Method for Producing Coated Drugs Having a Stable Profile for the Release of Active Ingredients
The invention relates to methods for producing drugs having a stable profile for the release of active ingredients, said drugs exhibiting a controlled release characteristic as a result of the coating of vinyl (co)polymers. The inventive methods are characterised in that the coated drugs are conditioned in a fluidised bed coating appliance or a drum coating appliance for at least 10 minutes until a stable profile for the release of active ingredients is reached at a temperature of between 30 and 70° C. A humidity of between 5 and 30% is regulated during the conditioning process.
1 . A method for producing pharmaceutical forms having a stable active ingredient release profile, the pharmaceutical forms having controlled release characteristics on account of a coating of vinyl (co)polymers,
characterized in that
the coated pharmaceutical forms are conditioned at a temperature of 30 to 70° C. in a fluidized bed coating apparatus or a drum coating apparatus for at least 10 minutes until achievement of a stable active ingredient release profile, an atmospheric humidity of 5 to 30% being set during the conditioning.
2 . The method as claimed in claim 1 , characterized in that the coated pharmaceutical forms are produced in a first production step by coating active ingredient-containing cores or pellet cores with vinyl (co)polymers in a fluidized bed coating apparatus or a drum coating apparatus and optionally drying and in a second step carrying out the conditioning of the coated pharmaceutical forms in the same apparatus immediately after their production.
3 . The method as claimed in claim 1 , characterized in that the necessary atmospheric humidity is adjusted by spraying in water.
4 . The method as claimed in claim 1 , characterized in that an aqueous suspension comprising 0.1 to 5% by weight of release agent based on the suspension, is sprayed in.
5 . The method as claimed in claim 4 , characterized in that the release agent employed is talc, magnesium stearate or a silicic acid.
6 . The method as claimed in claim 1 , characterized in that the coatings of the pharmaceutical forms consist of (meth)acrylate (co)polymers or of polyvinyl acetate or derivatives of polyvinyl acetate.
7 . The method as claimed in claim 6 , characterized in that the coatings of the pharmaceutical forms consist of (meth)acrylate (co)polymers which are polymerized to more than 95% by weight to 100% from monomers containing neutral radicals.
8 . The method as claimed in claim 7 , characterized in that the (meth)acrylate copolymers are polymerized from 20 to 40% by weight of ethyl acrylate and 60 to 80% by weight of methyl methacrylate.
9 . The method as claimed in claim 6 , characterized in that the coatings of the pharmaceutical forms consist of cationic (meth)acrylate copolymers.
10 . The method as claimed in claim 9 , characterized in that the coatings of the pharmaceutical forms consist of (meth)acrylate copolymers which contain quaternary amino groups.
11 . The method as claimed in claim 10 , characterized in that the coating of the pharmaceutical forms consist of (meth)acrylate copolymers which are synthesized from free radical-polymerized units of 50-70% by weight of methyl methacrylate, 20-40% by weight of ethyl acrylate and 12-2% by weight of 2-trimethylammonium ethyl methacrylate chloride.
12 . The method as claimed in claim 9 , characterized in that the coatings of the pharmaceutical forms consist of (meth)acrylate copolymers which contain tertiary amino groups.
13 . The method as claimed in claim 12 , characterized in that the coatings of the pharmaceutical forms consist of (meth)acrylate copolymers which are synthesized from 20-30% by weight of methyl methacrylate, 20-30% by weight of butyl methacrylate and 60-40% by weight of dimethylaminoethyl methacrylate.
14 . The method as claimed in claim 6 , characterized in that the coatings of the pharmaceutical forms consist of anionic (meth)acrylate (co)polymers.
15 . The method as claimed in claim 4 , characterized in that the coatings of the pharmaceutical forms consist of anionic (meth)acrylate (co)polymers which consist to 25 to 95% by weight of free radical-polymerized C 1 - to C 4 -alkyl esters of acrylic or methacrylic acid and to 5 to 75% by weight of (meth)acrylate monomers containing an anionic group in the alkyl radical.