Title: Salt formation in solid dispersions consisting of polyacrylic acid as a carrier and three basic model compounds resulting in very high glass transition temperatures and constant dissolution properties upon storage
Authors: Weuts, Ilse ×
Kempen, Dieter
Verreck, Geert
Peeters, J
Brewster, Marcus
Blaton, Norbert
Van den Mooter, Guy #
Issue Date: Jul-2005
Series Title: European Journal of Pharmaceutical Sciences vol:25 issue:4-5 pages:387-393
Abstract: The purpose of the study was to investigate the suitability of polyacrylic acid (PAA) as a carrier in solid dispersions, with the aim to delay crystallization of basic drugs and improve their dissolution behaviour. The physicochemical properties were investigated in order to link the physical state of some model compounds to their dissolution properties. Loperamide and two structurally related substances were selected as model compounds. Solid dispersions were prepared by spray drying. The amount of residual solvents and water was determined with gas chromatography (GCS: S: solvent) and thermogravimetric analysis (TGA). The drug loading of the dispersions was determined using high performance liquid chromatography (HPLC). ADSC (alternating or temperature modulated DSC), XRD and FT-IR-spectroscopy were used to evaluate the physical state and in vitro dissolution tests were performed to measure the dissolution properties. IR-measurements demonstrated the formation of a salt between the COOH-groups of the polymer and the amino-groups of the compounds. This phenomenon results in high T(g)-values of the dispersions, suppression of crystallization of the fragment molecules during preparation and an increase of the dissolution rate. Furthermore, the stability study conducted on the dispersions with loperamide showed that both, the amorphous state of the drug and the dissolution behaviour are stable under the applied storage conditions. Hence, from the experimental results it could be concluded that PAA is a suitable carrier in the formulation of stable solid dispersions for the basic compounds that were investigated.
ISSN: 0928-0987
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Biocrystallography
Drug Delivery and Disposition
× corresponding author
# (joint) last author

Files in This Item:
File Description Status SizeFormat
2005-Weuts-Salt formation in solid dispersions...-EUr J Pharm Sci.pdf Published 136KbAdobe PDFView/Open Request a copy

These files are only available to some KU Leuven Association staff members


All items in Lirias are protected by copyright, with all rights reserved.

© Web of science