de Villiers M M, Liebenberg W, Malan S F, Gerber J J
Research Institute for Industrial Pharmacy, School of Pharmacy, Potchefstroom University for CHE, South Africa.
Drug Dev Ind Pharm. 1999 Aug;25(8):967-72. doi: 10.1081/ddc-100102259.
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.
本研究的目的是改善难溶性非甾体抗炎药布洛芬和酮洛芬的水溶解性能，并探索使用N-甲基葡糖胺（葡甲胺）来增强难溶性药物粉末的溶解性能。差示扫描量热法（DSC）和X射线粉末衍射（XRD）结果的变化表明，布洛芬与N-甲基葡糖胺之间可能形成了复合物。对于等量的酮洛芬和N-甲基葡糖胺混合物，未观察到类似变化。在25℃和37℃水中的溶解度和溶出度研究结果表明，在混合物和共沉淀物中，N-甲基葡糖胺提高了酮洛芬和布洛芬的溶解度、固有溶出度和粉末溶出度。即使DSC和XRD行为未表明形成复合物，N-甲基葡糖胺也显著改善了布洛芬和酮洛芬的溶解度和溶解性能。
