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    • 2. 发明申请
    • BASE POLYMER FOR PERCUTANEOUSLY ABSORBABLE PREPARATION
    • 基础聚合物可用于可吸收制剂
    • WO1995004094A1
    • 1995-02-09
    • PCT/JP1994001253
    • 1994-07-29
    • TAKIRON CO., LTD.SHIKINAMI, Yasuo
    • TAKIRON CO., LTD.
    • C08G18/48
    • C08G18/4833A61K9/7023C08G18/283C08G18/4808
    • A base polymer for percutaneously absorbable preparations that is solid at ordinary temperatures but turns into a low-viscosity liquid near the human skin temperature, contains a hydrophilic segment, is responsive to heat and water, and enables drugs which have been difficult to compound into a percutaneously absorbable preparation to be stored stably for long and absorbed percutaneously with a high releasability and a high sustained releasability without causing much skin stimulation. The polymer comprises a heat-responsive segmented polyurethane represented by the general formula R-A-(U)-C-(U)-B-R , wherein A and B represent each independently a polymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide, or a random or block copolymer thereof; R and R represent each H, CH3, C2H5, C3H7 or C4H9 as the terminal group of A and B, respectively; C represents a residue of a diisocyanate compound; and (U) represents a urethane linkage; and wherein at least one of A and B is hydrophilic and at the same time will melt near the human skin temperature.
    • 用于经皮吸收制剂的基础聚合物,其在常温下为固体但在人体皮肤温度附近变成低粘度液体,含有亲水性片段,对热和水有反应,并且使难以复合的药物 经皮吸收制剂经长时间保存并经皮吸收,具有高释放性和高持久释放性,而不引起皮肤刺激。 聚合物包含由通式RA-(U)-C-(U)-BR 1表示的热响应性分段聚氨酯,其中A和B各自独立地表示环氧乙烷,环氧丙烷,四氢呋喃或 1,2-环氧丁烷或其无规或嵌段共聚物; R和R 1分别表示作为A和B的末端基团的H,CH 3,C 2 H 5,C 3 H 7或C 4 H 9; C表示二异氰酸酯化合物的残基; (U)表示氨基甲酸酯键; 并且其中A和B中的至少一个是亲水性的,并且同时将在人的皮肤温度附近熔化。
    • 4. 发明申请
    • OSTEOSYNTHETIC MATERIAL, COMPOSITED IMPLANT MATERIAL, AND PROCESS FOR PREPARING THE SAME
    • 合成材料,复合植入材料及其制备方法
    • WO1997010010A1
    • 1997-03-20
    • PCT/JP1996002642
    • 1996-09-13
    • TAKIRON CO., LTD.SHIKINAMI, YasuoOKUNO, Masaki
    • TAKIRON CO., LTD.
    • A61L27/00
    • C08L67/04A61L27/46A61L27/58A61L31/06A61L31/127A61L31/14A61L31/148A61L31/18B29C43/02B29C43/16B29C2791/001B29K2067/043B29K2067/046B29K2105/0005B29K2105/16B29K2105/251B29K2105/255B29K2267/043B29K2995/0041B29K2995/0051B29K2995/0059B29K2995/006B29L2031/7532A61L27/18A61F2/28A61B17/58
    • A high-bending-strength and high-density osteosynthetic material and a high-strength implant material, comprising either a biodegradable and bioabsorbable crystalline thermoplastic polymer material or a composite material comprising the above polymer material and a bioceramic powder having a particle diameter of 0.2 to 50 mu m dispersed therein, wherein crystals of the polymer material are pressure-oriented essentially parallel to a plurality of reference axes rather than uniaxially; and a process for preparing the above materials by pressure orientation, comprising preparing either a biodegradable and bioabsorbable crystalline thermoplastic polymer material or a mixture comprising a dispersion of a biodegradable and bioabsorbable crystalline thermoplastic polymer material and a dispersion of a bioceramic powder, melt-forming the mxiture into a preform, and pressure filling the preform into a cavity of a closed mold to prepare an oriented form. This process enables the preparation of ideal biomaterials, i.e., an osteosynthetic material and an implant material comprising an oriented form with crystals oriented parallel to a plurality of reference axes and possessing low anisotropy, high denseness, and high strength, which have suitable hydrolyzability, can retain satisfactory strength for a period of time necessary for bone coaptation and, after the recovery of the fractured portion, is degraded and adsorbed at such a rate as will not cuase any inflammation, thus eliminating the need to conduct reoperation.
