INCLUSION COMPLEXATION OF WARFARIN WITH BETA-CYCLODEXTRINS AND ITS INFLUENCE ON ABSORPTION KINETICS OF WARFARIN IN RAT

被引：4

作者：

KARADAG, O

GOK, E

ATES, IS

KIRAN, O

BOZKURT, A

机构：

[1] HACETTEPE UNIV,FAC SCI,DEPT CHEM,ANKARA,TURKEY

[2] HACETTEPE UNIV,FAC MED,DEPT PHARMACOL,ANKARA 06100,TURKEY

来源：

JOURNAL OF INCLUSION PHENOMENA AND MOLECULAR RECOGNITION IN CHEMISTRY | 1994年 / 20卷 / 01期

关键词：

INCLUSION COMPLEXATION OF WARFARIN WITH BETA-CDS; APPARENT BINDING CONSTANTS; BIOAVAILABILITY OF WARFARIN; BETA-CD COMPLEXES; FLUORESCENCE SPECTROSCOPY; BETA-CYCLODEXTRIN; 2-HYDROXYPROPYL-BETA-CYCLODEXTRIN; METHYL-BETA-CYCLODEXTRIN;

D O I：

10.1007/BF00707609

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The inclusion complexes of warfarin with beta-cyclodextrin, 2-hydroxypropyl-beta-CD and methyl-beta-CD have been investigated in aqueous solution. The apparent binding constants of warfarin are found to be 542 +/- 19, 442 +/- 18 and 112 +/- 6 M(-1) respectively, calculated from the increments in fluorescence emission of the drug. The influence of the beta-CDs on the absorption rate of the drug is investigated with in situ experiments in a chronically isolated internal loop, in the small intestine of the rat. The first-order disappearance (absorption) rate constant decreases to 3.6 x 10(-4) min(-1) in beta-CD, to 5.0 x 10(-4) min(-1) in 2-hydroxypropyl-beta-CD and to 1.4 x 10(-3) min(-1) in methyl-beta-CD compared to 3.2 x 10(-3) min(-1) in isotonic phosphate buffer (pH-7.4) solution, all of them showing a good agreement with the percentage of free warfarin in their complexed solutions: 16%, 18% and 47% calculated, respectively.

引用

页码：23 / 32

页数：10

共 18 条

[1] STEREOSPECIFIC HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC ANALYSIS OF WARFARIN IN PLASMA [J].