Sucrose esters with various hydrophilic-lipophilic properties: novel controlled release agents for oral drug delivery matrix tablets prepared by direct compaction

Acta Biomaterialia
K Chansanroj, G Betz

Abstract

Sucrose esters (SE) are esters of sucrose and fatty acids with various hydrophilic-lipophilic properties which have attracted interest from being used in pharmaceutical applications. This study aimed to gain insight into the use of SE as controlled release agents for direct compacted matrix tablets. The study focused on the effect of hydrophilic-lipophilic properties on tableting properties and drug release. Sucrose stearate with hydrophilic-lipophilic balance (HLB) values ranging from 0 to 16 was systematically tested. Tablet formulations contained SE, metoprolol tartrate as a highly soluble model drug and dibasic calcium phosphate dihydrate as a tablet formulation filler in the ratio 1:1:2. The compaction behaviour of matrix tablets was compared with the compacts of individual starting materials as reference. SE incorporation improved the plasticity, compressibility and lubricating property of powder mixtures. The hydrophilic-lipophilic properties of SE affected tableting properties, drug release rate and release mechanism. Increasing hydrophilicity corresponding to the increased monoesters in SE composition increased the relative porosity, elastic recovery and tensile strength of the tablets due to the increased hydrogen bon...Continue Reading

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Citations

May 10, 2011·Pharmaceutical Research·Phuong Ha-Lien TranBeom-Jin Lee
Nov 5, 2013·Trends in Pharmacological Sciences·Eduardo J GudiñaLígia R Rodrigues
Jul 22, 2014·Journal of Pharmaceutical Sciences·Lóránd KissMária A Deli
May 12, 2012·International Journal of Pharmaceutics·Angéla Szűts, Piroska Szabó-Révész
Sep 1, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Krisanin ChansanrojGabriele Betz
Apr 19, 2011·Journal of Controlled Release : Official Journal of the Controlled Release Society·Cristina MaderueloJosé M Lanao
Jul 28, 2015·Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment·Tatiana Cucu, Bruno De Meulenaer
Mar 24, 2015·Journal of Agricultural and Food Chemistry·Claudia BernalLorena Wilson
Jun 21, 2016·Advanced Drug Delivery Reviews·Sam MaherDavid J Brayden
May 2, 2017·Chemical & Pharmaceutical Bulletin·Shohei NakamuraHiroshi Yuasa
Mar 20, 2015·Pharmaceutical Research·Karin BeckerAndreas Zimmer

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