Delivery system for localized administration of medicaments...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/445 (2006.01) A61K 9/00 (2006.01) A61K 31/045 (2006.01) A61K 31/4453 (2006.01) A61K 45/00 (2006.01) A61K 47/36 (2006.01) A61K 9/20 (2006.01)

Patent

CA 2238937

The present invention pertains to delivery systems for the localized administration of a medicament to the upper respiratory tract. The delivery system comprises: (a) a safe and effective amount of a medicament useful for treating the upper respiratory tract; (b) an ionic polysaccharide; and (c) a cross-linking agent. The present invention provides for the controlled, in situ formation of a thin, bioadhesive film which may bind to the buccal epithelial cells which form the surface of said upper respiratory tract. Said film formation occurs when the delivery system of the present invention comprising a medicament, an ionic polysaccharide and a cross-linking agent, in a pharmaceutically acceptable carrier, is slowly ingested by dissolution through salivation of the pharmaceutically acceptable carrier. By a series of cross-linking reactions, the cross-linking agent polymerizes the ionic polysaccharide to a film in the form of aggregates, which bind to the buccal epithelial cells in the upper respiratory tract. During the in situ cross-linking reaction, the medicament becomes entrapped in the bioadhesive polymer aggregate and thereafter is gradually released, i.e., becomes available through dissolution.

La présente invention se rapporte à un système d'administration localisée d'un médicament destiné aux voies respiratoires supérieures. Ledit système comporte (a) une quantité sure et efficace d'un médicament utile au traitement des voies respiratoires supérieures, (b) un polysaccharide ionique et (c) un agent de réticulation. La présente invention permet la formation régulée in situ d'un film fin bioadhésif qui peut se lier aux cellules épithéliales buccales formant la surface desdites voies respiratoires supérieures. La formation dudit film se produit lorsque le système d'administration incorporant un médicament, un polysaccharide ionique et un agent de réticulation à l'intérieur d'un excipient pharmaceutiquement acceptable, est ingéré lentement par dissolution obtenue par salivation de l'excipient pharmaceutiquement acceptable. Par une série de réactions de réticulation, l'agent de réticulation polymérise le polysaccharide ionique en un film, constitué d'agrégats, qui se lie aux cellules épithéliales buccales desdites voies respiratoires supérieures. Au cours de la réaction de réticulation in situ, le médicament est piégé au sein de l'agrégat polymère bioadhésif et est par la suite progressivement libéré, c'est-à-dire qu'il devient disponible de par la dissolution.

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