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

被引:24
作者
de Villiers, MM [1 ]
Liebenberg, W
Malan, SF
Gerber, JJ
机构
[1] Potchefstroom Univ Christian Higher Educ, Res Inst Ind Pharm, ZA-2520 Potchefstroom, South Africa
[2] Potchefstroom Univ Christian Higher Educ, Sch Pharm, Dept Pharmaceut Chem, ZA-2520 Potchefstroom, South Africa
[3] Potchefstroom Univ Christian Higher Educ, Sch Pharm, Dept Pharmaceut Practice, ZA-2520 Potchefstroom, South Africa
关键词
D O I
10.1081/DDC-100102259
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The objectives of this study were to improve the aqueous dissolution properties of the pool lv 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 proper ties of both ibuprofen and ketoprofen even when DSC and XRD behavior did not indicate the formation of complexes.
引用
收藏
页码:967 / 972
页数:6
相关论文
共 8 条
[1]   DISSOLUTION RATES OF CORTICOSTEROIDS UTILIZING SUGAR GLASS DISPERSIONS [J].
ALLEN, LV ;
YANCHICK, VA ;
MANESS, DD .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1977, 66 (04) :494-497
[3]  
GHAMEN A, 1980, J PHARM PHARMACOL, V32, P675
[4]  
LOTTER AP, 1983, PHARM TECH, V7, P56
[5]  
*MERCK CO, 1996, MERCK IND
[6]  
Motola S., 1991, US Patent, Patent No. [5028625, 5,028,625]
[7]   MECHANISTIC STUDY OF INFLUENCE OF MICELLE SOLUBILIZATION AND HYDRODYNAMIC FACTORS ON DISSOLUTION RATE OF SOLID DRUGS [J].
SINGH, P ;
DESAI, SJ ;
FLANAGAN, DR ;
SIMONELL.AP ;
HIGUCHI, WI .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1968, 57 (06) :959-&
[8]  
Veronesi P.A., 1988, US Patent, Patent No. [4,748,174, 4748174]