コンテンツへスキップ
Merck
  • Investigation of drug-polymer interaction in solid dispersions by vapour sorption methods.

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
要旨

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.

材料
製品番号
ブランド
製品内容

Sigma-Aldrich
1-ビニル-2-ピロリジノン, contains sodium hydroxide as inhibitor, ≥99%
Sigma-Aldrich
メタクリル酸メチル, contains ≤30 ppm MEHQ as inhibitor, 99%
Sigma-Aldrich
メタクリル酸2-(ジメチルアミノ)エチル, contains 700-1000 ppm monomethyl ether hydroquinone as inhibitor, 98%
Sigma-Aldrich
L-リシン 一塩酸塩, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
Sigma-Aldrich
ε-カプロラクタム, 99%
Sigma-Aldrich
ブチル・メタクリラート, 99%, contains monomethyl ether hydroquinone as inhibitor
Sigma-Aldrich
L-リシン 一塩酸塩, reagent grade, ≥98% (HPLC)
Supelco
L-リシン 一塩酸塩, Pharmaceutical Secondary Standard; Certified Reference Material
リシン 塩酸塩, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
L-リシン 一塩酸塩, BioUltra, ≥99.5% (AT)
Sigma-Aldrich
メタクリル酸メチル, SAJ first grade, ≥99.0%
Supelco
L-Lysine hydrochloride solution, 100 mM amino acid in 0.1 M HCl, analytical standard
メタクリル酸メチル, European Pharmacopoeia (EP) Reference Standard
Supelco
ε-カプロラクタム, analytical standard
メタクリル酸2-(ジメチルアミノ)エチル, European Pharmacopoeia (EP) Reference Standard
Supelco
L-リシン 一塩酸塩, certified reference material, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland
ブチル・メタクリラート, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
L-リシン 一塩酸塩, SAJ special grade, ≥99.0%