Department of Pharmaceutics, Laboratory of Pharmaceutical Technology, Ghent University, Ghent, Belgium.
Drug Dev Ind Pharm. 2013 May;39(5):791-8. doi: 10.3109/03639045.2012.709251. Epub 2012 Aug 8.
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.
在这里,我们旨在评估 Gelucire 44/14 作为非离子表面活性剂赋形剂,以生产水溶性差的药物的速释固体剂型。Gelucire 是由单、二和三甘油酯以及单和二 PEG 酯组成的聚乙二醇 (PEG) 甘油酯。它们是惰性半固体蜡质两亲性赋形剂,具有表面活性,与水接触时会自发形成精细的分散体或乳液。单一的 Gelucire 44/14 结构容易延长侵蚀时间,从而减缓药物溶解。为了克服这个问题,我们将制粒或喷雾干燥与优化的崩解促进剂组合,然后压制成片剂。这种配方策略可在 10 分钟的溶解时间内实现近 100%的药物释放。