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    • 11. 发明申请
    • TRANSDERMAL PHARMACEUTICAL PREPARATION
    • 超声波药物制备
    • US20090148504A1
    • 2009-06-11
    • US12359073
    • 2009-01-23
    • Fumio KamiyamaYing-shu Quan
    • Fumio KamiyamaYing-shu Quan
    • A61F13/02A61K31/4468
    • A61K9/7053A61K9/7061A61K31/4468
    • A percutaneous administration type pharmaceutical preparation in tape form comprising a flexible backing, which is not permeable by the active ingredient, and an adhesive base layer formed on said flexible backing; said adhesive base layer consisting essentially of an adhesive base material, ingredients, and an active ingredient, wherein said adhesive base is a copolymer containing one or more (meth) alkyl acrylate monomers and one or more monomers copolymerizable with the (a) monomer selected from the group of unsaturated ethylenically unsaturated monomers, and said ingredients are diethylene glycol monocetyl ether, octanoic acid and/or oleic acid, lauric acid diethanolamide, polyvinylpyrollidone; and said active ingredient is fentanyl.
    • 一种胶带形式的经皮给药型药物制剂,其包含不能被活性成分渗透的柔性背衬和形成在所述柔性背衬上的粘合剂基层; 所述粘合剂基层基本上由粘合剂基材,成分和活性成分组成,其中所述粘合剂基是含有一种或多种丙烯酸(甲基)丙烯酸酯单体和一种或多种可与(a)单体共聚的单体的共聚物,所述单体选自 不饱和烯属不饱和单体组,所述成分是二甘醇单乙醚,辛酸和/或油酸,月桂酸二乙醇酰胺,聚乙烯吡咯烷酮; 所述活性成分是芬太尼。
    • 12. 发明申请
    • TRANSDERMALLY ABSORPTIVE PREPARATION
    • 超吸收制剂
    • US20100266670A1
    • 2010-10-21
    • US12746594
    • 2008-12-09
    • Akira YamamotoToshiyasu SakaneHidemasa KatsumiFumio KamiyamaYing-shu Quan
    • Akira YamamotoToshiyasu SakaneHidemasa KatsumiFumio KamiyamaYing-shu Quan
    • A61K9/70A61K31/663A61P19/10A61P3/14
    • A61K31/663A61K9/7061A61K47/10A61K47/28A61K47/32
    • This invention is to provide a transdermal administration type pharmaceutical preparation which has better transdermal absorptivity, safety and practical application for treatment of bone calcium metabolic diseases, such as high calcium in blood which resulted from osteoporosis, osteitis deformans and malignant tumors.A percutaneous administration type pharmaceutical preparation in tape form comprising a flexible backing, which is not permeable by the active ingredient, and an adhesive base layer formed on said flexible backing; said adhesive base layer consisting essentially of an adhesive base material of acrylic copolymer, polyhydric alcohol and bisphosphonate or its derivatives, wherein the bisphosphonate or its derivatives are in their therapeutic dose, adhesive base material and polyhydric alcohol in a concentration ratio of 100:150 to 600 by weight; said acrylic copolymer are copolymerized by acrylic acid, 2-ethylhexyl acrylate and polar monomer (except for acrylic acid) in the concentration ratio of 50 to 88%:8 to 40%:1 to 40% by weight respectively. PEG modify and antioxidants are also applicable to reduce the skin stimulation.
    • 本发明提供一种透皮给药型药物制剂,其具有较好的经皮吸收性,安全性和实际应用,用于治疗由骨质疏松症,变形性骨畸形和恶性肿瘤引起的骨钙代谢疾病如血钙高。 一种胶带形式的经皮给药型药物制剂,其包含不能被活性成分渗透的柔性背衬和形成在所述柔性背衬上的粘合剂基层; 所述粘合剂基层主要由丙烯酸共聚物,多元醇和二膦酸盐或其衍生物的粘合剂基材组成,其中双膦酸盐或其衍生物的治疗剂量为粘合剂基材和多元醇,浓度比为100:50至 600重量份; 所述丙烯酸共聚物由丙烯酸,丙烯酸2-乙基己酯和极性单体(丙烯酸除外)以50〜88%的浓度比分别为8〜40%:1〜40重量%。 PEG修饰和抗氧化剂也适用于减少皮肤刺激。
    • 14. 发明申请
    • PERCUTANEOUSLY ABSORBABLE PREPARATION, PROCESS FOR PRODUCTION THEREOF AND METHOD FOR PERCUTANEOUS ABSORPTION
    • 非常可吸收的制备方法,其生产方法和经济吸收方法
    • US20100113348A1
    • 2010-05-06
    • US12529175
    • 2008-02-26
    • Fumio KamiyamaYing-shu Quan
    • Fumio KamiyamaYing-shu Quan
    • A61K38/23A61K38/22A61P43/00
    • A61K45/06A61K9/7061A61K31/00
    • This invention is to provide a transdermal permeation preparation which includes a concentrated transdermal active ingredient laminate and exhibits high transdermal permeation effect; and a method for producing the preparationA transdermal permeation preparation which comprises a base material which is a hydrophilic macromolecule which can swell after absorbing the water and/or water-containing alcohol and comprises a transdermal active ingredient which is in a molecular weight higher than 1000 Dalton and can dissolve or suspend in water and/or water-containing alcohol laminated on the surface of the base material; and a method for producing the transdermal permeation preparation wherein the transdermal active ingredient of a molecular weigh higher than 1000 Dalton is dissolved or suspended in water and/or water-containing alcohol to form an aqueous solution or suspension and the said aqueous solution or suspension is coated on the surface of base materials which are hydrophilic macromolecules which can swell after absorbing the water or e water-containing alcohol as a result of absorption of the water or the water-containing alcohol in the base material, thereby forming a layer containing the transdermal active ingredient in a concentrated state on the surface of the base material.
