Coated medicament forms with controlled active substance release
    1.
    发明授权
    Coated medicament forms with controlled active substance release 有权
    具有受控活性物质释放的涂层药物形式

    公开(公告)号:US06878387B1

    公开(公告)日:2005-04-12

    申请号:US09787438

    申请日:1999-09-28

    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.

    摘要翻译: 本发明涉及一种药物制剂,其包含:(a)含有活性物质的核心,任选的赋形剂和常见的药用添加剂,除了无机酸的盐,其核心重量的比例为2.5至97% (b)和由一种或多种(甲基)丙烯酸酯共聚物和任选的普通药用佐剂组成的外膜包衣,其中40至100重量%的(甲基)丙烯酸酯共聚物由93至98重量% 聚合丙烯酸或甲基丙烯酸的C 1至C 4 - 烷基酯和7至2重量%的在烷基中具有季铵基团的(甲基)丙烯酸酯单体,并且其可以任选地存在于由1至60% 一种或多种与上述(甲基)丙烯酸酯共聚物不同的另外的(甲基)丙烯酸酯共聚物的重量,其由85至100重量%的丙烯酸类聚丙烯酸酯的自由基聚合的C 1 -C 4烷基酯 酸和任选地和任选地至多15重量%的在烷基中具有碱性基团或酸基团的另外的(甲基)丙烯酸酯单体。

    Injection molding method for (meth)acrylate copolymers having tertiary ammonium groups
    2.
    发明授权
    Injection molding method for (meth)acrylate copolymers having tertiary ammonium groups 失效
    具有叔铵基的(甲基)丙烯酸酯共聚物的注射成型方法

    公开(公告)号:US06576255B1

    公开(公告)日:2003-06-10

    申请号:US09889565

    申请日:2001-07-30

    IPC分类号: A61K948

    CPC分类号: A61K9/1635 A61J3/071

    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.

    摘要翻译: 本发明涉及一种通过注射成型制备模塑制品的方法,其工艺步骤为:a)熔融(甲基)丙烯酸酯共聚物,其由30至80重量%的自由基聚合的C1至C4烷基酯组成 丙烯酸或甲基丙烯酸和70〜20重量%的烷基残基中具有叔铵基的(甲基)丙烯酸酯单体,其中(甲基)丙烯酸酯共聚物与1至70重量%的增塑剂和干燥剂 以1:1至1:20的比例和0.05至5重量%的脱模剂,并且进一步的标准添加剂或佐剂,并且如果需要甚至药物活性成分也可以存在于混合物中,并且在混合物之前 熔化,其含量大于0.5重量%的低沸点成分,蒸气压在120℃下至少为1.9巴,b)在热塑性条件下,在至少120℃的温度下脱气混合物 ,其中低沸点成分含量为a 在120℃下至少1.9巴的蒸汽压降低至至多0.5重量%,和c)将熔融和脱气的混合物注射到注射成型模具的模腔中,其中模腔具有位于 在(甲基)丙烯酸酯共聚物的玻璃化转变温度以下至少10℃,冷却熔融混合物并从模具中除去得到的模塑制品。

    Multilayer pharmaceutical product for release in the colon
    5.
    发明授权
    Multilayer pharmaceutical product for release in the colon 有权
    多层药物在结肠中释放

    公开(公告)号:US06632454B2

    公开(公告)日:2003-10-14

    申请号:US09926567

    申请日:2001-11-19

    IPC分类号: A61K958

    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.

    摘要翻译: 本发明涉及多层药物产品的应用,其基本上包括a)含有药物活性物质的核心,b)由共聚物或共聚物混合物组成的内涂层,其由85-98wt。%的 丙烯酸或甲基丙烯酸的自由基聚合的C1-C4烷基酯和在烷基中具有季铵基团的15至2重量%的(甲基)丙烯酸酯单体,和c)由共聚物组成的外涂层, 75至95重量%的丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯和5至25重量%的在(甲基)丙烯酸烷基酯中具有阴离子基团的(甲基)丙烯酸酯单体。 本发明产品用于生产一种药物产品,根据USP的释放试验,在pH2.2的时间内释放其中所含的活性物质,并在试验开始后的2.0小时内,随后的反渗透至pH 7.0,小于5% 并且在开始测试后八小时后,再增加30到80%

    Multi-particulate form of medicament, comprising at least two differently coated forms of pellet
    6.
    发明授权
    Multi-particulate form of medicament, comprising at least two differently coated forms of pellet 有权
    多颗粒形式的药物,包含至少两种不同的包衣形式的丸剂

    公开(公告)号:US07438929B2

    公开(公告)日:2008-10-21

    申请号:US10949323

    申请日:2004-09-27

    IPC分类号: A61K9/52 A61K9/14

    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.

