Controlled release formulations having rapid onset and rapid decline of effective plasma drug concentrations
First Claim
1. A oral controlled release formulation which provides a rapid onset of therapeutic effect and a rapid drop in plasma concentration after a prolonged period of therapeutic effect, comprising a plurality of substrates comprising a portion of the effective dose of a therapeutically active agent in immediate release form, a hydrophobic material coated onto the surface of said substrates in an amount sufficient to retard the release of said drug, an enteric coating applied over said hydrophobic coating in an amount sufficient to substantially delay the release of said drug from said substrate until after said formulation passes through the stomach, the formulation further comprising the remaining portion of said therapeutically active agent in immediate release form.
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Accused Products
Abstract
The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.
19 Citations
20 Claims
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1. A oral controlled release formulation which provides a rapid onset of therapeutic effect and a rapid drop in plasma concentration after a prolonged period of therapeutic effect, comprising
a plurality of substrates comprising a portion of the effective dose of a therapeutically active agent in immediate release form, a hydrophobic material coated onto the surface of said substrates in an amount sufficient to retard the release of said drug, an enteric coating applied over said hydrophobic coating in an amount sufficient to substantially delay the release of said drug from said substrate until after said formulation passes through the stomach, the formulation further comprising the remaining portion of said therapeutically active agent in immediate release form.
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14. A method for preparing an oral controlled release formulation which provides a rapid onset of therapeutic effect and a rapid drop in plasma concentration after a prolonged period of therapeutic effect, comprising
preparing immediate release drug-coated inert beads by spraying a solution of the drug onto said inert beads; -
applying release coating to said immediate release drug-coated beads to convert the same into controlled release beads;
applying an enteric coating onto said controlled release coating; and
applying and immediate release overcoat of said drug onto the surface of said enteric coated beads. - View Dependent Claims (15, 16, 17, 18, 19, 20)
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Specification