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Solid Dispersions of Carvedilol with Porous Silica

Authors :
Franc Vrecer
Odon Planinšek
Borut Kovačič
Source :
Chemical and Pharmaceutical Bulletin. 59:427-433
Publication Year :
2011
Publisher :
Pharmaceutical Society of Japan, 2011.

Abstract

Solid dispersion particles of carvedilol (CAR) were prepared with porous silica (Sylysia 350) by the solvent evaporation method in a vacuum evaporator to ensure an effective pore-filling procedure. Two sets were prepared, each with various amounts of CAR in solid dispersions, and with the pore-filling process differing each time. Set A was prepared by a one-step filling method and set B by a multiple-step pore-filling method of CAR into porous silica. The solid dispersions were then characterized using thermal analysis, X-ray diffraction, and nitrogen adsorption experiments. The results showed that the drug release can be significantly improved compared with the dissolution of the drug in its pure crystalline or amorphous state. Drug release from solid dispersion was faster when the drug content in the solid dispersion was low, which enabled the drug to be finely dispersed along the hydrophilic carrier's surface. The results also showed that a multiple-step pore-filling procedure is more effective for drug loading as indicated by the absence of a crystalline drug state, greatly reduced porosity, and improved wettability and physical stability of the amorphous CAR.

Details

ISSN :
13475223 and 00092363
Volume :
59
Database :
OpenAIRE
Journal :
Chemical and Pharmaceutical Bulletin
Accession number :
edsair.doi.dedup.....42c0c293f199a05d44e2c860ea036349
Full Text :
https://doi.org/10.1248/cpb.59.427