    • 本发明提供一种透皮渗透制剂,其包括浓缩的透皮活性成分层压体并显示高透皮渗透作用; 以及制备该制剂的方法A.一种透皮渗透制剂,其包含基础材料,其为吸收水和/或含水醇之后可膨胀的亲水性大分子,并且包含分子量高于1000的透皮活性成分 道尔顿,可以溶解或悬浮在层叠在基材表面的水和/或含水醇中; 以及生产透皮渗透制剂的方法,其中将分子量高于1000道尔顿的透皮活性成分溶解或悬浮在水和/或含水醇中以形成水溶液或悬浮液,并且所述水溶液或悬浮液为 涂布在基材表面上,该基材是由于在基材中吸收水或含水醇而吸收水或e含水醇之后可膨胀的亲水性大分子,由此形成含有透皮​​的层 处于集中状态的活性成分在基材的表面上。
    • 15. 发明申请
    • APPARATUS FOR MEASURING DIFFUSION OF TRANSDERMAL ABSORPTION PREPARATION
    • 用于测量扩张吸收制剂扩散的装置
    • US20100071445A1
    • 2010-03-25
    • US12525305
    • 2007-01-31
    • Fumio KamiyamaYing-shu Quan
    • Fumio KamiyamaYing-shu Quan
    • G01N13/04
    • G01N13/00G01N2013/003
    • This invention is to provide a diffusion testing device to facilitate determination of diffusivity of prolonged release of drugs from transdermal therapeutic preparation.The diffusion testing device is characterized by a receptor liquid reservoir; a diffusion testing cell having a receptor chamber functioning to be full of receptor liquid and within which a stirrer be placed, a receptor liquid supply unit, a thermostat bath to hold the diffusion testing cell, a stirring apparatus located beneath the thermostat bath to cause the rotation action of the stirrer set in the receptor chamber, a sampling unit permitting sampling and storage of receptor liquid dissolving permeated drugs. Said receptor liquid reservoir, said receptor chamber, said receptor liquid supply unit and said sampling unit are connected with each other via infusion tube. Said thermostat bath comprises aperturees or through-holes functioning to hold the diffusion testing cells, and metal block which has temperature regulation unit to be installed.
    • 本发明提供一种扩散测试装置,以便于确定药物从经皮治疗制剂中延长释放的扩散性。 扩散测试装置的特征在于受体液体储存器; 扩散测试电池,其具有充满受体液体并且其中放置搅拌器的受体室,受体液体供应单元,用于保持扩散测试电池的恒温槽,位于恒温槽下方的搅拌设备, 受体室中设置的搅拌器的旋转作用,允许取样和储存受溶液溶解渗透药物的取样单元。 所述受体液体储存器,所述受体室,所述受体液体供应单元和所述取样单元通过输注管相互连接。 所述恒温槽包括用于保持扩散测试电池的孔或通孔,以及具有要安装的温度调节单元的金属块。
    • 17. 发明申请
    • Transdermal Steriod for Formulation
    • 透皮制剂
    • US20070231373A1
    • 2007-10-04
    • US11568387
    • 2004-04-28
    • James MurrayFumio KamiyamaErnst Wulfert
    • James MurrayFumio KamiyamaErnst Wulfert
    • A61K31/57A61K31/56A61K9/70
    • A61K31/5685
    • Compounds of formula (I) (in which R1; R2, R3 and R4 are the same as or different from each other and each represents an oxo group, a hydroxy group, a mercapto group, a hydrogen atom, a halogen atom, an alkoxy group or an aryloxy group; and the dotted line indicates that there may be a single or double bond between one of the respective pairs of carbon atoms) and esters thereof can be administered by transdermal administration. They are particularly effective when applied as a patch, preferably with an adhesive comprising a copolymer of from 40 to 60% by weight of methoxyethyl acrylate, from 30 to 40% by weight of lauryl acrylate or lauryl methacrylate and from 10 to 25% by weight of a polar monomer.
    • 式(I)(其中R 1,R 2,R 3和R 4)的化合物是 各自表示氧基,羟基,巯基,氢原子,卤素原子,烷氧基或芳氧基;虚线表示可以存在单个或者多个 各对碳原子之间的双键)和其酯可以通过经皮施用来施用。 当作为贴剂使用时,它们是特别有效的,优选使用包含40至60重量%的丙烯酸甲氧基乙酯,30至40重量%的丙烯酸月桂酯或甲基丙烯酸月桂酯和10至25重量%的共聚物的粘合剂 的极性单体。