Extended release formulation and method of treating...

A - Human Necessities – 61 – K

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A61K 9/22 (2006.01)

Patent

CA 2689978

A composition and method of treating adrenergic dysregulation by administering the composition is disclosed, wherein the composition comprises a .alpha.2-adrenergic receptor agonist; a pharmaceutically acceptable hydrophilic matrix and a release-retardant of a metal alkyl sulfate. In embodiments, the composition provides a sustained release of the agonist, wherein after administration of the composition no more than once about every 12 hours to a subject having a steady state plasma concentration of the .alpha.2-adrenergic receptor agonist, the agonist's plasma concentration peak-to-trough ratio is no greater than about 1.9.

L'invention concerne une composition et un procédé de traitement d'un dérèglement adrénergique en administrant la composition, où la composition comprend un agoniste du récepteur a2-adrénergique; une matrice hydrophile pharmaceutiquement acceptable et un retardateur de libération d'un sulfate d'alkyle de métal. Dans des modes de réalisation, la composition fournit une libération prolongée de l'agoniste, où après l'administration de la composition pas plus d'une fois environ toutes les 12 heures à un sujet ayant une concentration dans le plasma en équilibre dynamique de l'agoniste du récepteur a2-adrénergique, le rapport crête à creux de la concentration dans le plasma de l'agoniste n'est pas supérieur à environ 1,9.

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