Compositions of estrogen-cyclodextrin complexes
    1.
    发明申请
    Compositions of estrogen-cyclodextrin complexes 有权
    雌激素 - 环糊精复合物的组成

    公开(公告)号:US20070093451A1

    公开(公告)日:2007-04-26

    申请号:US11607919

    申请日:2006-12-04

    IPC分类号: A61K31/724

    摘要: Pharmaceutical compositions comprising low doses of sensitive complexes between an estrogen and a cyclodextrin are provided with improved stability. In specific embodiments the composition comprises a complex between ethinyl estradiol and β-cyclodextrin in a granulate preparation and in yet another embodiment the composition comprises a limited amount of polyvinylpyrrolidone since this excipient was found to degrade ethinyl estradiol. Furthermore, a method for improving the stability of an estrogen in a composition and for manufacturing such a stable composition is provided. Essentially, the granulate preparation are manufactured under careful control of the relative humidity.

    摘要翻译: 提供包含雌激素和环糊精之间的低剂量灵敏复合物的药物组合物具有改进的稳定性。 在具体实施方案中,组合物包含颗粒制剂中乙炔雌二醇和β-环糊精之间的复合物,在另一个实施方案中,该组合物包含有限量的聚乙烯吡咯烷酮,因为发现该赋形剂降解乙炔雌二醇。 此外,提供了用于提高组合物中雌激素的稳定性和制造这种稳定组合物的方法。 基本上,在仔细控制相对湿度的情况下制造颗粒制剂。

    Compositions of estrogen-cyclodextrin complexes
    4.
    发明授权
    Compositions of estrogen-cyclodextrin complexes 有权
    雌激素 - 环糊精复合物的组成

    公开(公告)号:US07569557B2

    公开(公告)日:2009-08-04

    申请号:US11607919

    申请日:2006-12-04

    IPC分类号: A01N43/04 A61K31/715

    摘要: Pharmaceutical compositions comprising low doses of sensitive complexes between an estrogen and a cyclodextrin are provided with improved stability. In specific embodiments the composition comprises a complex between ethinyl estradiol and β-cyclodextrin in a granulate preparation and in yet another embodiment the composition comprises a limited amount of polyvinylpyrrolidone since this excipient was found to degrade ethinyl estradiol. Furthermore, a method for improving the stability of an estrogen in a composition and for manufacturing such a stable composition is provided. Essentially, the granulate preparation are manufactured under careful control of the relative humidity.

    摘要翻译: 提供包含雌激素和环糊精之间的低剂量灵敏复合物的药物组合物具有改进的稳定性。 在具体实施方案中,组合物包含颗粒制剂中乙炔雌二醇和β-环糊精之间的复合物,在另一个实施方案中,该组合物包含有限量的聚乙烯吡咯烷酮,因为发现该赋形剂降解乙炔雌二醇。 此外,提供了用于提高组合物中雌激素的稳定性和制造这种稳定组合物的方法。 基本上,在仔细控制相对湿度的情况下制造颗粒制剂。

    DROSPIRENONE FOR HORMONE REPLACEMENT THERAPY
    8.
    发明申请
    DROSPIRENONE FOR HORMONE REPLACEMENT THERAPY 审中-公开
    用于激素替代治疗的DROSPIRENONE

    公开(公告)号:US20120220556A1

    公开(公告)日:2012-08-30

    申请号:US13356005

    申请日:2012-01-23

    摘要: A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6β,7β;15β;16β-dimethylene-3-oxo-17α-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.

    摘要翻译: 一种药物组合物,其包含作为第一活性成分的雌激素,例如雌二醇或戊酸雌二醇,其用量足以治疗与女性内源性雌激素水平不足相关的疾病和症状,并且作为第二活性成分6& ; 16和bgr-二亚甲基-3-氧代-17α-前 - 4-烯-21,17-碳内酯(屈螺酮,DRSP)足以保护子宫内膜免受雌激素的不利影响,其中包括治疗 绝经期,绝经期和绝经后妇女。 该组合物可用于激素替代疗法,并且可以作为多阶段药物制剂施用。 这种联合疗法可以包括DRSP和雌激素的连续,顺序或中断给药或其组合,每种任选以微粉化形式。

    DROSPIRENONE FOR HORMONE REPLACEMENT THERAPY
    9.
    发明申请
    DROSPIRENONE FOR HORMONE REPLACEMENT THERAPY 审中-公开
    用于激素替代治疗的DROSPIRENONE

    公开(公告)号:US20100093679A1

    公开(公告)日:2010-04-15

    申请号:US12640578

    申请日:2009-12-17

    IPC分类号: A61K31/56 A61P15/00

    摘要: A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6β,7β;15β;16β-dimethylene-3-oxo-17α-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.

    摘要翻译: 一种药物组合物,其包含作为第一活性成分的雌激素,例如雌二醇或戊酸雌二醇,其用量足以治疗与女性内源性雌激素水平不足相关的疾病和症状,并且作为第二活性成分6& ; 16和bgr-二亚甲基-3-氧代-17α-前 - 4-烯-21,17-碳内酯(屈螺酮,DRSP)足以保护子宫内膜免受雌激素的不利影响,其中包括治疗 绝经期,绝经期和绝经后妇女。 该组合物可用于激素替代疗法,并且可以作为多阶段药物制剂施用。 这种联合疗法可以包括DRSP和雌激素的连续,顺序或中断给药或其组合,每种任选以微粉化形式。

    Pharmaceutical composition for use as a contraceptive

    公开(公告)号:US20060058272A1

    公开(公告)日:2006-03-16

    申请号:US11266395

    申请日:2005-11-04

    IPC分类号: A61K31/56

    摘要: A pharmaceutical composition comprises, as a first active agent, 6β,7β;15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone (drospirenone) in an amount corresponding to a daily dosage, on administration of the composition, of from about 2 mg to about 4 mg, and, as a second active agent, 17α-ethinylestradiol (ethinylestradiol) in an amount corresponding to a daily dosage of from about 0.01 mg to about 0.05 mg, together with one or more pharmaceutically acceptable carriers or excipients. In a specific embodiment, the composition consists of a number of separately packaged and individually removable daily dosage units placed in a packaging unit and intended for oral administration for a period of at least 21 consecutive days, wherein said daily dosage units comprises the combination of drospirenone and ethinylestradiol. The composition may further comprise 7 or less daily dosage units containing no active agent or containing ethinylestradiol alone.