Enhanced Bioavailability of Digoxin by γ-Cyclodextrin Complexation : Evaluation for Sublingual and Oral Administrations in Humans

Cyclodextrin Drug Carrier Systems

“…117 Other illuminating results were obtained for the sublingual administration of tablets containing complexes of steroids with cyclodextrins. [117][118][119][120][121][122][123] Hydrophilic cyclodextrins including 2-hydroxypropylβ-cyclodextrin and β-cyclodextrin polymer supported the absorption of testosterone from the oral cavity and not from the gastrointestinal tracts; these solubilizers neither enter nor damage the oral tissues. 118 Inherently, the blood level of endogenous testosterone rises a few times a day in episodes lasting approximately 1 h. Such pulsatile release of testosterone can be imitated by the sublingual administration of its 2-hydroxypropyl-β-cyclodextrin complex, giving the desired pharmacological effects.…”

“…A water-soluble complex of digoxin with γ-cyclodextrin can be formulated into a sublingual tablet to enhance bioavailability and to avoid acid hydrolysis of the drug by the gastric juices . Other illuminating results were obtained for the sublingual administration of tablets containing complexes of steroids with cyclodextrins. − Hydrophilic cyclodextrins including 2-hydroxypropyl-β-cyclodextrin and β-cyclodextrin polymer supported the absorption of testosterone from the oral cavity and not from the gastrointestinal tracts; these solubilizers neither enter nor damage the oral tissues .…”

Improvement of Drug Properties by Cyclodextrins

“…55 When tablets containing a γ -CyD complex of digoxin were administered sublingually to human volunteers, the serum levels of drug were signifi cantly increased compared with digoxin alone, owing to the prevention of acid hydrolysis in the stomach. 56 The stoichiometric ratio is in practice responsible for the dosage form design of a drug molecule. In the case of digoxin, for example, one digoxin molecule needs four molecules of γ -CyD to form a 1:4 stable crystalline complex, resulting in an eight-fold increase in the molecular weight of digoxin.…”

Χρήση Μοριακής Δυναμικής Σε Συνδυασμό Με Φασματοσκοπία NMR Για Την Πρόταση Σύνθεσης Βιοδραστικών Μορίων Και Συστημάτων Μεταφοράς Τους

“…Τα σύμπλοκα πολυμερών με HP-β-CD και β-CD χρησιμοποιούνται για την απορρόφηση της τεστοστερόνης από τη στοματική κοιλότητα και όχι από τη γαστρεντερική οδό. Αυτοί οι διαλυτοποιητές δεν προκαλούν καμία βλάβη στους στοματικούς ιστούς[102]. Εγγενώς, το επίπεδο της ενδογενούς τεστοστερόνης στο αίμα αυξάνεται μερικές φορές την ημέρα κατά ώσεις που διαρκούν περίπου μια ώρα.…”