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1. 发明授权

US6133251A Combination compound for contraception based on natural estrogen 失效
标题翻译：基于天然雌激素的避孕组合化合物
公开(公告)号：US6133251A
公开(公告)日：2000-10-17
申请号：US738314
申请日：1996-10-25
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
IPC分类号： A61K31/565 , A61K31/57 , A61P15/00 , A61P15/18 , C07J1/00 , C07J7/00 , A61K31/56
CPC分类号： A61K31/57 , Y10S514/843
摘要： The combination preparation for contraception includes a first stage of 2 to 4 first stage daily dosage portions, a second stage of two groups of second stage daily dosage portions, a third stage of 2 to 4 third stage daily dosage portions and an additional stage of 2 to 4 additional stage daily dosage portions. The first stage daily dosage portion is an effective amount of natural estrogen, the second stage daily dosage portion is an effective amount of a combination of natural estrogen and natural or synthetic gestogen, the third stage daily dosage portion is another effective amount of natural estrogen and an additional stage daily dosage portion consists of a placebo. The first group of the second stage consists of 3 to 5 daily dosage portions and the second group, 13 to 17 daily dosage portions. More of the gestogen is included in the effective amount in the second group of the second stage than in the first group. The effective amount of the natural estrogen is constant in both the first and third stages, but smaller in the third stage than in the first stage.
摘要翻译：用于避孕的组合制剂包括第一阶段的2至4个第一阶段每日剂量部分，第二阶段的两组第二阶段日剂量部分，第三阶段的2至4个第三阶段每日剂量部分和另外的阶段2 至4个额外的阶段日剂量部分。第一阶段日剂量是天然雌激素的有效量，第二阶段日剂量是天然雌激素和天然或合成gestogen的组合的有效量，第三阶段日剂量是另一有效量的天然雌激素，额外的阶段每日剂量部分由安慰剂组成。第一组第一组由3〜5个日剂量组成，第二组为每日13〜17次。第二组的第二组中有更多的gestogen包含在第一组中。天然雌激素的有效量在第一和第三阶段都是恒定的，但在第三阶段中比在第一阶段更小。

2. 发明授权

US06884793B2 Combination preparation for contraception based on natural estrogens 失效
标题翻译：基于天然雌激素的避孕组合制剂
公开(公告)号：US06884793B2
公开(公告)日：2005-04-26
申请号：US09950915
申请日：2001-09-12
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
IPC分类号： A61K31/565 , A61K31/57 , A61P15/00 , A61P15/18 , C07J1/00 , C07J7/00 , A61K33/56
CPC分类号： A61K31/57 , Y10S514/843 , A61K31/565 , A61K2300/00
摘要： The combination preparation for contraception includes from 2 to 4 first stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient, from 16 to 22 second stage daily dosage portions each including an effective amount of a combination of at least one natural estrogen and at least one natural or synthetic gestogen as active ingredient; from 2 to 4 third stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient; and from 2 to 4 final stage daily dosage portions containing a pharmaceutically acceptable placebo. The estrogen may be estradiol, an estradiol compound that is metabolized to estradiol when taken into the body, a conjugated equine estrogen or a phytoestrogen. The natural or synthetic gestogen can be natural progesterone or a synthetic gestogens, such as medroxyprogesterone acetate.
摘要翻译：用于避孕的组合制剂包括2至4个第一阶段每日剂量部分，每个剂量部分包含有效量的至少一种天然雌激素作为唯一活性成分，16至22个第二阶段日剂量部分，每个包含有效量的组合至少一种天然雌激素和至少一种天然或合成的Gestogen作为活性成分; 2至4个第三阶段每日剂量部分，每个包含有效量的至少一种天然雌激素作为唯一活性成分; 和含有药学上可接受的安慰剂的2至4个最终阶段每日剂量部分。雌激素可以是雌二醇，当被摄入体内时被代谢为雌二醇的雌二醇化合物，共轭马雌激素或植物雌激素。天然或合成的gestogen可以是天然孕酮或合成的gestogens，如醋酸甲羟孕酮。

3. 发明申请

US20050032756A1 Multistage preparation for contraception based on natural estrogens 审中-公开
标题翻译：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
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Oster Wald
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Oster Wald
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。

