Controlled release formulations coated with aqueous dispersions of acrylic polymers
AssigneePurdue Pharma L.P.
InventorsBenjamin Oshlack, Mark Chasin, Frank Pedi, Jr.
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Abstract
A stable solid controlled release formulation having a coating derived from an aqueous dispersion of a hydrophobic acrylic polymer includes a substrate including an active agent selected from the group consisting of a systemically active therapeutic agent, a locally active therapeutic agent, a disinfecting and sanitizing agent, a cleansing agent, a fragrance agent and a fertilizing agent, overcoated with an aqueous dispersion of the plasticized water-insoluble acrylic polymer. The formulation provides a stable dissolution of the active agent which is unchanged after exposure to accelerated storage conditions.
Claims20
A method for obtaining a controlled release formulation of an active agent, comprising:
- preparing a solid substrate comprising an active agent;
- coating said substrate with a sufficient amount of an aqueous dispersion of (i) a plasticized water-insoluble acrylic polymer comprised of monomers selected from the group consisting of an ester of acrylic acid, an ester of methacrylic acid, an alkyl ester of acrylic acid, an alkyl ester of methacrylic acid, and mixtures of any of the foregoing, and (ii) a further material selected from the group consisting of a polymerizable permeability-enhancing agent, a water-soluble acrylic polymer, a pore-former, and mixtures of any of the foregoing, to provide a controlled release of said active agent when said coated substrate is exposed to an environmental fluid, and
- curing said coated substrate at a temperature greater than the glass transition temperature of the plasticized water-insoluble acrylic polymer until a curing endpoint is reached at which said coated substrate upon exposure to an environmental fluid provides a band range, when comparing the dissolution profile after exposure to accelerated storage conditions of at least one month at 40.degree. C./75% RH to the dissolution profile prior to exposure of said coated substrate to said accelerated storage conditions, which is not wider than about 15% of total active agent released at any point of time during said dissolution.
The method of obtaining a solid controlled release oral dosage formulation comprising;
- preparing a substrate comprising a systemically active therapeutic agent in an amount sufficient to provide a desired therapeutic effect when said formulation is orally administered and coating said substrate with an aqueous dispersion of a plasticized copolymer of acrylic and methacrylic acid esters having a permeability which is unaffected by the pH conditions prevailing in the digestive tract, to a weight gain sufficient to obtain a controlled release of said active agent when measured by the U.S.P. Paddle or Basket Method at 100 rpm at 900 ml aqueous buffer (pH1 between 1.6 and 7.2) at 37.degree. C. from about 0% to about 42.5% (by wt) active agent released after 1 hour, from about 25% to about 55% (by wt) active agent released after 2 hours, from about 45% to about 75% (by wt) active agent released after 4 hours and greater than about 55% (by wt) active agent released after 6 hours, said coated substrate when subjected to accelerated storage conditions of at least one month at 40.degree. C./75% RH releasing an amount of said therapeutically active agent upon in-vitro dissolution which does not vary at any given time point by more than about 15% of the total amount of therapeutically active agent released when compared to in-vitro dissolution conducted prior to storage, and when administered orally providing effective blood levels of said systemically active therapeutic agent for at least about 12 hours.
A method for obtaining a controlled release formulation of an active agent, comprising:
- preparing a solid substrate comprising an active agent;
- coating said substrate with a sufficient amount of an aqueous dispersion of a plasticized water-insoluble acrylic polymer comprised of monomers selected from the group consisting of an ester of acrylic acid, an ester of methacrylic acid, an alkyl ester of acrylic acid, an alkyl ester of methacrylic acid, and mixtures of any of the foregoing, and
- curing said coated substrate at a temperature greater than the glass transition temperature of the aqueous dispersion of plasticized water-insoluble acrylic polymer until a curing endpoint is reached at which said coated substrate upon exposure to an environmental fluid provides a band range, when comparing the dissolution profile after exposure to accelerated storage conditions of at least one month at 40.degree. C./75% RH to the dissolution profile prior to exposure of said coated substrate to said accelerated conditions, which is not wider than about 15% of total active agent released at any point of time during said dissolution.
Dependencies are inferred from the claim text.