble drugs

Abstract

Here, we aim to evaluate Gelucire 44/14 as non-ionic surface-active excipient to produce immediate-release solid dosage forms for poorly water-soluble drugs. Gelucires are polyethylene glycol (PEG) glycerides composed of mono-, di- and triglycerides and mono- and diesters of PEG. They are inert semi-solid waxy amphiphilic excipients with surface-active properties that spontaneously form a fine dispersion or emulsion upon contact with water. Monolithic Gelucire 44/14 structures are prone to prolonged erosion times, thereby slowing down drug dissolution. To overcome this issue, we combine either granulation or spray-drying, followed by compression into tablets, with an optimized composition of disintegration promoting agents. This formulation strategy allows obtaining nearly 100% drug release within 10 min dissolution time.