International Journal of Pharmaceutics 2011-01-01

Dissolution from solid lipid extrudates containing release modifiers

Sinan Güres, Peter Kleinebudde, Sinan Güres, Peter Kleinebudde

Index: Int. J. Pharm. 412(1-2) , 77-84, (2011)

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Abstract

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°C at which PEG exists in the molten state. The hypothesis was tested using different PEGs and another solid lipid.Copyright © 2011 Elsevier B.V. All rights reserved.