    摘要翻译: 本发明涉及适于在小肠和大肠中均匀释放活性药物成分的多颗粒药物形式,其包含至少两种形式的颗粒A和B,其包含芯中的活性药物成分并具有不同的聚合物 确定在不同pH值下释放活性成分的涂层,其特征在于,颗粒形式A具有能够连续释放活性成分的内部聚合物涂层,并且具有快速溶解在约pH 5.5以上的外部肠溶衣,以及 颗粒形式B具有聚合物涂层,其在USP释放试验中在6小时内在pH 6.8下释放少于20%的活性成分,并在6小时内在pH 7.2下释放超过50%的活性成分。 本发明还涉及生产多颗粒药物形式的方法以及用于制备药物形式的颗粒形式A和B的用途。

    Binding agent which is stable in storage and used for pharmaceutical applications
    8.
    发明申请
    Binding agent which is stable in storage and used for pharmaceutical applications 审中-公开
    在储存中稳定并用于制药应用的结合剂

    公开(公告)号:US20050019381A1

    公开(公告)日:2005-01-27

    申请号:US10239187

    申请日:2001-01-29

    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.

    摘要翻译: 本发明涉及用于皮肤或透皮治疗系统的粘合剂和粘合剂,其由(a)由丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯和(甲基)丙烯酸酯单体与阳离子铵组成的(甲基)丙烯酸酯共聚物 在(a)有机二羧酸或三羧酸或丙烯酸酯或(甲基)丙烯酸酯或含有酸基团的共聚物或共聚物中,(a)为(a)为0.1-45重量% c)相对于(a)增塑剂为20-80重量%,和(d)如果需要,药物活性物质和/或药学上通常的添加剂,其特征在于包含癸二酸二丁酯作为增塑剂。

    Multi-particulate form of medicament, comprising at least two differently coated forms of pellet
    9.
    发明申请
    Multi-particulate form of medicament, comprising at least two differently coated forms of pellet 有权
    多颗粒形式的药物,包含至少两种不同的包衣形式的丸剂

    公开(公告)号:US20050053660A1

    公开(公告)日:2005-03-10

    申请号:US10949323

    申请日:2004-09-27

    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.

    摘要翻译: 本发明涉及适于在小肠和大肠中均匀释放活性药物成分的多颗粒药物形式,其包含至少两种形式的颗粒A和B,其包含芯中的活性药物成分并具有不同的聚合物 确定在不同pH值下释放活性成分的涂层,其特征在于,颗粒形式A具有能够连续释放活性成分的内部聚合物涂层,并且具有快速溶解在约pH 5.5以上的外部肠溶衣,以及 颗粒形式B具有聚合物涂层,其在USP释放试验中在6小时内在pH 6.8下释放少于20%的活性成分,并在6小时内在pH 7.2下释放超过50%的活性成分。 本发明还涉及生产多颗粒药物形式的方法以及用于制备药物形式的颗粒形式A和B的用途。

    Multilayer dosage forms, which contain active substances and which comprise a neutral core, and an inner and outer coating consisting of methacrylate copolymers and methacrylate monomers
    10.
    发明申请
    Multilayer dosage forms, which contain active substances and which comprise a neutral core, and an inner and outer coating consisting of methacrylate copolymers and methacrylate monomers 审中-公开
    包含活性物质并且包含中性核心的多层剂型,以及由甲基丙烯酸酯共聚物和甲基丙烯酸酯单体组成的内外涂层

    公开(公告)号:US20060204576A1

    公开(公告)日:2006-09-14

    申请号:US10532831

    申请日:2003-09-04

    IPC分类号: A61K9/24

    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.

    摘要翻译: 本发明涉及一种多层剂型,其包括:a)中性核; b)由甲基丙烯酸酯共聚物组成的内涂层; c)由共聚物组成的外涂层,其中40至95重量%由丙烯酸或甲基丙烯酸的C 4-14烷基酯的自由基聚合的C 1〜 并且其中5至60重量%由在烷基中具有阴离子基团的(甲基)丙烯酸酯单体组成。 本发明的特征在于,内涂层基本上由甲基丙烯酸酯共聚物组成,其中至少高达90重量%由具有中性自由基的(甲基)丙烯酸酯单体组成,其根据DIN 53787具有最小值 成膜温度不高于30℃,含有结合形式的药物活性物质。