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Improvement of the oral bioavailability of digitalis glycosides by cyclodextrin complexation.

Authors
  • Uekama, K
  • Fujinaga, T
  • Hirayama, F
  • Otagiri, M
  • Yamasaki, M
  • Seo, H
  • Hashimoto, T
  • Tsuruoka, M
Type
Published Article
Journal
Journal of pharmaceutical sciences
Publication Date
Nov 01, 1983
Volume
72
Issue
11
Pages
1338–1341
Identifiers
PMID: 6644599
Source
Medline
License
Unknown

Abstract

Inclusion complexes of the digitalis glycosides digitoxin, digoxin, and methyl digoxin with three cyclodextrins (alpha-, beta-, gamma-homologues) in water and in the solid state were studied by a solubility method, IR and 1H-NMR spectroscopy, and X-ray diffractometry. Solid complexes (in a molar ratio of 1:4) of the digitalis glycosides with gamma-cyclodextrin were prepared and their in vivo absorption examined. The rapidly dissolving form of the gamma-cyclodextrin complex significantly increased plasma levels of digoxin (approximately 5.4-fold) after oral administration to dogs.

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