4. 发明授权

US06977083B1 Bioadhesive tablet containing testosterone/testosterone ester mixtures and method for producing a predetermined testosterone time-release profile with same 失效
标题翻译：含有睾酮/睾酮酯混合物的生物粘附片剂和用于产生具有相同的预定睾酮时间释放特性的方法
公开(公告)号：US06977083B1
公开(公告)日：2005-12-20
申请号：US09806639
申请日：1999-09-30
申请人： Doris Huebler , Guenter Kaufmann , Michael Oettel , Holger Zimmermann , Michael Dittgen , Sabine Fricke , Manfred Boese , Ralf Ladwig , Sven Claussen , Carsten Timpe
发明人： Doris Huebler , Guenter Kaufmann , Michael Oettel , Holger Zimmermann , Michael Dittgen , Sabine Fricke , Manfred Boese , Ralf Ladwig , Sven Claussen , Carsten Timpe
IPC分类号： A61F13/00 , A61K9/00
CPC分类号： A61K9/006
摘要： The method of making a bioadhesive tablet for controlling testosterone blood level, especially in elderly men suffering from partial androgen deficiency, includes spray-drying an alcoholic solution or suspension of testosterone and at least one testosterone ester, preferably in a ratio of 1:10 to 1:1.5, separately or together, with an organic polymer and optionally one or more auxiliary ingredient to form an active ingredient premix. Then various other auxiliary ingredients are mixed, as needed, with the active ingredient premix to form the bioadhesive tablet with an active ingredient layer and an adhesive layer. The active ingredient layer contains an effective amount of the active ingredient premix. The adhesive layer includes auxiliary ingredients including the bioadhesive polymer. The bioadhesive tablet may be buccally administered to provide a predetermined timed release profile of testosterone, advantageously varying according to a circadian rhythm.
摘要翻译：制备用于控制睾酮血液水平的生物粘附片剂的方法，特别是在患有部分雄激素缺乏症的老年男性中，包括将睾酮和至少一种睾酮酯的醇溶液或悬浮液喷雾干燥，优选1:10至 1：1.5，分别或一起与有机聚合物和任选的一种或多种辅助成分形成活性成分预混物。然后根据需要将各种其它辅助成分与活性成分预混合物混合以形成具有活性成分层和粘合剂层的生物粘附片剂。活性成分层含有有效量的活性成分预混物。粘合层包括辅助成分，包括生物粘附聚合物。生物粘附片剂可以经口给药以提供睾酮的预定定时释放曲线，其有利地根据昼夜节律改变。

5. 发明授权

US06214377B1 Melatonin for the production of a peroral pulsatile form of medication 失效
标题翻译：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
申请人： Michael Dittgen , Sabine Fricke , Thomas Gräser , Hermann Osterwald , Michael Oettel , Theodor Hermann Lippert
发明人： Michael Dittgen , Sabine Fricke , Thomas Gräser , Hermann Osterwald , Michael Oettel , Theodor Hermann Lippert
IPC分类号： A61K958
CPC分类号： A61K9/4875 , A61K9/4858 , A61K31/4045
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。

6. 发明授权

US6117450A Method of making a perorally administered solid drug with controlled effective ingredient delivery 失效
标题翻译：制备具有受控有效成分递送的经口施用的固体药物的方法
公开(公告)号：US6117450A
公开(公告)日：2000-09-12
申请号：US65863
申请日：1998-04-24
申请人： Michael Dittgen , Sabine Fricke , Carsten Timpe , Hagen Gerecke , Annette Eichardt
发明人： Michael Dittgen , Sabine Fricke , Carsten Timpe , Hagen Gerecke , Annette Eichardt
IPC分类号： A61K9/22 , A61K9/48 , A61K9/52 , A61P43/00 , A61K9/26 , A61K9/28
CPC分类号： A61K9/4808
摘要： The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.
摘要翻译：制备具有受控制的有效成分递送用于口服给药的固体药物的方法包括选择预定数量的四种压缩组合物中的至少三种，其包含由有效成分和/或有效成分组合的释放曲线限定的有效成分或有效成分组合。固体药物或药物制剂根据已知的方法形成，只需要较小的装置费用和最少的时间。通过该方法制备经口施用的固体药物，其可以提供有效成分或有效成分组合的广泛变化的药学需要的释放曲线，例如延迟释放，均匀保持的释放或脉动释放，以适应特殊的节律。

7. 发明授权

US06303137B1 Injectable implant 失效
标题翻译：可注射植入物
公开(公告)号：US06303137B1
公开(公告)日：2001-10-16
申请号：US09341206
申请日：1999-08-16
申请人： Michael Dittgen , Sabine Fricke , Hagen Gerecke , Ines-Patricia Möller , Christoph Völkel
发明人： Michael Dittgen , Sabine Fricke , Hagen Gerecke , Ines-Patricia Möller , Christoph Völkel
IPC分类号： A61F202
CPC分类号： A61K9/0024 , A61K47/10 , A61K47/34 , A61L27/26 , A61L27/58 , A61L27/54 , A61L27/50 , C08L67/04 , C08L71/02
摘要： This invention relates to an in-situ implant that can be produced by placing a sterile, injectable, and water-insoluble complex from a biodegradable polymer and a biocompatible polyether with functional end-groups in the organism, and coagulating them under the influence of the body fluid. This coagulate may optionally contain at least one bioactive substance selected from the group of hormones, immunomodulators, immunosuppressants, antibiotics, cytostatics, diuretics, gastro-intestinal agents, analgesics, local anaesthetics and/or neuropharmacological agents.
摘要翻译：本发明涉及一种原位植入物，其可以通过将生物可降解聚合物和具有功能性端基的生物相容性聚醚与生物相容性聚合物置于无菌，可注射和水不溶性复合物的生物体中，并在其影响下凝结体液。该凝结物可以任选地含有至少一种选自激素，免疫调节剂，免疫抑制剂，抗生素，细胞抑制剂，利尿剂，胃肠药，止痛剂，局部麻醉剂和/或神经药物剂的生物活性物质。

