Methods and dosage forms for controlled delivery of...

A - Human Necessities – 61 – K

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A61K 9/24 (2006.01) A61K 31/506 (2006.01) A61K 31/519 (2006.01) A61P 25/18 (2006.01)

Patent

CA 2494234

Dosage forms and methods for providing a substantially ascending rate of release of paliperidone are provided. The sustained release dosage forms provide therapeutically effective average steady-state plasma paliperidone concentrations when administered once per day. This once-a-day dosing regimen results in only one peak plasma paliperidone concentration occurrence in each 24 hour period. In addition, the peak plasma paliperidone concentration occurs at a later time following dose administration and exhibits a lesser magnitude than the peak plasma paliperidone concentration that occurs following administration of paliperidone in an immediate-release dosage form.

La présente invention concerne des formes de dose et des techniques permettant d'obtenir une vitesse de libération sensiblement croissante de palipéridone. Les formes de dose libérée en continu fournissent des concentrations moyennes de palipéridone plasmatique stables et thérapeutiquement efficaces lorsqu'elles sont administrées une fois par jour. Ce régime d'administration quotidien donne uniquement une crête dans la concentration de palipéridone plasmatique par période de 24 heures. Par ailleurs, cette crête de concentration de palipéridone plasmatique survient plus tardivement après l'administration de la dose et présente une amplitude moins grande que la crête de concentration de palipéridone plasmatique survenant après l'administration de palipéridone sous une forme de dose à libération immédiate.

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