Delayed release formulations of 6-mercaptopurine

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01)

Patent

CA 2560997

The present invention provides enteric ally coated formulations of 6- mercaptopurine that exhibit a delay in release of the 6-mercaptopurine such that substantial release of 6-mercaptopurine does not occur until after passage through the stomach. Optionally, the formulations also comprise a delay coating in addition to the enteric coating that provides an even further delay such that substantial release of 6-mercaptopurine does not occur until after a certain period of time following passage through the stomach. Such a period of time is preferably at least one hour after passage through the stomach. Following the delay imparted by the enteric coating and optional delay coating, the formulations exhibit better bioavailability and faster dissolution than previous formulations.

La présente invention concerne des formulations de 6-mercaptopurine revêtues de façon entérique, présentant un délai de libération de 6-mercaptopurine de telle manière que l'essentiel de la 6-mercaptopurine ne soit pas libéré avant passage dans l'estomac. Lesdites formulations peuvent également contenir un revêtement de retardement, en plus du revêtement entérique, de façon à obtenir un effet retardateur supplémentaire, de telle manière que l'essentiel de la 6-mercaptopurine ne soit pas libéré avant un certain intervalle de temps après passage dans l'estomac. Un tel intervalle de temps est de préférence d'au moins une heure après passage dans l'estomac. Après le délai dû au revêtement entérique et au revêtement de retardement optionnel, les formulations selon l'invention présentent une meilleure biodisponibilité et une dissolution plus rapide que les formulations habituelles.

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