Antibiotic compositions of modified release and process of...

A - Human Necessities – 61 – K

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A61K 31/43 (2006.01) A61K 9/22 (2006.01) A61K 9/52 (2006.01) A61K 31/424 (2006.01) A61P 31/00 (2006.01)

Patent

CA 2644911

Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60 % of the antibiotic in about 30 minutes and not less than about 70 % of the antibiotic after 8 hours when subjected to in vitro dissolution study or when tested in vivo. Further, the compositions of the present invention which when tested in a group of healthy humans provide a mean peak plasma concentration (Cmax) after at least about 0.5 hour of administration of the dosage form. The present invention also provides process of preparing such dosage form and methods of using such dosage form.

La présente invention concerne des compositions pharmaceutiques à libération modifiée innovantes qui comprennent au moins un antibiotique, de préférence de l'amoxicilline ou ses sels, esters, polymorphes, isomères, promédicaments, solvates, hydrates ou dérivés pharmaceutiquement acceptables, seul ou en combinaison avec un ou des autres antibiotiques en tant que matière active, avec au moins un agent modificateur de la libération destiné à réguler la libération du bêta lactame antibiotique, facultativement avec un ou plusieurs autres excipients pharmaceutiquement acceptables, la forme pharmaceutique assurant une libération ne dépassant pas environ 60 % de l'antibiotique en environ 30 minutes et n'étant pas inférieure à environ 70 % de l'antibiotique après 8 heures dans une étude de dissolution in vitro ou lors d'un essai in vivo. L'invention concerne en outre des compositions qui, lors d'essais sur un groupe d'humains en bonne santé, fournit une concentration plasmatique maximale moyenne (Cmax) au moins environ 0,5 heure après l'administration de la forme pharmaceutique. La présente invention concerne également des procédés de préparation d'une telle forme pharmaceutique et des procédés d'utilisation d'une telle forme pharmaceutique.

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