Medicine based on anti-hyperglycaemic microcapsules with...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/50 (2006.01) A61K 31/00 (2006.01) A61K 31/155 (2006.01) A61P 3/10 (2006.01)

Patent

CA 2428782

The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti- hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti- hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti- hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti- hyperglycaemic medicine. The invention is applicable to the treatment of type II diabetes.

L'invention concerne une forme galénique orale pour la libération prolongée de principes actifs anti-hyperglycémiques (metformine). Ce médicament permet d'obtenir une couverture thérapeutique performante sur 24 heures en surmontant les problèmes de bipasse de la fenêtre d'absorption et de libération massive localisée de principes actifs. A cette fin, ce médicament comprend plusieurs milliers de microcapsules d'anti-hyperglycémiques (metformine) constituées chacune par un coeur comportant au moins un anti-hyperglycémique et par une pellicule d'enrobage appliquée sur le coeur et permettant la libération prolongée in vivo de l'anti-hyperglycémique. Ces microcapsules ont une granulométrie comprise entre 50 et 1000 microns. La reproductibilité de la cinétique de transit et donc la biodisponibilité sont très bonnes. Il en résulte pour le patient un risque moindre d'hyper ou d'hypoglycémie. L'invention concerne également la préparation de ce médicament et l'utilisation d'une pluralité de microcapsules telles que définies ci-dessus pour la fabrication d'un médicament anti-hyperglycémique. Application: traitement des diabètes de type II.

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