Transnasal anticonvulsive pharmaceutical composition

Details Transnasal anticonvulsive pharmaceutical composition Transnasal anticonvulsive pharmaceutical composition

A - Human Necessities

61

K

A61K 9/72 (2006.01) A61K 31/5513 (2006.01) A61K 47/10 (2006.01) A61K 47/14 (2006.01) A61P 21/02 (2006.01)

Patent

CA 2678225

Disclosed herein is a transnasal anticonvulsive pharmaceutical composition comprising diazepam as an active ingredient, water, a fatty acid ester, diethylene glycol monoethyl ether, ethanol and sodium glycocholate, wherein the weight of the fatty acid ester is at least 2-fold higher than that of water and is at least 2-fold higher than that of ethanol. The anticonvulsive pharmaceutical composition for transmucosal delivery of diazepam according to the present invention includes a minimized content of water and ethanol, a fatty acid ester as a main ingredient and no use of a polar solvent, e.g. glycol, and exhibits improved diazepam solubility and transmucosal permeability due to using a small amount of water and ethanol. The present invention also includes treatment of convulsions by transnasally administering to a patient in need thereof a therapeutically effective amount of the disclosed compositions.

L'invention concerne une composition anticonvulsive transnasale comprenant du diazépam comme ingrédient actif, de l'eau, un ester d'acide gras, du monoéthyl éther de diéthylène glycol, de l'éthanol et du glycolate de sodium, le poids de l'ester d'acide gras étant au moins le double de celui de l'eau et étant au moins le double de celui de l'éthanol. La composition pharmaceutique anticonvulsive pour l'administration transmuqueuse de diazépam selon l'invention comprend une teneur minimisée en eau et éthanol, un ester d'acide gras en tant qu'ingrédient principal et est dépourvue de solvant polaire, par exemple de glycol, et présente une solubilité du diazépam améliorée et une perméabilité transmuqueuse améliorée, en raison de l'utilisation d'une petite quantité d'eau et d'éthanol. L'invention concerne en outre le traitement de convulsions par administration transnasale, à un patient en demande, d'une quantité thérapeutiquement efficace des compositions précitées.

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