THE TERFENADINE BETA-CYCLODEXTRIN INCLUSION COMPLEX

被引:0
|
作者
REDENTI, E
PASINI, M
VENTURA, P
SPISNI, A
VIKMON, M
SZEJTLI, J
机构
[1] UNIV PARMA,IST CHIM BIOL,I-43100 PARMA,ITALY
[2] CYCLODEXTRIN RES & DEV LAB LTD,CYCLOLAB,H-1525 BUDAPEST,HUNGARY
关键词
TERFENADINE; BETA-CYCLODEXTRIN; INCLUSION COMPLEX;
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Terfenadine (TFN) is a very hydrophobic antiallergic drug. It exists in three polymorphic and two solvated forms and is practically insoluble in water. These properties make a pharmaceutical formulation with acceptable biopharmaceutical characteristics difficult to prepare. Inclusion complexation with beta-cyclodextrin (betaCD) may eliminate such problems. The properties of the TFN/betaCD system have been studied in liquid, gaseous and solid phases by H-1 and C-13 NMR spectroscopy, powder X-ray diffractometry, differential scanning calorimetry and fast atom bombardment mass spectrometry. The solubility phase diagram was also recorded. In solution and in the gaseous phase the 1 : 1 complex prevails, whereas a 1 : 2 TFN/betaCD complex has been isolated by precipitation from homogeneous solution.
引用
收藏
页码:281 / 292
页数:12
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