    • 高抗弯强度和高密度骨接合材料和高强度植入材料,其包括可生物降解和生物可吸收的结晶热塑性聚合物材料或包含上述聚合物材料的复合材料和粒径为0.2至 50μm分散在其中,其中聚合物材料的晶体基本上平行于多个参考轴而不是单轴压力取向; 以及通过压力取向制备上述材料的方法,包括制备可生物降解和生物可吸收的结晶热塑性聚合物材料或包含可生物降解和生物可吸收的结晶热塑性聚合物材料的分散体和生物陶瓷粉末的分散体的混合物, 将预成型件浇注到预成型件中,并且将预成型件的压力填充到封闭模具的空腔中以制备取向形式。 该方法使得能够制备理想的生物材料,即,包括具有平行于多个参考轴定向且具有低各向异性,高致密度和高强度的晶体的定向形式的骨接合材料和植入材料,其具有合适的可水解性,可以 在骨接合所需的时间内保持令人满意的强度,并且在破裂部分恢复之后,以不会引起任何炎症的速度降解和吸附,因此不需要进行再手术。
    • 6. 发明申请
    • PERCUTANEOUSLY ABSORBABLE PREPARATION
    • PERCUTANEOUSYOUSLY可吸收制剂
    • WO1995009008A1
    • 1995-04-06
    • PCT/JP1994001584
    • 1994-09-27
    • TAKIRON CO., LTD.ONO PHARMACEUTICAL CO., LTD.SHIKINAMI, YasuoHATA, KunihiroSASATANI, SeieiSUDOH, Masao
    • TAKIRON CO., LTD.ONO PHARMACEUTICAL CO., LTD.
    • A61K47/30
    • A61K9/7084
    • A percutaneously absorbable preparation which can long stably preserve a water-soluble drug capable of exhibiting the effect in a small dose and being readily decomposable, solid at ordinary temperature and difficultly absorbable percutaneously and which can sustainedly release the drug percutaneously at a high rate when applied to the skin. The preparation comprises a drug store layer wherein a drug is incorporated and a drug release control membrane for coating the drug release surface of the drug store layer. This layer is made from a heat-sensitive segmented polyurethane which is represented by the following general formula: R-A-(U)-F-(U)-B-R', (wherein A and B represent each a homopolymer or a random or block copolymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide; R and R' represent each H, CH3, C2H5, C3H7 or C4H9 as the terminal of each of A nad B; A=B or A NOTEQUAL B; R=R' or R NOTEQUAL R'; F represents the residue of a diisocyanate compound; and (U) represents a urethane bond) and wherein at least one of A and B is hydrophilic and at least one of them will melt near the human skin temperature. The drug release control membrane comprises a phase-separation membrane wherein a cross-linked gelatin phase and a non-cross-linked segmented polyurethane phase are intermingled.
    • 一种经皮吸收制剂,其可以长期稳定地保持能够以小剂量显示效果并且易于分解的常温下的固体,并且经皮难以吸收的水溶性药物,并且其可以在施用时以高速率经皮持续释放药物 到皮肤。 该制剂包括其中掺入药物的药物储存层和用于涂覆药物储存层的药物释放表面的药物释放控制膜。 该层由热敏分段聚氨酯制成,其由以下通式表示:RA-(U)-F-(U)-B-R',(其中A和B各自表示均聚物或随机或 环氧乙烷,环氧丙烷,四氢呋喃或1,2-环氧丁烷的嵌段共聚物; R和R'表示作为A nad B各自的H,CH 3,C 2 H 5,C 3 H 7或C 4 H 9; A = B或A B; R = R'或R“等式R”; F表示二异氰酸酯化合物的残基;(U)表示氨基甲酸酯键),并且其中A和B中的至少一个是亲水性的,并且其中至少一个将在近 人体皮肤温度。 药物释放控制膜包括其中交联的凝胶相和非交联的分段的聚氨酯相混合的相分离膜。