Dissolution from solid lipid extrudates containing release modifiers

被引:13
作者
Gueres, Sinan [1 ]
Kleinebudde, Peter [1 ]
机构
[1] Univ Dusseldorf, Inst Pharmaceut & Biopharmaceut, D-40225 Dusseldorf, Germany
关键词
Solid lipid extrusion; Dissolution; Polyethylene glycol; Pore former; Disintegrants; Hydrocolloids; DRUG-RELEASE; SUSTAINED-RELEASE; FORMULATIONS; DEPOSITION; EXTRUSION; MIXTURES;
D O I
10.1016/j.ijpharm.2011.04.010
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The influence of different types of release modifiers on the dissolution from solid lipid extrudates was investigated. Diprophylline was extruded together with 45% tristearin and 5% (w/w) of a release modifier to suitable extrudates. Three groups of release modifiers were defined: Hydrocolloids, disintegrants and pore formers. All of the release modifier-containing extrudates showed a faster release compared to the reference extrudate, which contained 50% (w/w) of each. API and lipid. Increasing the amount of diprophylline in the binary mixture up to 55% (w/w) also increased its release rate. Compared to this new reference, not all of the release modifier-containing extrudates exhibited an increased dissolution rate. Within the group of pore formers, there was a great discrepancy concerning the dissolution rates. Extrudates containing polyethylene glycol (PEG) exhibited a much higher release rate compared with extrudates containing sodium chloride or mannitol. This behaviour was assumed to be based on the extrusion temperature of 65 degrees C at which PEG exists in the molten state. The hypothesis was tested using different PEGs and another solid lipid. (C) 2011 Elsevier B.V. All rights reserved.
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页码:77 / 84
页数:8
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