Galantamine salts, method of producing it and nasal...

Details Galantamine salts, method of producing it and nasal... Galantamine salts, method of producing it and nasal...

A - Human Necessities

61

K

A61K 9/00 (2006.01) A61K 31/473 (2006.01) A61K 47/42 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2564353

Methods and compositions of the invention employ acethylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer~s disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.

L'invention porte sur des méthodes et sur des compositions qui utilisent des inhibiteurs d'acéthylcholinestérase (ACE) pour prévenir et traiter des maladies et autres troubles du système nerveux central (SNC) tels que la maladie d'Alzheimer. Les inhibiteurs d'ACE sont administrés au système nerveux central de manière ciblée, par exemple par voie intranasale. Les méthodes et les compositions de cette invention génèrent des concentrations thérapeutiques d'inhibiteurs d'ACE dans un tissu ou une partie du SNC sans les désavantages, risques et effets secondaires concomitants de l'administration par voie buccale ou par injection. Les inhibiteurs d'ACE destinés à être utilisés dans cette invention sont la galantamine et divers sels et dérivés de la galantamine. Des sels de carboxylate de la galantamine (tels que le gluconate de galantamine, le lactate de galantamine, le citrate de galantamine et le glucarate de galantamine) présentent une solubilité bien supérieure comparé à d'autres formes de la galantamine telles que l'hydrobromure de galantamine.

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