8. 发明授权

US06238284B1 Transdermal compositions with enhanced skin penetration properties 有权
标题翻译：具有增强皮肤渗透性能的透皮组合物
公开(公告)号：US06238284B1
公开(公告)日：2001-05-29
申请号：US09341416
申请日：1999-09-10
申请人： Michael Dittgen , Sabine Fricke , Christoph Völkel , Kathrin Ahrens , Hagen Gerecke , Kai Köpke
发明人： Michael Dittgen , Sabine Fricke , Christoph Völkel , Kathrin Ahrens , Hagen Gerecke , Kai Köpke
IPC分类号： C09J502
CPC分类号： A61K9/7038 , A61K9/145 , A61K9/7023
摘要： The invention relates to a transdermal therapeutic system for application to the skin and/or mucosa consisting of at least one active substance in the form of a solid dispersion in combination with at least one destructuring agent and/or at least one structuring agent in a common matrix.
摘要翻译：本发明涉及一种用于皮肤和/或粘膜的透皮治疗系统，其由至少一种固体分散体形式的活性物质与至少一种破坏剂和/或共同的至少一种结构化试剂组合矩阵。

9. 发明授权

US06225299B1 Hormonal agent for skin treatment 失效
标题翻译：皮肤治疗激素剂
公开(公告)号：US06225299B1
公开(公告)日：2001-05-01
申请号：US09219660
申请日：1998-12-23
申请人： Siegfried Golbs , Michael Oettel , Michael Dittgen , Thomas Graser , Christoph Luderschmidt
发明人： Siegfried Golbs , Michael Oettel , Michael Dittgen , Thomas Graser , Christoph Luderschmidt
IPC分类号： A61K3156
CPC分类号： A61K31/56 , A61K8/63 , A61Q7/00 , Y10S514/859 , Y10S514/864
摘要： The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin. The pharmaceutical preparation including the dienogest and conventional dermatologically acceptable carrier and auxiliary substances in the described galenic formulation advantageously provides a drastic reduction in androstandiol glucuronide and moderate androgen receptor blockage without passing through the skin barrier so that systemic effects including side reactions are substantially prevented.
摘要翻译：药物组合物，特别是用于治疗皮脂溢，皮肤寻常痤疮和阴道调理性脱发的皮肤，含有激素剂，包括睾酮，依那诺或二烯酸和雌激素的组合作为活性成分。用于治疗这种类型皮肤病症的方法包括局部应用组合物，其包括引起明显的抑制作用的替奈格明，葡萄糖醛酸葡萄糖醛酸葡聚糖和葡萄糖醛酸葡聚糖的剧烈降低以及雄激素受体位点的适度竞争性阻断。描述了限制和/或防止活性成分渗透皮肤的Galenic制剂。在所述盖仑制剂中包含地那烯酸和常规皮肤病学可接受的载体和辅助物质的药物制剂有利地提供了葡萄糖醛酸葡萄糖醛酸葡萄糖苷和中和雄激素受体阻断物的急剧降低，而不会通过皮肤屏障，从而基本上防止包括副反应的全身效应。

10. 发明授权

US5910493A Hormonal agent for skin treatment 失效
标题翻译：皮肤治疗激素剂
公开(公告)号：US5910493A
公开(公告)日：1999-06-08
申请号：US714463
申请日：1996-09-16
申请人： Siegfried Golbs , Michael Oettel , Michael Dittgen , Thomas Graser , Christoph Luderschmidt
发明人： Siegfried Golbs , Michael Oettel , Michael Dittgen , Thomas Graser , Christoph Luderschmidt
IPC分类号： A61K8/63 , A61Q5/00 , A61Q7/00 , A61Q19/00 , A61K31/56
CPC分类号： A61K31/567 , A61K8/63 , A61Q19/00 , A61Q5/00 , A61Q7/00 , Y10S514/859 , Y10S514/864
摘要： The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin. The pharmaceutical preparation including the dienogest and conventional dermatologically acceptable carrier and auxiliary substances in the described galenic formulation advantageously provides a drastic reduction in androstandiol glucuronide and moderate androgen receptor blockage without passing through the skin barrier so that systemic effects including side reactions are substantially prevented.
摘要翻译：药物组合物，特别是用于治疗皮脂溢，皮肤寻常痤疮和阴道调理性脱发的皮肤，含有激素剂，包括睾酮，依那诺或二烯酸和雌激素的组合作为活性成分。用于治疗这种类型皮肤病症的方法包括局部应用组合物，其包括引起明显的抑制作用的替奈格明，葡萄糖醛酸葡萄糖醛酸葡聚糖和葡萄糖醛酸葡聚糖的剧烈降低以及雄激素受体位点的适度竞争性阻断。描述了限制和/或防止活性成分渗透皮肤的Galenic制剂。在所述盖仑制剂中包含地那烯酸和常规皮肤病学可接受的载体和辅助物质的药物制剂有利地提供了葡萄糖醛酸葡萄糖醛酸葡萄糖苷和中和雄激素受体阻断物的急剧降低，而不会通过皮肤屏障，从而基本上防止包括副反应的全身效应。

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