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    Pharmaceutical combination preparation for hormonal contraception
    1.
    发明授权
    Pharmaceutical combination preparation for hormonal contraception 失效
    药物组合制剂用于激素避孕

    公开(公告)号：US5756490A

    公开(公告)日：1998-05-26

    申请号：US718401

    申请日：1996-12-16

    申请人： Ursula Lachnit ,  Bernd Dusterberg ,  Jurgen Spona

    发明人： Ursula Lachnit ,  Bernd Dusterberg ,  Jurgen Spona

    IPC分类号： A61K31/565 ,  A61K31/57 ,  A61P15/18 ,  C07J1/00 ,  A61K31/56

    CPC分类号： A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  Y10S514/843

    摘要： A pharmaceutical combination preparation with two hormone components that are manufactured physically separately in a packaging unit and that are intended for time-sequential oral administration, which in each case consist of a number of daily dosage units that are placed physically separately and are individually removable in the packaging unit. As a hormonal active ingredient, a first hormone component contains in combination an estrogen preparation and, in at least a dosage that is sufficient to inhibit ovulation, a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation. The first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4 to 10 daily units. The total number of hormone daily units is equal to the total number of days of the desired cycle, but at least 28 days in length. This combination preparation is used for female birth control, and allows for an estrogen content that is as low as possible in each individual dosage unit and also has a low total hormone content per administration cycle, with high contraceptive reliability, low incidence of follicular development, and satisfactory cycle control, with reliable avoidance of intracyclic menstrual bleeding as well as of undesirable side-effects.

    摘要翻译： PCT No.PCT / EP95 / 01190 Sec。 371日期1996年12月16日第 102（e）日期1996年12月16日PCT提交1995年3月30日PCT公布。 公开号WO95 / 26730 PCT 日期1995年10月12日一种具有两种激素组分的药物组合制剂，其在包装单元中物理分开制造，并且用于时间顺序的口服给药，其每种情况由多个物理分开的每日剂量单位组成 并且可以在包装单元中单独移除。 作为激素活性成分，第一激素成分组合含有雌激素制剂，至少含有足以抑制排卵的剂量，孕激素制剂，作为激素活性成分，第二激素成分仅含有雌激素制剂。 第一激素组分包含23或24日单位，第二激素组分包含4至10个每日单位。 激素每日单位的总数等于所需周期的总天数，但长度至少为28天。 这种组合制剂用于女性避孕，并且允许在每个单独剂量单位中尽可能低的雌激素含量，并且每个给药周期的总荷尔蒙含量低，具有高避孕可靠性，滤泡发育发生率低， 和令人满意的周期控制，可靠地避免周期性月经出血以及不良副作用。

    Pharmaceutical combination preparation for hormonal contraception
    3.
    发明授权
    Pharmaceutical combination preparation for hormonal contraception 失效
    药物组合制剂用于激素避孕

    公开(公告)号：US5980940A

    公开(公告)日：1999-11-09

    申请号：US930630

    申请日：1998-01-27

    申请人： Jurgen Spona ,  Bernd Dusterberg

    发明人： Jurgen Spona ,  Bernd Dusterberg

    IPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/585 ,  A61P15/08 ,  A61K31/56

    CPC分类号： A61K31/57 ,  A61K31/565 ,  A61K31/585 ,  Y10S514/843

    摘要： The invention provides a pharmaceutical combination preparation with two hormone components in a packaging unit and intended for time-sequential oral administration, comprising a number of daily dosage units physically separate and individually removable in the packaging unit, whereby as a hormonal active ingredient a first hormone component contains in combination an estrogen preparation and in at least a dosage that is sufficient to inhibit ovulation a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation, whereby the first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4, 3 or 2 daily units, and between these two hormone components, 2 or 1 active ingredient-free daily units are present or 2 or 1 blank pill days are indicated, and the total number of hormone daily units and the active ingredient-free daily units or the blank pill days is equal to the total number of days of the desired cycle, but at least 28 days in length. This combination preparation is useful for female birth control, and allows for an estrogen content that is as low as possible in each individual dosage unit and also has a low total hormone content per administration cycle, with high contraceptive reliability, low incidence of follicular development, and satisfactory cycle control, with reliable avoidance of intracyclic menstrual bleeding as well as of undesirable side-effects.

    摘要翻译： PCT No.PCT / EP96 / 01529 Sec。 371日期：1998年1月27日 102（e）日期1998年1月27日PCT提交1996年4月4日PCT公布。 出版物WO96 / 32114 日期：1996年10月17日本发明提供了包装单元中具有两种激素组分的药物组合制剂，其用于时间顺序的口服给药，其包括在包装单元中物理分离并可单独除去的多个日剂量单位，由此作为激素 活性成分第一激素成分组合含有雌激素制剂和至少一种足以抑制孕妇制剂排卵的剂量，并且作为激素活性成分，第二激素成分仅含有雌激素制剂，其中第一激素成分包含 23或24日单位，第二激素成分含有4，3或2日单位，在这两种激素组分之间，存在2或1种无活性成分的每日单位，或者指示2或1个空白药丸日， 激素每日单位数量和无活性成分的每日单位或空白药片天数等于t 期望周期的天数，但长度至少为28天。 这种组合制剂对于女性避孕是有用的，并且允许在每个单独剂量单位中尽可能低的雌激素含量，并且每个给药周期具有低的总激素含量，具有高避孕可靠性，滤泡发育发生率低， 和令人满意的循环控制，可靠地避免周期性月经出血以及不良副作用。

