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US 9,801,823 B2Granted
Controlled release formulations having rapid onset and rapid decline of effective plasma drug concentrations
AssigneeRhodes Pharmaceuticals L.P.
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.
Claims12
A formulation comprising:
- a plurality of substrates comprising a portion of an effective dose of methylphenidate or a pharmaceutically acceptable salt coated with a hydrophobic material in an amount to obtain a weight gain from about 2% to about 25%, the hydrophobic material comprising a first acrylic polymer,
- an enteric coating applied over said hydrophobic material in an amount sufficient to delay the release of said portion until after said formulation passes through the stomach, wherein said enteric coating is derived from an aqueous dispersion comprising a second acrylic polymer,
- the formulation further comprising the remaining portion of said dose in an immediate release form,
- wherein the formulation provides a biphasic release profile, a mean maximum plasma concentration of said methylphenidate at about 2 hours and methylphenidate plasma concentrations below effective plasma concentration at about 8 hour to about 12 hours after an oral administration.
1 more element
A formulation comprising:
- a plurality of substrates comprising a portion of an effective dose of methylphenidate or a pharmaceutically acceptable salt coated with a hydrophobic material in an amount to obtain a weight gain from about 2% to about 25%, the hydrophobic material comprising an alkylcellulose, a first acrylic polymer or mixtures thereof,
- an enteric coating applied over said hydrophobic material in an amount sufficient to delay the release of said portion until after said formulation passes through the stomach, wherein said enteric coating is derived from an aqueous dispersion comprising a second acrylic polymer, the formulation further comprising the remaining portion of said dose in an immediate release form,
- wherein the formulation provides a mean AUC0-t of 48493.80 pg×h/ml, a mean AUC0-inf of 51213.86 pg×h/ml, a mean Cmax of 4410.25 pg/ml, a mean Tmax of 3.27 hours, a mean Kel of 0.1672 h−1, and a mean T1/2 el of 4.32 hours, based on a fasting administration of a formulation comprising 20 mg of said methylphenidate.
Dependencies are inferred from the claim text.