Effervescent pharmaceutical formulations containing...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/48 (2006.01) A61K 9/16 (2006.01) A61K 9/46 (2006.01) A61K 9/51 (2006.01)

Patent

CA 2187153

Effervescent pharmaceutical formulations for the sustained and controlled oral administration of a drug selected from a calcium channel blocker, an ACE inhibitor, a narcotic analgesic or analogues or combinations thereof, the formulation comprising microcapsules in which the drug is entrapped in a biodegradable polymer, for example poly-L lactide. The pH of the formulation can be varied to optimize the release of the or each drug from the formulation. Microcapsules suitably have a D 50 % between about 100 nm and 900 nm and a drug loading of the order of about 10 % to 70 % by weight. The formulations can be used to administer the drugs to a patient on a once-daily basis so as to achieve a therapeutic effect over a substantially 24-hour period.

Formulations pharmaceutiques effervescentes servant à effectuer l'administration orale prolongée ou contrôlée d'un médicament sélectionné à partir d'un agent bloquant du canal de calcium, d'un inhibiteur d'ACE (enzyme de conversion d'angiotensine), d'un analgésique narcotique, ou de leurs analogues, ou de leurs combinaisons, ladite formulation étant composée de microgélules dans lesquelles le médicament est renfermé dans un polymère biodégradable, par exemple, poly-L-lactide. On peut modifier le pH de la formulation, afin d'optimiser la libération du médicament, ou de chaque médicament, de la formulation. Les microgélules possèdent, de préférence, un D 50 % situé entre 100 nm et 900 nm et une charge de médicament de l'ordre de 10 % à 70 % en poids. On peut utiliser ces formulations, afin d'administrer les médicaments à un patient selon une fréquence d'une fois par jour, de manière à réaliser un effet thérapeutique sur une durée de sensiblement 24 heures.

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