Orally administrable acid stable anti-ulcer benzimidazole...

C - Chemistry – Metallurgy – 08 – F

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C08F 126/06 (2006.01) A61K 31/4184 (2006.01) A61K 31/787 (2006.01) A61P 1/04 (2006.01) C07D 235/04 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2400953

Orally administrable acid stable anti-ulcer benzimidazole derivatives which are polymer based. The process of preparation comprises condensing a benzimidazole with a biocompatible partially orally biodegradable synthetic cross linked polymer in aqueous medium at 5-80 ~C and pH 4-11 under inert atmosphere. The weight percentage of benzimidazole with respect to the polymeric benzimidazole is 1-50. The reaction mixture is cooled and the product is isolated and dried at 25-45 ~C. There is also provided a formulation of the polymeric benzimidazoles in combination with pharmaceutically acceptable excipients.

L'invention concerne des dérivés de benzimidazole antiulcéreux à acidité stable administrables oralement qui sont à base polymère. Le procédé de préparation consiste à condenser un benzimidazole avec un polymère réticulé, partiellement biodégradable oralement, biocompatible dans un milieu aqueux à une température de 5-80 ·C et un pH de 4-11 sous une atmosphère inerte. Le pourcentage en poids du benzimidazole par rapport au benzimidazole polymère est de 1-50. Le mélange de réaction est refroidi et le produit est isolé et séché à 25-45 ·C. L'invention concerne également une formulation des benzimidazoles polymères en combinaison avec des excipients pharmaceutiquement acceptables.

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