Controlled release formulations having rapid onset and rapid decline of effective plasma drug concentrations
AssigneeEuro-Celtique S.A.
InventorsThinnayam N. Krishnamurthy, Andrew Darke
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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.
Claims18
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
- a plurality of substrates comprising a portion of the effective dose of a drug 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 drug in immediate release form;
- wherein the oral dosage form provides a time to maximum plasma concentration at about 0.5 to about 4 hours after oral administration and wherein the duration of effect provided by the drug contained in the formulation falls below effective plasma concentrations at about 8 to about 12 hours after oral administration.
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 a plurality of substrates comprising a portion of the effective dose of a drug in immediate release form by spraying a solution of the drug onto said substrates;
- applying a hydrophobic material to said substrates in an amount to retard the release of said drug;
- applying an enteric coating 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;
- applying an immediate release overcoat of said drug onto said enteric coated substrates;
- wherein the oral dosage form provides a time to maximum plasma concentration at about 0.5 to about 4 hours after oral administration and wherein the duration of effect provided by the drug contained in the formulation falls below effective plasma concentrations at about 8 to about 12 hours after oral administration.
Dependencies are inferred from the claim text.