The dissolution and complexing properties of ibuprofen and ketoprofen when mixed with N-methylglucamine.
The objectives of this study were to improve the aqueous dissolution properties of the poorly soluble nonsteroidal anti-inflammatory drugs ibuprofen and ketoprofen and to explore the use of N-methylglucamine (meglumine) to enhance the dissolution properties of poorly water-soluble drug powders. Changes in both differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) results indicate that possibly complexes were produced between ibuprofen and N-methylglucamine. Similar changes were not observed for equivalent ketoprofen and N-methylglucamine mixtures. The results of solubility and dissolution studies in water at 25 degrees C and 37 degrees C showed that N-methylglucamine, in mixtures and coprecipitates, increased the solubility, intrinsic dissolution, and powder dissolution of ketoprofen and ibuprofen. N-Methylglucamine significantly improved the solubility and dissolution properties of both ibuprofen and ketoprofen even when DSC and XRD behavior did not indicate the formation of complexes.
de Villiers
M M
MM
Research Institute for Industrial Pharmacy, School of Pharmacy, Potchefstroom University for CHE, South Africa.
Liebenberg
W
W
Malan
S F
SF
Gerber
J J
JJ
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D006358:Hot Temperature; D007052:Ibuprofen / Q000737:chemistry*; D007660:Ketoprofen / Q000737:chemistry*; D008536:Meglumine / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011208:Powders; D014867:Water; D008536:Meglumine; D007660:Ketoprofen; D007052:Ibuprofen