The dissolution and complexing properties of ibuprofen and ketoprofen whenmixed with N-methylglucamine

Citation
Mm. De Villiers et al., The dissolution and complexing properties of ibuprofen and ketoprofen whenmixed with N-methylglucamine, DRUG DEV IN, 25(8), 1999, pp. 967-972
Citations number
8
Categorie Soggetti
Pharmacology & Toxicology
Journal title
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
ISSN journal
03639045 → ACNP
Volume
25
Issue
8
Year of publication
1999
Pages
967 - 972
Database
ISI
SICI code
0363-9045(1999)25:8<967:TDACPO>2.0.ZU;2-2
Abstract
The objectives of this study were to improve the aqueous dissolution proper ties of the pool lv soluble nonsteroidal anti-inflammatory drugs ibuprofen and ketoprofen and to explore the use of N-methylglucamine (meglumine) to e nhance the dissolution properties of poorly water-soluble drug powders. Cha nges in both differential scanning calorimetry (DSC) and X-ray powder diffr action (XRD) results indicate that possibly complexes were produced between ibuprofen and N-methylglucamine. Similar changes were not observed for equ ivalent ketoprofen and N-methylglucamine mixtures. The results of solubilit y and dissolution studies in water at 25 degrees C and 37 degrees C showed that N-methylglucamine, in mixtures and coprecipitates, increased the solub ility, intrinsic dissolution, and powder dissolution of ketoprofen and ibup rofen. N-Methylglucamine significantly improved the solubility and dissolut ion proper ties of both ibuprofen and ketoprofen even when DSC and XRD beha vior did not indicate the formation of complexes.