Injectable preparations of diclofenic and its...

A - Human Necessities – 61 – K

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A61K 31/196 (2006.01) A61K 9/08 (2006.01)

Patent

CA 2596031

The present invention provides injectable formulations of water-soluble salts of diclofenac in single doses of less than 2 ml, which cause significantly less pain at the site of injection and can be administered by intradeltoid route, in addition to intragluteal and slow intravenous route. More specifically the injectable preparations contain 75 mg to 100 mg of water- soluble salts of diclofenac, in about 1 ml injection solution without significantly raising the viscosity of the injection solution without the use surfactants. The formulations are adjusted to pH 6 to 10 containing up to 100mg of diclofenac salt in a medium comprising of water, along with one or more co-solvent(s) / solubiliser(s), antioxidants, preservatives, buffers, alkali and stabilizers.

L'invention concerne des formulations injectables de sels hydrosolubles de diclofénac en doses uniques inférieures à 2 ml, engendrant nettement moins de douleur au niveau du site d'injection et pouvant être administrées par voie intradeltoïde et par voie intrafessier et intraveineuse lente. Plus précisément, les préparations injectables renferment entre 75 mg et 100 mg de sels hydrosolubles de diclofénac, dans une solution d'injection d'environ 1 ml sans augmentation importante de la viscosité de la solution d'injection et sans avoir recours à des tensioactifs. Les formulations sont adaptées à un pH compris entre 6 et 10 renfermant jusqu'à 100mg de sel de diclofénac dans un milieu comprenant de l'eau, conjointement avec un ou plusieurs co-solvant(s) / agent(s) de solubilisation, antioxydants, conservateurs, tampons, alcalins et agents de stabilisation.

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