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    • 1. 发明申请
    • Selective cyclooxygenase-2 inhibitor patch
    • 选择性环加氧酶-2抑制剂贴片
    • US20050020658A1
    • 2005-01-27
    • US10683623
    • 2003-10-10
    • Katsuyuki InooKen-Ichi HattoriNoriko Shimizu
    • Katsuyuki InooKen-Ichi HattoriNoriko Shimizu
    • A61K9/70A61K31/415A61K31/42A61K31/18
    • A61K9/7053A61K9/7061A61K9/7076A61K31/415A61K31/42
    • A pharmaceutical composition for application to an area of skin of a subject for local and/or systemic treatment of a COX-2 mediated disorder comprises a backing sheet that is flexibly conformable to the area of skin, the backing sheet having opposing surfaces that are respectively distal and proximal to the skin when applied; and a coating on the proximal surface of the backing sheet that comprises (a) an adhesive, (b) an active agent comprising a selective COX-2 inhibitory sulfonamide drug of low water solubility, and (c) a solvent system for the active agent, wherein the active agent is in a therapeutically effective total amount and the solvent system is selected with regard to composition and amount thereof to be effective to maintain the active agent substantially completely in solubilized form. A method of local treatment of a site of pain and/or inflammation in a subject comprises applying the composition to a skin surface of the subject, preferably at a locus overlying or adjacent to the site of pain and/or inflammation, and leaving the composition in place for a time period effective to permit delivery of a locally therapeutic amount of the active agent. A method of systemic treatment of a subject having a COX-2 mediated disorder comprises applying the composition to a skin surface of the subject, and leaving the composition in place for a time period effective to permit transdermal delivery of a therapeutic amount of the active agent.
    • 用于局部和/或全身治疗COX-2介导的病症的受试者皮肤区域的药物组合物包括柔性地适应皮肤区域的背衬片,背衬片分别具有相对的表面 应用时远端和皮肤近端; 和背衬片的近侧表面上的涂层,其包含(a)粘合剂,(b)包含低水溶性的选择性COX-2抑制性磺酰胺药物的活性剂,和(c)活性剂的溶剂体系 其中活性剂处于治疗有效的总量,并且关于其组成和量的选择溶剂体系以有效地维持活性剂基本上完全为溶解形式。 局部治疗受试者的疼痛和/或炎症部位的方法包括将组合物施用于受试者的皮肤表面,优选在位于疼痛和/或炎症部位的上方或邻近的部位,并使组合物 在一段时间内有效地允许递送局部治疗量的活性剂。 具有COX-2介导的病症的受试者的全身治疗的方法包括将组合物施用于受试者的皮肤表面,并将组合物置于适当的时间段,以有效地允许经皮递送治疗量的活性剂 。
    • 4. 发明申请
    • Anti-Inflammatory Analgesic External Preparation
    • 抗炎镇痛外用药
    • US20110160194A1
    • 2011-06-30
    • US12999164
    • 2009-06-12
    • Katsuyuki InooMitsuhiro Kawada
    • Katsuyuki InooMitsuhiro Kawada
    • A61K31/5415A61K31/405A61K31/192A61K31/196A61K31/24A61K31/381A61P25/00
    • A61K9/7038A61K9/7023A61K31/165A61K31/192A61K31/245A61K31/381A61K31/405A61K31/5415A61K45/06A61K2300/00
    • An external preparation that effectively produces the anti-inflammatory analgesic effect of a non-steroidal anti-inflammatory analgesic agent, and reduces skin irritation on the application site of the preparation and has an excellent effect on pain associated with inflammation such as chronic rheumatoid arthritis, osteoarthritis, and also lumbago is provided. The external preparation includes a non-steroidal anti-inflammatory analgesic agent and oxybuprocaine or a pharmaceutically acceptable salt thereof. The external preparation includes the non-steroidal anti-inflammatory analgesic agent at a content of 0.1 to 10 wt % based on the total weight of the formulation and oxybuprocaine or a pharmaceutically acceptable salt thereof at a content of 0.01 to 60 wt % based on the total weight of the formulation. The external preparation has a dosage form as an external preparation wherein the dosage form is an ointment, a solution, a suspension, an emulsion, a lotion, a cataplasm, a tape, an aerosol, or a powder for external use.
    • 一种外用制剂,其有效地产生非甾体抗炎止痛剂的消炎镇痛作用,并减少制剂施用部位的皮肤刺激,并且对与炎症有关的疼痛具有优异的作用,例如慢性类风湿性关节炎, 骨关节炎,还有腰痛。 外用制剂包括非类固醇消炎止痛剂和羟普鲁卡因或其药学上可接受的盐。 外用制剂包括非甾体抗炎止痛剂,其含量为0.1至10重量%,基于制剂的总重量和基于以下物质的0.01-60重量%的奥布对卡因或其药学上可接受的盐 制剂的总重量。 外用制剂具有作为外用制剂的剂型,其中剂型为软膏剂,溶液剂,悬浮液剂,乳剂剂,洗剂剂,粘膜剂,胶带剂,气雾剂或外用粉剂。
    • 10. 发明授权
    • Piroxicam-containing transdermally absorbable preparation
    • 含吡罗昔康的经皮吸收制剂
    • US09119861B2
    • 2015-09-01
    • US13516014
    • 2010-12-14
    • Akiko KatayamaKatsuyuki Inoo
    • Akiko KatayamaKatsuyuki Inoo
    • A61K31/5415A61P29/00A61K31/245A61K9/70
    • A61K31/5415A61K9/7053A61K31/245A61K2300/00
    • An adhesive patch is provided in which piroxicam is formulated as a non-steroidal anti-inflammatory analgesic. In particular, provided is a piroxicam-containing transdermally absorbable adhesive patch in which an absorption promoter to piroxicam is formulated to achieve high anti-inflammatory and analgesic effects without inhibiting releasing of these drugs. The piroxicam-containing transdermally absorbable adhesive patch contains piroxicam as a medicinal component and oxybuprocaine or a pharmaceutically acceptable salt thereof as an absorption promoter. In the piroxicam-containing transdermally absorbable adhesive patch, the content of piroxicam is from 0.1% to 5% by weight to the total weight of a drug-containing plaster and the content of oxybuprocaine or the pharmaceutically acceptable salt thereof is from 1% to 30% by weight to the total weight of the drug-containing plaster.
    • 提供了一种胶粘贴剂,其中吡罗昔康被配制成非甾体抗炎止痛剂。 特别地,提供了含有喜树毒素的透皮吸收性粘合贴剂,其中将吡罗昔康的吸收促进剂配制成达到高抗炎和止痛作用而不抑制这些药物的释放。 含有喜树碱的透皮吸收性粘合剂贴剂含有作为药物成分的吡罗昔康和作为吸收促进剂的氧麻黄碱或其药学上可接受的盐。 在含有喜树毒素的透皮吸收性贴剂中,炎痛喜树碱的含量相对于含药膏体的总重量为0.1〜5重量%,并且奥布卡因或其药学上可接受的盐的含量为1〜30 相对于含药膏药的总重量的重量百分比。