Formulations for tyrosine kinase inhibitors

A - Human Necessities – 01 – N

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A01N 43/42 (2006.01) A61K 31/44 (2006.01)

Patent

CA 2519106

The present invention is related to a powder, powder blend or granulation formulation of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H- quinolin-2-one, a tyrosine kinase inhibitor, which is adapted for reconstitution with a diluent. This invention is also related to a prepared aqueous suspension, or dispersion, formulation, particularly to a stable oral pharmaceutical formulation, comprising granules of 3-[5-(4-methanesulfonyl- piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one mixed with a diluent. Additionally, the present invention is related to the method of preparing these formulations.

La présente invention porte sur une poudre, un mélange de poudre ou une formulation de granulation of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one, sur un inhibiteur de tyrosine kinase qui est adapté pour la reconstitution avec un diluant. Cette invention porte également sur une suspension aqueuse préparée, ou sur une dispersion, une formulation, en particulier sur une formulation pharmaceutique stable se prenant par voie buccale, comprenant des granules de 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one mélangés à un diluant. La présente invention porte également sur un procédé de préparation de ces formulations.

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