Multistage preparation for contraception based on natural estrogens
    2.
    发明申请
    Multistage preparation for contraception based on natural estrogens 审中-公开
    基于天然雌激素的避孕多步骤准备

    公开(公告)号:US20050032756A1

    公开(公告)日:2005-02-10

    申请号:US10891729

    申请日:2004-07-15

    IPC分类号: A61K31/57 A61K31/56

    CPC分类号: A61K31/57 A61K2300/00

    摘要: A multistage preparation for contraception based on a combination of natural estrogen and synthetic gestogen is described. The preferred preparation contains estradiol valerate as the natural estrogen and dienogest or drospirenone as the synthetic gestogen. In comparison to conventional multistage preparations the multistage preparation according to the invention has a higher contraceptive reliability over the entire cycle, improved cyclic bleeding behavior and minimizes or prevents side effects, such as breast tension, headaches, depressive moods and libido changes.

    摘要翻译: 描述了基于天然雌激素和合成gestogen的组合的用于避孕的多级制剂。 优选的制剂包含戊酸雌二醇作为天然雌激素和依诺孕酮或屈螺酮作为合成孕酮。 与常规多级制剂相比,根据本发明的多级制剂在整个循环中具有更高的避孕可靠性,改善的循环出血行为并且最小化或预防副作用,例如乳房张力,头痛,抑郁情绪和性欲改变。

    Homogeneous preformulations containing high concentrations of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations
    3.
    发明授权
    Homogeneous preformulations containing high concentrations of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations 失效
    含有高浓度类固醇的均质预制品,用于生产低剂量固体和半固体药物制剂

    公开(公告)号:US06290931B1

    公开(公告)日:2001-09-18

    申请号:US09319802

    申请日:1999-06-10

    IPC分类号: A61K912

    摘要: A homogeneous steroid-containing preformulation for production of solid and semi-solid pharmaceutical preparations containing a uniform constant dosage of at least one steroid in a range from 0.001 to 1 percent by weight is described. This steroid-containing preformulation contains of from 0.001 to 50 percent by weight of the at least one steroid. The homogeneous steroid-containing preformulation is made by a method including dissolving the at least one steroid in a solvent to form a dispersant; dispersing an adjuvant consisting of adjuvant particles in the dispersant in a mass ratio of the adjuvant to the at least one steroid of 1:1 to 1000:1 to form a suspension; and creating a spray-mist of the suspension so as to evaporate and remove the solvent from the suspension and thus to form a dried particulate which includes steroid-containing particles. The droplets in the spray mist have a droplet diameter greater than a mean diameter of the adjuvant particles. The maximum particle size of the dried particulate forming the steroid-containing preformulation is increased by less than 30 percent in comparison to an average particle size of the adjuvant particles.

    摘要翻译: 描述了用于生产固体和半固体药物制剂的均匀类固醇预制剂,其含有0.001至1重量%范围内的至少一种类固醇的均匀恒定剂量。 该含类固醇的预制剂含有0.001至50重量%的至少一种类固醇。 通过包括将至少一种类固醇溶解在溶剂中以形成分散剂的方法制备含均匀类固醇的预配制剂; 将助剂颗粒组成的佐剂以佐剂与至少一种类固醇的质量比为1:1至1000:1分散在分散剂中以形成悬浮液; 并产生悬浮液的喷雾,从而从悬浮液中蒸发除去溶剂,从而形成包含类固醇颗粒的干燥颗粒。 喷雾中的液滴的液滴直径大于辅助颗粒的平均直径。 与佐剂颗粒的平均粒径相比,形成含类固醇的预制剂的干燥颗粒的最大粒度增加小于30%。

    Uv stable transdermal therapeutic plaster
    6.
    发明申请
    Uv stable transdermal therapeutic plaster 有权
    Uv稳定透皮治疗膏药

    公开(公告)号:US20060251707A1

    公开(公告)日:2006-11-09

    申请号:US10545826

    申请日:2004-02-04

    IPC分类号: A61K9/70

    摘要: The invention relates to a UV stable transdermal therapeutic system (TTS) consisting of a back layer, at least one matrix containing an active substance and, optionally, a withdrawal film and an UV-radiation absorber. An adhesive layer containing said UV-radiation absorber is arranged between the back layer and the matrix containing an active substance which is distant as much as possible from a surface, a separation layer is arranged between the adhesive layer containing said UV-radiation absorber and the matrix containing an active substance, which is as remote as possible from the surface which is impermeable to the active substance and UV radiation absorber. The inventive transdermal therapeutic system exhibits a high stability and is devoid of inconveniences of existing TTS containing a light-sensitive substance.

    摘要翻译: 本发明涉及由背层,至少一种含有活性物质的基质和任选的取出膜和UV-辐射吸收剂组成的UV稳定透皮治疗系统(TTS)。 含有所述紫外线吸收剂的粘合剂层被布置在背层和含有活性物质的基质之间,所述活性物质尽可能远离表面,分离层设置在包含所述紫外线吸收剂的粘合剂层和 含有活性物质的基质,该活性物质尽可能远离活性物质和紫外线吸收剂不可渗透的表面。 本发明的透皮治疗系统表现出高稳定性,并且没有含有光敏物质的现有TTS的不便。

    Transdermal delivery of hormones without the need of penetration enhancers
    7.
    发明申请
    Transdermal delivery of hormones without the need of penetration enhancers 有权
    激素的透皮递送,而不需要渗透促进剂

    公开(公告)号:US20050142175A1

    公开(公告)日:2005-06-30

    申请号:US11008642

    申请日:2004-12-10

    IPC分类号: A61K31/56 A61K9/70

    摘要: The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.

    摘要翻译: 本发明涉及包含含有低含量激素的药物含量层(如孕二烯酮)和任选的雌激素(如乙炔雌二醇)的贴剂。 在向女性施用贴剂时,在稳定状态条件下达到至少1.0ng / ml的Gestodene的血浆水平,而不需要在含药层中掺入渗透促进剂或渗透促进剂。 令人满意的激素水平也可以在至少1周的时间内达到,使补丁适用于女性避孕方法,每周施用补片的概念。

    Melatonin for the production of a peroral pulsatile form of medication
    8.
    发明授权
    Melatonin for the production of a peroral pulsatile form of medication 失效
    褪黑激素用于产生口服脉搏形式的药物

    公开(公告)号:US06214377B1

    公开(公告)日:2001-04-10

    申请号:US08567294

    申请日:1995-12-05

    IPC分类号: A61K958

    摘要: The use of melatonin for the production of peroral pulsatile forms of medications assures the safeguard of an effective level of the medical substance of melatonin in the blood, and which realize a relatively short invasion phase with a controlled delivery in comparison to conventional forms of medication containing melatonin, and which simultaneously exclude the known side effects. A control of the delivery of the melatonin is effected which is associated with the precise adaptation to the illness episodes or the pain attacks of certain illnesses, which can be treated prophylactically and therapeutically with the active agent melatonin.

    摘要翻译: 使用褪黑激素来生产口服脉搏形式的药物确保维持血液中褪黑激素的有效水平,并且与常规形式的药物相比,其具有受控递送的相对较短的入侵期 褪黑激素,同时排除已知的副作用。 对褪黑激素的输送进行控制,这与精神适应疾病发作或某些疾病的疼痛攻击有关,可以用活性剂褪黑激素进行预防和治疗。