Injectable formulation of antibiotic and solution for...

A - Human Necessities – 61 – K

Patent

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A61K 38/15 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2656604

Disclosed is a pharmaceutical composition for injection purposes, which comprises WAP-8294A2 (a depsipeptide-type antibiotic) as an active ingredient, which is stable, and which contains WAP-8294A2 in a high concentration. Specifically, disclosed is a pharmaceutical composition for injection purposes, which comprises WAP-8294A2 having the structure represented by the formula (1) as an active ingredient and 2-hydroxypropyl-.beta.-cyclodextrin or .beta.-cyclodextrin as a stabilizing agent or a solubilizer, and whose pH value is not adjusted. Also disclosed is a solution for injection comprising WAP-8294A2,which can be prepared by mixing the pharmaceutical composition with a pH-adjusting agent comprising a solution containing disodium hydrogen phosphate, monosodium dihydrogen phosphate and sodium hydroxide and an infusion or a diluent such as dextrose just before use. (1)

L'invention concerne une composition pharmaceutique destinée à être utilisée pour une injection, laquelle comprend WAP-8294A<SUB>2</SUB> (un antibiotique de type depsipeptide) en tant qu'ingrédient actif, laquelle est stable et laquelle contient WAP-8294A<SUB>2</SUB> en concentration élevée. L'invention concerne précisément une composition pharmaceutique destinée à être utilisée pour une injection, laquelle comprend WAP-8294A<SUB>2</SUB> ayant la structure représentée par la formule (1) en tant qu'ingrédient actif et de la 2-hydroxypropyl-ß-cyclodextrine ou de la ß-cyclodextrine en tant qu'agent stabilisant ou agent de solubilisation et dont la valeur du pH n'est pas ajustée. L'invention concerne également une solution pour injection comprenant WAP-8294A<SUB>2</SUB>, laquelle peut être préparée en mélangeant la composition pharmaceutique avec un agent d'ajustement du pH comprenant une solution contenant de l'hydrogénophosphate disodique, du dihydrogénophosphate monosodique et de l'hydroxyde de sodium et avec une infusion ou un diluant tel que le dextrose juste avant utilisation. (1)

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