Détail de la notice
Titre du Document
Solubility of (±)-ibuprofen and S (+)-ibuprofen in the presence of cosolvents and cyclodextrins
Auteur(s)
NERURKAR Jayanti ; BEACH J. W. ; PARK M. O. ; ...
Résumé
Aqueous solubility .is an important parameter for the development of liquid formulations and in the determination of bioavailability of oral dosage forms. Ibuprofen (IB), a nonste-roidal anti-inflammatory drug. is a chiral molecule and is currently used clinically as a racemate (racIB). However, the S form of ibuprofen or S(+)-ibuprofen (SIB) is the biologically active isomer and is primarily responsible for the anti-inflammatory activity. Phase solubility studies were carried out to compare the saturation solubilities of racIB and SIB in the presence of common pharmaceutical solvents such as glycerol, sorbitol solution, propylene glycol (PG), and polyethylene glycol (PEG 300) over the range of 20% to 80% v/v in aqueous based systems. The solubilities of the two compounds were also compared in the presence of cyclodextrins such as beta cyclodextrin (CD), hydroxypropyl beta cyclodextrin (HPCD), and beta cyclodextrin sulfobutyl ether sodium salt (CDSB) over the range of 5% to 25% w/v. Solubility determinations were carried at 25°C and 37°C. Cosolvents exponentially increased the solubility of both SIB and racIB, especially in the presence of PG and PEG 300. Glycerol was not very effective in increasing the aqueous solubilities of both compounds, whereas sorbitol solution had a minimal effect on their solubility. PG and PEG 300 increased the solubility of SIB by 400-fold and 1500-fold, respectively, whereas the rise in solubility for racIB was 193-fold and 700-fold, respective
Editeur
Informa Healthcare
Identifiant
PMID : 16176022 ISSN : 1083-7450
Source
Pharmaceutical development and technology A. 2005, vol. 10, n° 3, pp. 413-421 [9 pages] [bibl. : 23 ref.]
Langue
Anglais
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