Abstract
The inclusion complexes of warfarin with β-cyclodextrin, 2-hydroxypropyl-β-CD and methyl-β-CD have been investigated in aqueous solution. The apparent binding constants of warfarin are found to be 542±19, 442±18 and 112±6M-1 respectively, calculated from the increments in fluorescence emission of the drug. The influence of the β-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 3.6×10-4 min-1 in β-CD, to 5.0×10-4 min-1 in 2-hydroxypropyl-β-CD and to 1.4×10-3 min-1 in methyl-β-CD compared to 3.2×10-3 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.
| Original language | English |
|---|---|
| Pages (from-to) | 23-32 |
| Number of pages | 10 |
| Journal | Journal of Inclusion Phenomena and Molecular Recognition in Chemistry |
| Volume | 20 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Mar 1994 |
Keywords
- β-CD complexes
- β-cyclodextrin
- 2-hydroxypropyl-β-cyclodextrin
- apparent binding constants
- bioavailability of warfarin
- fluorescence spectroscopy
- Inclusion complexation of warfarin with β-CDs
- methyl-β-cyclodextrin
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