A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/4045 (2006.01) A61K 45/00 (2006.01)
Patent
CA 2535803
The present invention provides novel compositions for the delivery of a 5- hydroxytryptamine (5-HT) agonist across the oral mucosa. In particular, the buffer system in the compositions of the present invention raises the pH of saliva to a pH greater than about 9.9, thereby facilitating the substantially complete conversion of the 5-HT agonist from its ionized to its un-ionized form. As a result, the dose of 5-HT agonist is rapidly and efficiently absorbed by the oral mucosa. Furthermore, delivery of the 5-HT agonist across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating migraines are also provided.
L'invention concerne de nouvelles compositions permettant d'administrer un agoniste de la 5-hydroxytryptamine (5-HT) à travers la muqueuse orale. D'une manière plus spécifique, le système tampon des compositions selon l'invention augmente le pH de la salive à un taux supérieur à environ 9,9, ce qui facilite la conversion sensiblement complète de l'agoniste de la 5-HT de sa forme ionisée à sa forme non ionisée. En conséquence, la dose d'agoniste de la 5-HT est rapidement et efficacement absorbée par la muqueuse orale. De plus, l'administration de l'agoniste de la 5-HT à travers la muqueuse orale présente l'avantage de contourner le métabolisme de premier passage hépatique du médicament et d'éviter la dégradation enzymatique du médicament dans le tractus gastro-intestinal. L'invention concerne également des méthodes permettant d'utiliser les compositions selon l'invention dans le traitement des migraines.
Sim & Mcburney
Transoral Pharmaceuticals Inc.
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