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    • 2. 发明授权
    • Borderline active dosage forms of beta blockers
    • β受体阻滞剂的边界活性剂型
    • US5496560A
    • 1996-03-05
    • US322420
    • 1994-10-13
    • Rainer K. Liedtke
    • Rainer K. Liedtke
    • A61K9/70A61F13/00A61K9/20
    • A61K9/7023Y10S514/821
    • For short-term therapy of transient functional cardiovascular symptoms, borderline active dosage forms of beta blockers are used which produce in the body only the borderline active concentrations of active ingredient which produce no significant changes in the physiological values in the cardiovascular system under resting conditions for the respective specific beta blocker used and significantly reduce adrenergically induced transient stimulation effects. Oral, transdermal, or topical dosage forms are particularly advantageous. A differentiated therapy of functional symptoms which does not exist with the customary dosage forms of beta blockers designed for long-term therapies is possible. Both the quality of life and the risk-benefit ratio of the beta blockers are improved. The duration of the therapy also does not have to be extended beyond the symptomatically required scale since no rebound danger exists after withdrawal. As an additional and now indication, this also permits the short-term use for the primary therapy of sleep disturbances, within the framework of vegetative syndromes, in particular, within the framework of postmenopausal symptoms.
    • 对于短暂治疗短暂功能性心血管症状,使用β阻断剂的边界活性剂型,其在体内仅产生活性成分的边界活性浓度,其在静息条件下在心血管系统中的生理值没有显着变化 各自的特异性β受体阻滞剂使用并显着减少肾上腺素诱导的瞬时刺激作用。 口服,透皮或局部剂型是特别有利的。 对于长期治疗设计的β阻滞剂的常规剂型不存在功能性症状的分化治疗是可能的。 β受体阻滞剂的生活质量和风险利益比均有所改善。 治疗的持续时间也不必超出症状所需的量表,因为撤回后不存在反弹危险。 作为补充和现在的指示,这也允许在植物综合征的框架内,特别是在绝经后症状的框架内,短期使用睡眠障碍的主要疗法。
    • 5. 发明授权
    • Single dosage semi-solid topical pharmaceutical forms for transdermal
therapy
    • 用于经皮治疗的单次剂量半固体局部药物形式
    • US5686112A
    • 1997-11-11
    • US569958
    • 1995-12-20
    • Rainer K. Liedtke
    • Rainer K. Liedtke
    • A61J1/03A61J1/00A61K9/00A61K9/06A61K9/70A61M35/00B65D75/34A61K9/14
    • A61M35/00A61K9/06B65D75/327B65D2575/3245
    • To improve the efficacy and tolerability of customary topical applications for transdermal systemically acting pharmaceutical substances, single dosage topical pharmaceutical forms which are therapeutically exactly ready-to-administer are formed from suitable semi-solid pharmaceutical forms. The topical single doses are specified pharmaceutically with respect to their dose, their topical spreading behaviour and their permeation properties. Several of the topically ready-to-administer single doses are in this case accommodated in a common commercial packaging container. Complex treatments can be developed by means of different individual dosages or alternatively active compound combinations. As pharmacological active compounds, steroids, peptides, various analgesics, local anaesthetics and non-steroidal antirheumatics are employed in particular. The single dosage topical pharmaceutical form is a safe, easy to administer and inexpensive application form which makes possible a more exact topical therapy for systemic administrations than could previously be achieved using conventional topical administration forms.
    • 为了改善常规局部应用于经皮系统作用的药物物质的功效和耐受性,治疗上准确给药的单剂量局部药物形式由合适的半固体药物形式形成。 关于其剂量,其局部铺展行为及其渗透性质,局部单剂量是药学上规定的。 在这种情况下,几种局部准备施用的单次剂量容纳在共同的商业包装容器中。 可以通过不同的单独剂量或者活性化合物组合来开发复杂的治疗。 作为药理活性化合物,特别使用类固醇,肽,各种止痛剂,局部麻醉剂和非甾体抗风湿剂。 单剂量局部药物形式是安全,易于施用和廉价的应用形式,其使得可以比以前可以使用常规局部给药形式实现更全面的局部治疗用于全身给药。
    • 7. 发明授权
    • Oral lipid medicinal composition
    • 口服药物组合物
    • US5120710A
    • 1992-06-09
    • US524787
    • 1990-05-17
    • Rainer K. Liedtke
    • Rainer K. Liedtke
    • A61K9/40A61K9/48A61K9/66A61K31/545A61K31/56A61K31/565A61K31/57A61K38/00A61K38/04A61K38/22A61K38/23A61K38/28A61K47/44
    • A61K9/4858A61K38/28A61K9/485
    • To improve the absorption of actve ingredients, which are not adequately bio-available on oral administration, an oral lipid medicinal composition is formed by combining a semi-solid, lipophilic component with a solid, water-soluble component. The semi-solid component is a homogeneous lipid mixture that exists as a hard fat with thermally reversible fat/liquid melting property, at least 95% of which is present in the liquid aggregate state below the body temperature of 37.degree. C. and comprises monoacyl-, diacyl-, and triacylglycerides of saturated vegetable fatty acids with chain lengths ranging from 6 to 18 carbon atoms, preferably comprising a mixture of 40 to 60% monoacyl- and diacylglycerides and 40 to 60% triacylglycerides, in which the active ingredients are either dissolved, suspended or emulsified. The solid component comprises a non-diffusible, water-soluble shell which is not chemically bonded to the lipid compound and envelops the entire lipid compound and is preferably made of gelatin or starch. The use of protease inhibitors in the lipid mixture can improve the permeation conditions for peptides and proteins. The use of highly disperse silicon dioxide can stabilize the suspension formulations. Physical-chemical and biochemical aspects of the oral lipid medicinal form yield improvements for the absorption of drugs that are not adequately bio-available on oral administration.
    • 为了改善在口服给药时不能充分生物利用的作用成分的吸收,通过将半固体,亲脂性成分与固体,水溶性成分组合形成口服脂质药物组合物。 半固体组分是均匀的脂质混合物,其以具有热可逆脂肪/液体熔融性质的硬脂肪存在,其至少95%以低于体温37℃的液体聚集状态存在,并且包含单酰基 具有6-18个碳原子的饱和植物脂肪酸的二酰基和三酰基甘油酯,优选包含40至60%的单酰基和二酰基甘油酯和40至60%的三酰基甘油酯的混合物,其中活性成分是 溶解,悬浮或乳化。 固体组分包括不与脂质化合物化学键合并且包封整个脂质化合物的非扩散性水溶性壳,并且优选由明胶或淀粉制成。 在脂质混合物中使用蛋白酶抑制剂可以改善肽和蛋白质的渗透条件。 使用高度分散的二氧化硅可以稳定悬浮液配方。 口服脂质药物形式的物理化学和生物化学方面产生改善,用于吸收在口服给药时不能充分生物利用的药物。