公开(公告)号：US6027749A

公开(公告)日：2000-02-22

申请号：US981488

申请日：1998-06-03

申请人： Karin Schmidt-Gollwitzer ,  Walter Klemann

发明人： Karin Schmidt-Gollwitzer ,  Walter Klemann

IPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/585 ,  A61P5/24 ,  A61K9/20 ,  A61K31/56

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

摘要： The present invention describes a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days. This combined preparation, in the form of a monthly pack, which is used for female fertility control, permits as low as possible an oestrogen content in each individual unit dose and also has a low total hormone content per cycle of administration, with high contraceptive reliability, low incidence of follicle development, and satisfactory cycle control with reliable avoidance of intermediate bleeding as well as undesired side effects.

摘要翻译： PCT No.PCT / DE96 / 01192 Sec。 371日期1998年6月3日第 102（e）1998年6月3日PCT PCT 1996年6月27日PCT公布。 第WO97 / 01342号公报 日期1997年1月16日本发明描述了含有至少30个每日单位剂量的激素避孕的两阶段药物组合制剂，其制备在其第一阶段包含作为激素活性成分的雌激素制剂的组合， 至少足以抑制排卵的孕激素制剂，单阶段形式的孕激素制剂，并且在第二阶段中仅包含作为激素活性成分的雌激素制剂，其中第一阶段至少包含25和最多77天离散 或连续单位剂量，第二阶段包括5,6或7天每日离散或连续的单位剂量，并且其中每日单位的总数等于所需周期的总天数至少为30，最大值为 84天。 用于女性生殖力控制的每月包装形式的组合制剂允许尽可能低的每个单位剂量的雌激素含量，并且每个给药周期的总荷尔蒙含量低，具有高避孕可靠性 ，卵泡发育发生率低，循环控制令人满意，可以避免中度出血以及不良副作用。

公开(公告)号：US06312722B1

公开(公告)日：2001-11-06

申请号：US09476333

申请日：2000-01-03

申请人： Karin Schmidt-Gollwitzer ,  Walter Klemann

发明人： Karin Schmidt-Gollwitzer ,  Walter Klemann

IPC分类号： A61K920

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/585 ,  Y10S514/843 ,  A61K2300/00

摘要： The present invention describes a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days. This combined preparation, in the form of a monthly pack, which is used for female fertility control, permits as low as possible an oestrogen content in each individual unit dose and also has a low total hormone content per cycle of administration, with high contraceptive reliability, low incidence of follicle development, and satisfactory cycle control with reliable avoidance of intermediate bleeding as well as undesired side effects.

摘要翻译： 本发明描述了一种用于激素避孕的两阶段药物组合制剂，其包含至少30个每日单位剂量，其制备在其第一阶段中包含作为激素活性成分的雌激素制剂的组合，并且至少为至少 足以抑制排卵，单阶段形式的孕激素制剂，并且在第二阶段中仅包含作为激素活性成分的雌激素制剂，其中第一阶段包含最少25次和最多77次每日离散或连续的单位剂量，以及 第二阶段包括5,6或7天每日离散或连续的单位剂量，并且其中每日单位的总数等于所需周期的总天数最少为30天，最多为84天。 用于女性生殖力控制的每月包装形式的组合制剂允许尽可能低的每个单位剂量的雌激素含量，并且每个给药周期的总荷尔蒙含量低，具有高避孕可靠性 ，卵泡发育发生率低，循环控制令人满意，可以避免中度出血以及不良副作用。

公开(公告)号：US6143754A

公开(公告)日：2000-11-07

申请号：US273485

申请日：1999-03-22

申请人： Kristof Chwalisz ,  Klaus Stockemann ,  Karin Schmidt-Gollwitzer ,  Walter Klemann

发明人： Kristof Chwalisz ,  Klaus Stockemann ,  Karin Schmidt-Gollwitzer ,  Walter Klemann

IPC分类号： A61K31/57 ,  A61K31/00 ,  A61K31/575 ,  A61K31/58 ,  A61P15/18 ,  C07J9/00 ,  A61K31/435 ,  A61K31/13

CPC分类号： A61K31/567 ,  A61K31/00 ,  A61K31/569 ,  A61K31/575 ,  A61K31/58 ,  Y10S514/843

摘要： This invention describes the novel use of dissociated competitive progesterone antagonists for the production of a pharmaceutical agent for demand-oriented female birth control (pill on demand), which can be used regardless of the point in the menstrual cycle, in a dosage unit that is to be administered on a one-time basis, whose dosage is below the ovulation-inhibiting dosage.

摘要翻译： 本发明描述了分离的竞争性孕酮拮抗剂在生产用于需求导向的女性避孕（药物需求））的药剂中的新用途，其可以在月经周期中的任何一点使用，剂量单位是 一次性施用，其剂量低于排卵抑制剂量。