摘要:
The invention relates to a pharmaceutical preparation consisting of: (a) a core containing an active substance, optionally an excipient and common pharmaceutical additives in addition to the salt of an inorganic acid whose proportion in the weight of the core ranges from 2.5 to 97% by weight and (b) and outer film coating consisting of one or more (meth)acrylate copolymers and optionally common pharmaceutical adjuvants, wherein 40 to 100% by weight of the (meth)acrylate copolymers consist of 93 to 98% by weight of radically polymerized C1- to C4-alkylesters of acrylic or methacrylic acid and 7 to 2% by weight of (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical and that may be optionally present in a mixture consisting of 1 to 60% by weight of one or more additional (meth)acrylate copolymers different from the above-mentioned (meth)acrylate copolymers, consisting of 85 to 100% by weight of a radically polymerized C1- to C4-alkylesters of acrylic orethacrylic acid and optionally and optionally up to 15% by weight of additional (meth)acrylate monomers with basic groups or acid groups in the alkyl radical.
摘要:
The invention relates to a process for making molded articles by means of injection molding with the process steps of a) melting of a (meth)acrylate copolymer, which is composed of 30 to 80 wt % of radical-polymerized C1 to C4 alkyl esters of acrylic or methacrylic acid and 70 to 20 wt % of (meth)acrylate monomers with a tertiary ammonium group in the alkyl residue, wherein the (meth)acrylate copolymer is present in a mixture with 1 to 70 wt % of a plasticizer and a desiccant in the ratio of 1:1 to 1:20 and also with 0.05 to 5 wt % of a release agent, and further standard additives or adjuvants and if necessary even a pharmaceutical active principle can also be present in the mixture, and before the mixture is melted it has a content of more than 0.5 wt % of low-boiling constituents with a vapor pressure of at least 1.9 bar at 120° C., b) degassing of the mixture in the thermoplastic condition at temperatures of at least 120° C., whereby the content of low-boiling constituents with a vapor pressure of at least 1.9 bar at 120° C. is lowered to at most 0.5 wt % and c) injection of the melted and degassed mixture into the mold cavity of an injection-molding die, wherein the mold cavity has a temperature which lies at least 10° C. below the glass transition temperature of the (meth)acrylate copolymer, cooling of the melt mixture and removal of the obtained molded article from the mold.
摘要:
The invention relates to an adhesive and binder for dermal or transdermal therapy systems, that includes (a) 85-99.9 weight % of (meth)acrylate copolymer of structural and functional monomers, where the functional monomers have tertiary or quaternary amino groups, (b) 0.1-15 weight % of an organic dicarboxylic or tricarboxylic acid, and (c) 40-70 weight %, relative to the total of (a) and (b), of a plasticizer.
摘要:
The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C. into the mould of an injection moulding system and removing the resultant moulding from the mould.
摘要:
The invention relates to the use of a multilayer pharmaceutical product that substantially comprises a) a core containing a pharmaceutically active substance, b) an inner coating consisting of a copolymer or a mixture of copolymers that are composed of 85 to 98 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 15 to 2 wt.- % of (meth)acrylate monomers with a quaternary ammonium group in the alkyl group, and c) an outer coating consisting of a copolymer that is composed of 75 to 95 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 5 to 25 wt.- % of (meth)acrylate monomers with an anionic group in the alkyl group. The inventive product is used for producing a pharmaceutical product that releases the active substance contained therein according to the USP release test, at pH 1.2 during 2 hours and subsequent rebuffering to pH 7.0, by less than 5% after 2.0 hours after start of the test and by 30 to 80% after eight hours after start of the test.
摘要:
The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
摘要:
The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
摘要:
The invention relates to an adhesive and binder for dermal or transdermal therapy systems, consisting of (a) a (meth)acrylate copolymer composed of radically polymerized C1 to C4 alkyl esters of acrylic or methacrylic acid and (meth)acrylate monomers with a cationic ammonium group in the alkyl radical, containing (b) 0.1-45 wt.-% with reference to (a) of an organic dicarboxylic or tricarboxylic acid or an acrylate or (meth)acrylate polymer or copolymer containing an acid group, as well as (c) 20-80 wt.-% with reference to (a) of a plasticizer, and (d) if necessary, a pharmaceutically active substance and/or pharmaceutically usual additives, characterized in that dibutyl sebacate is contained as the plasticizer.
摘要:
The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.
摘要:
The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.