Accéder au contenu
Merck

Investigation of drug-polymer interaction in solid dispersions by vapour sorption methods.

International journal of pharmaceutics (2014-04-23)
Kateřina Punčochová, Jerry Y Y Heng, Josef Beránek, František Stěpánek
RÉSUMÉ

The objective of this study was to investigate the effect of different polymeric carriers in solid dispersions with an active pharmaceutical ingredient (API) on their water vapour sorption equilibria and the influence of the API-polymer interactions on the dissolution rate of the API. X-ray diffraction, scanning electron microscopy (SEM), moisture sorption analysis, infrared (IR) spectroscopy and dissolution tests were performed on various API-polymer systems (Valsartan as API with Soluplus, PVP and Eudragit polymers) after production of amorphous solid dispersions by spray drying. The interactions between the API and polymer molecules caused the water sorption isotherms of solid dispersions to deviate from those of ideal mixtures. The moisture sorption isotherms were lower in comparison with the isotherms of physical mixtures in all combinations with Soluplus and PVP. In contrast, the moisture sorption isotherms of solid dispersions containing Eudragit were significantly higher than the corresponding physical mixtures. The nature of the API-polymer interaction was explained by shifts in the characteristic bands of the IR spectra of the solid dispersions compared to the pure components. A correlation between the dissolution rate and the water sorption properties of the API-polymer systems has been established.

MATÉRIAUX
Référence du produit
Marque
Description du produit

Sigma-Aldrich
1-Vinyl-2-pyrrolidinone, contains sodium hydroxide as inhibitor, ≥99%
Sigma-Aldrich
Méthacrylate de méthyle, contains ≤30 ppm MEHQ as inhibitor, 99%
Sigma-Aldrich
2-(Dimethylamino)ethyl methacrylate, contains 700-1000 ppm monomethyl ether hydroquinone as inhibitor, 98%
Sigma-Aldrich
L-Lysine monohydrochloride, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
Sigma-Aldrich
ε-Caprolactam, 99%
Sigma-Aldrich
Butyl methacrylate, 99%, contains monomethyl ether hydroquinone as inhibitor
Sigma-Aldrich
Méthacrylate de méthyle, 99%, stabilized
Sigma-Aldrich
L-Lysine monohydrochloride, reagent grade, ≥98% (HPLC)
Supelco
L-Lysine monohydrochloride, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
L-Lysine monohydrochloride, BioUltra, ≥99.5% (AT)
Lysine hydrochloride, European Pharmacopoeia (EP) Reference Standard
Méthacrylate de méthyle, European Pharmacopoeia (EP) Reference Standard
Supelco
ε-Caprolactam, analytical standard
Supelco
L-Lysine monohydrochloride, certified reference material, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland
Supelco
L-Lysine hydrochloride solution, 100 mM amino acid in 0.1 M HCl, analytical standard
2-(Dimethylamino)ethyl methacrylate, European Pharmacopoeia (EP) Reference Standard
Butyl methacrylate, European Pharmacopoeia (EP) Reference Standard