    NEW DROSPIRENONE/17BETA-ESTRADIOL REGIMEN, PHARMACEUTICAL COMBINATION PRODUCT AND KIT FOR PERFORMING THIS REGIMEN
    6.
    发明申请
    NEW DROSPIRENONE/17BETA-ESTRADIOL REGIMEN, PHARMACEUTICAL COMBINATION PRODUCT AND KIT FOR PERFORMING THIS REGIMEN 审中-公开
    新的DROSPIRENONE / 17BETA-ESTRADIOL REGIMEN，药物组合产品和用于执行本方案的工具包

    公开(公告)号：US20090023693A1

    公开(公告)日：2009-01-22

    申请号：US12098831

    申请日：2008-04-07

    申请人： Vladimir HANES ,  Hartnut Blode ,  Rolf Schurmann ,  Bernd Dusterberg ,  Joachim Marr

    发明人： Vladimir HANES ,  Hartnut Blode ,  Rolf Schurmann ,  Bernd Dusterberg ,  Joachim Marr

    IPC分类号： A61K31/56 ,  A61P15/18

    CPC分类号： A61K31/565 ,  A61K31/585

    摘要： The present invention relates to a pharmaceutical combination product with at least 21 daily consecutive dosage units containing from 2.0 mg to 3.0 mg of drospirenone and 1.0 to 2.0 mg of 17β-estradiol in each daily dosage unit followed by intermittent daily dosage units containing the same or smaller amount of drospirenone (i.e. 0.5 mg to 3.0 mg) as the consecutive daily dosage units wherein each intermittent daily dosage unit is preceded by at least one day without administration of drospirenone.These pharmaceutical combination products can be used for female oral contraception, guarantee a withdrawal bleeding each 4 weeks and allow for the full maintenance of the drospirenone related benefits.

    摘要翻译： 本发明涉及药物组合产品，其具有至少21个每日连续剂量单位，每个日剂量单位含有2.0mg至3.0mg的屈螺酮和1.0至2.0mg的17β-雌二醇，随后是含有其的间歇性日剂量单位或 较小量的屈螺酮（即0.5mg至3.0mg）作为连续的每日剂量单位，其中每个间歇日剂量单位之前至少一天，而不服用屈螺酮。 这些药物组合产品可用于女性口服避孕药，保证每4周戒断出血，并能充分维持屈螺酮相关益处。

    Aqueous crystalline suspension of steroid glycoesters
    7.
    发明授权
    Aqueous crystalline suspension of steroid glycoesters 失效
    类固醇糖水溶液的水溶液悬浮液

    公开(公告)号：US4794119A

    公开(公告)日：1988-12-27

    申请号：US844642

    申请日：1986-03-27

    申请人： Paul-Eberhard Schulze ,  Bernard Acksteiner ,  Bernd Dusterberg

    发明人： Paul-Eberhard Schulze ,  Bernard Acksteiner ,  Bernd Dusterberg

    IPC分类号： A61K31/565 ,  A61K31/57 ,  C07J1/00 ,  A61K31/56

    CPC分类号： C07J1/0096

    摘要： An aqueous crystalline suspension of a 17-tertiary steroid glycoester contains a compound of Formula I ##STR1## wherein X is two hydrogen atoms or an oxygen atom,Y is two hydrogen atoms or a methylene group,R.sup.1 is hydrogen or methyl,Z is hydroxy or --O--CO--R.sup.2R.sup.2 is methyl or phenyl, and ##STR2## in the following fractions: 0-30% by weight of a particle size of 3-15 .mu.m,40-90% by weight of a particle size of 15-60 .mu.m, and20-60% by weight of a particle size of 30-100 .mu.m.Upon a one-time intramuscular injection of 30-75 mg of steroid glycoester as an aqueous crystalline suspension, a steroid level is achieved in the plasma which, over a period of 4 weeks, is adequately high and shows a uniform course.

    摘要翻译： 17-叔甾类糖酯水溶液的结晶悬浮液含有式Ⅰ化合物（Ⅰ）其中X为2个氢原子或氧原子，Y为2个氢原子或亚甲基，R1为氢或甲基， Z是羟基或-O-CO-R2R2是甲基或苯基，＆lt; IMAGE＆gt;在以下组分中：0-30重量％的粒度为3-15μm，40-90重量％ 粒径为15-60μm，粒径为30-100μm的20-60重量％。 一次肌内注射30-75mg类固醇糖酵母作为水性结晶悬浮液时，在等离子体中实现类固醇水平，其在4周的时间内足够高并且显示均匀的过程。