Effect of Tablet Structure on Controlled Release from Supersaturating Solid Dispersions Containing Glyceryl Behenate

The objective of this study was to evaluate the use of glyceryl behenate as a plasticizer and release modifier in solid dispersion systems containing itraconazole and carbamazepine. Amorphous solid dispersions of high molecular weight polyvinylpyrrolidone were prepared by hot-melt extrusion, the pro...

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Bibliographic Details
Published in:Molecular pharmaceutics 2015-01, Vol.12 (1), p.120-126
Main Authors: Keen, Justin M, Hughey, Justin R, Bennett, Ryan C, Jannin, Vincent, Rosiaux, Yvonne, Marchaud, Delphine, McGinity, James W
Format: Article
Language:English
Subjects:
Carbamazepine - chemistry
Chromatography, High Pressure Liquid
Delayed-Action Preparations
Drug Delivery Systems
Fatty Acids - chemistry
Hot Temperature
Itraconazole - chemistry
Kinetics
Lipids - chemistry
Molecular Weight
Plasticizers
Povidone - chemistry
Powders
Tablets - chemistry
X-Ray Diffraction
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Summary:The objective of this study was to evaluate the use of glyceryl behenate as a plasticizer and release modifier in solid dispersion systems containing itraconazole and carbamazepine. Amorphous solid dispersions of high molecular weight polyvinylpyrrolidone were prepared by hot-melt extrusion, the processing of which was improved by the inclusion of glyceryl behenate. Dispersions were milled and subsequently compressed into tablets. Solid dispersions were also prepared by KinetiSol Dispersing, which allowed for the manufacture of monolithic tablets of the same composition and shape as compressed tablets. Tablets without glyceryl behenate and all compressed tablets were observed to have an incomplete release profile likely due to drug crystallization within the tablet as this occurred at conditions in which dissolution concentrations were below saturation. Monolithic tablets formulated to be more hydrophobic, by including glyceryl behenate, allowed for sustained release below and above saturation conditions.
ISSN:1543-8384
1543-8392
DOI:10.1021/mp500480y