Effervescent granules and methods for their preparation

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/16 (2006.01) A61K 9/00 (2006.01) A61K 9/20 (2006.01) A61K 9/46 (2006.01)

Patent

CA 2406833

Disclosed here are effervescent granules having a controllable rate of effervescence. In some embodiments, the such granules comprise an acidic agent, an alkaline agent, a pharmacologically active agent, hot-melt extrudable binder capable of form-ing a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process. The present invention also provides a thermal heat process for preparing a pharmacologically active agent containing ef-fervescent granule. In certain aspects, the granules contain pharmacologically active agents such as narcotics, antidiarrheal agents, antiviral agents, anxiolytic agents, a cholesterol lowering agent, an alpha adrenergic blocking agent, a phenanthrene derivative. By way of example, some of the narcotics that may be included in the granules and in the process of preparing the granules include, by way of example: phenanthrene derivatives (e.g., morphine sulfate), and morphine derivatives (e.g., hydromorphone hydrochloride).

La présente invention concerne des granulés effervescents à taux d'effervescence contrôlable. Dans certains modes de réalisation de l'invention, ces granulés comprennent un agent acide, un agent alcalin, un agent pharmacologiquement actif, un liant extrudable à chaud capable de former un mélange eutectique avec l'agent acide et, éventuellement, un ramollissant. Ces granulés effervescents sont fabriqués par processus d'extrusion à chaud. Cette invention concerne aussi un processus thermique permettant de préparer ce granulé effervescent contenant un agent pharmacologiquement actif. Dans certains aspects de cette invention, les granules contiennent des agents pharmacologiquement actifs tel que des agents narcotiques, antidiarrhéiques, des agents antiviraux, anxiolytiques, des agents réducteurs de cholestérol, un agent bloquant alpha-adrénergique, un dérivé de phénanthrène. A titre d'exemple, certains de ces agents narcotiques qui peuvent être inclus dans les granulés et dans ce processus de préparation de granulés comprennent: des dérivés de phénanthrène (par exemple un sulfate de morphine), et des dérivés de morphine (par exemple un hydrochlorure d'hydromorphone).

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