Controlled release formulations having rapid onset and rapid decline of effective plasma drug concentrations

  • US 9,066,869 B2
  • Filed: 10/09/2013
  • Issued: 06/30/2015
  • Est. Priority Date: 12/17/1998
  • Status: Expired due to Term
First Claim
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1. An oral controlled release formulation comprising a plurality of multi-layer release beads collectively comprising a dose of methylphenidate, each bead comprising:

  • (i) an outer immediate release layer comprising a portion of the dose of methylphenidate,(ii) a release delaying layer under the outer immediate release layer, the release delaying layer comprising a pH-dependent polymer,(iii) a controlled release layer under the release delaying layer, the controlled release layer comprising a hydrophobic material selected from the group consisting of an alkylcellulose, an acrylic polymer and mixtures thereof; and

    (iv) an immediate release core under the controlled release layer, the immediate release core comprising a further portion of the dose of methylphenidate,wherein from about 30% to about 40% of the dose of methylphenidate is in the outer immediate release layers of the beads and from about 60% to about 70% of the dose of methylphenidate is in the immediate release cores of the beads, andthe formulation provides(a) a time to a maximum plasma concentration of methylphenidate at about 0.5 to about 4 hours after oral administration to a human patient,(b) a plasma concentration of methylphenidate which does not differ by more than 10% during a measuring interval, wherein the measuring interval is from about 6 hours to about 12 hours, and(c) an in-vitro dissolution as follows;

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