Once-daily administration of central nervous system drugs

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/52 (2006.01) A61K 9/16 (2006.01) A61K 31/137 (2006.01) A61K 31/421 (2006.01) A61K 31/439 (2006.01) A61K 31/4458 (2006.01) A61K 31/485 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2628031

Delayed onset chronotherapeutic formulations of central nervous system (CNS) drugs are disclosed. The formulations comprise at least one CNS drug or pharmaceutically acceptable salt thereof that exhibits an in vivo elimination half-life of less than about 8 hours, wherein the formulation exhibits at least one in vivo parameter, at steady state following administration to a subject, chosen from: an initial lag in absorption from about 2 hours to about 6 hours; a peak-to-trough ratio greater than or equal to about 4:1; a percent fluctuation of greater than or equal to about 100%; and a minimum time cover of greater than or equal to 50% of Cmax of at least 8 hours.

La présente invention concerne des formulations chronothérapeutiques à action retardée de médicaments agissant sur le système nerveux central (SNC). Les formulations contiennent au moins un médicament, ou un sel pharmaceutiquement acceptable de ce médicament, qui agit sur le SNC et possède une demi-vie d'élimination in vivo inférieure à environ 8 heures, la formulation possédant, à l'état stationnaire qui suit l'administration à un sujet, au moins un paramètre in vivo choisi parmi : un retard initial d'absorption d'environ 2 heures à environ 6 heures, un rapport pic à creux supérieur ou égal à environ 4:1, un pourcentage de fluctuation supérieur ou égal à environ 100 %, et un champ d'action minimum supérieur ou égal à 50 % de Cmax d'au moins 8 heures.

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