Extended Release Formulation
First Claim
1. An oral extended release composition comprising an active ingredient selected from pramipexole and its pharmaceutically acceptable salts, derivatives, solvates, and isomers, wherein the active ingredient is released in vitro over a period of at least 4 hours and wherein the release profile is adapted to achieve average pramipexole plasma concentrations (Cavg) over the release period which does not differ by more than 25% from the Cavg achieved at steady state upon administration of a thrice daily immediate release formulation of pramipexole at the same total daily dose of pramipexole as is administered using the extended release composition, wherein the thrice daily administration of the immediate release formulation is conducted at time intervals of about 6 hours between the first and the second administration and between the second and the third administration.
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Abstract
The invention is directed to an extended release formulation comprising pramipexole or a pharmaceutically acceptable salt thereof.
81 Citations
16 Claims
- 1. An oral extended release composition comprising an active ingredient selected from pramipexole and its pharmaceutically acceptable salts, derivatives, solvates, and isomers, wherein the active ingredient is released in vitro over a period of at least 4 hours and wherein the release profile is adapted to achieve average pramipexole plasma concentrations (Cavg) over the release period which does not differ by more than 25% from the Cavg achieved at steady state upon administration of a thrice daily immediate release formulation of pramipexole at the same total daily dose of pramipexole as is administered using the extended release composition, wherein the thrice daily administration of the immediate release formulation is conducted at time intervals of about 6 hours between the first and the second administration and between the second and the third administration.
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2. An oral extended release composition comprising an active ingredient selected from pramipexole and its pharmaceutically acceptable salts, derivatives, solvates, and isomers, wherein the active ingredient is released in vitro over a period of at least 4 hours and wherein the release profile is adapted to achieve a time to peak plasma concentration (tmax) of pramipexole of at least about 2.5 hours after administration to a human in the fasted state.
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3. An oral sustained release composition comprising an active ingredient selected from pramipexole and its pharmaceutically acceptable salts, derivatives, solvates, and isomers, wherein the active ingredient is released in vitro over a period of at least 4 hours and wherein the released amount of active ingredient after 4 hours at pH 6.8, when determined at a basket rotation speed of 100 rpm, is not more than about 80% of the released amount of active ingredient when determined at a basket rotation speed of 100 rpm after 4 hours at pH 6.8.
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4. An oral extended release composition comprising an active ingredient selected from pramipexole and its pharmaceutically acceptable salts, derivatives, solvates, and isomers, wherein the release profile of the active ingredient is adapted to achieve a peak-trough fluctuation (PTF) of less than that obtained after reaching steady state conditions with an immediate release formulation of pramipexole given thrice a day.
Specification