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    • 6. 发明授权
    • Controlled drug delivery system for diltiazem
    • 地尔硫卓治疗药物输送系统
    • US6074669A
    • 2000-06-13
    • US984733
    • 1997-12-04
    • Vishnubhotla NagaprasadHimadri Sen
    • Vishnubhotla NagaprasadHimadri Sen
    • A61K9/20A61K9/26A61K9/52
    • A61K9/2054
    • A pharmaceutical composition in the form of a tablet or a capsule for the controlled release of diltiazem, comprises about 30 to about 97% by weight of a hydrophilic polymer, about 0.5 to about 30% by weight of an enteric (pH-dependent) polymer, and about 2.5 to about 60% by weight of diltiazem or a pharmaceutically acceptable salt or ester thereof. The ratio of hydrophilic polymer to enteric polymer is in the range of about 1:1 to about 15:1. Such a pharmaceutical composition releases diltiazem at a rate that allows effective plasma levels of diltiazem to be maintained over a period of twenty-four hours after administration to human adult subjects.
    • 片剂或胶囊形式的用于控制地尔硫卓的药物组合物包含约30至约97重量%的亲水性聚合物,约0.5至约30重量%的肠溶(pH依赖性)聚合物 ,和约2.5至约60重量%的地尔硫卓或其药学上可接受的盐或酯。 亲水性聚合物与肠溶性聚合物的比率在约1:1至约15:1的范围内。 这样的药物组合物以给予人成年受试者的二十四小时内维持有效血浆水平的地尔硫卓的速度释放地尔硫卓。
    • 8. 发明申请
    • Long acting compositions comprising zidovudine and lamivudine
    • 包含齐多夫定和拉米夫定的长效组合物
    • US20050175694A1
    • 2005-08-11
    • US10512464
    • 2002-04-23
    • Himadri SenSurva Jayanthi
    • Himadri SenSurva Jayanthi
    • A61K9/20A61K9/22A61K31/7068A61K31/7072A61P31/18
    • A61K9/205A61K9/2054A61K9/2059A61K31/7068A61K31/7072A61K2300/00
    • A pharmaceutical composition in the form of a tablet for controlled release of active ingredient(s) comprises lamivudione, zidovudine or combination of lamivudine and zidovudine or their pharmaceutically acceptable derivatives, and a mixture of hydrophilic polymers selected from the group consisting of at least one hydroxypropyl methylcellulose, at least one sodium alginate and at least one guar gum as controlled release matrix and a pharmaceutically acceptable calcium salt as a matrix stabilizer. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers, the calcium salt and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient(s) is released at a rate suitable for once daily administration of the pharmaceutical composition. The tablets may be coated with a water soluble polymeric film coat.
    • 用于控制释放活性成分的片剂形式的药物组合物包括拉米夫定,齐多夫定或拉米夫定和齐多夫定或其药学上可接受的衍生物的组合,以及选自至少一种羟丙基 甲基纤维素,至少一种藻酸钠和至少一种瓜尔胶作为控释基质和药学上可接受的钙盐作为基质稳定剂。 组合物还可以含有一种或多种水溶性和/或水分散性稀释剂,其中亲水性聚合物,钙盐和水溶性和/或水分散性稀释剂的量使得治疗有效的活性成分 以适合于每日一次给予药物组合物的速率释放。 片剂可以用水溶性聚合物膜包衣包衣。
    • 9. 发明授权
    • Orally administered controlled drug delivery system providing temporal and spatial control
    • 口服给药控制药物输送系统提供时间和空间控制
    • US06261601B1
    • 2001-07-17
    • US09152932
    • 1998-09-14
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • Naresh TalwarHimadri SenJohn N. Staniforth
    • A61K946
    • A61K9/0065A61K31/496
    • A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug, resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% ciprofloxacin base, 0.34% sodium alginate, 1.03% xanthan gum, 13.7% sodium bicarbonate, 12.1% cross-linked polyvinylpyrrolidone, and optionally other pharmaceutical excipients, the formulation being in the form of a coated or uncoated tablet or capsule.
    • 片剂或胶囊形式的药物组合物提供药物递送到患者的时间和空间控制的组合以获得有效的治疗结果。 药物组合物包含药物,气体发生组分,溶胀剂,粘稠剂和任选的凝胶形成聚合物。 溶胀剂属于称为超级崩解剂的一类化合物(例如交联聚乙烯吡咯烷酮或羧甲基纤维素钠)。 最初的粘稠溶剂和凝胶形成聚合物之后形成一种水合凝胶基质,其夹带气体,导致片剂或胶囊保留在胃或小肠上部(空间对照)中。 同时,水合凝胶基质为药物产生曲折的扩散途径,导致药物的持续释放(时间控制)。 优选的每日一次环丙沙星制剂包含69.9%环丙沙星碱,0.34%藻酸钠,1.03%黄原胶,13.7%碳酸氢钠,12.1%交联聚乙烯吡咯烷酮和任选的其它药物赋形剂,该制剂呈涂层或 未包衣的片剂或胶囊。
    • 10. 发明授权
    • Stable taste masked formulations of cephalosporins
    • 头孢菌素的稳定口罩掩蔽制剂
    • US08900637B2
    • 2014-12-02
    • US12095767
    • 2005-12-02
    • Sachin Pundlik KolheSubrata KunduSanjay Chhagan WaghMakarand Krishnakumar AvachatHimadri Sen
    • Sachin Pundlik KolheSubrata KunduSanjay Chhagan WaghMakarand Krishnakumar AvachatHimadri Sen
    • A61K9/16A61K31/00A61K9/28
    • A61K31/00A61K9/1635A61K9/2886
    • A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in α-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the α-crystalline form, wherein the particle size distribution of the α-crystalline form being such that 100% of the particles have a particle size below 250μ. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15μ. The process of preparation of coated, non-disintegrating pellets comprising the steps of reducing the particle size of the one or more cephalosporins, blending with the other excipients, wet granulation, extrusion, spheronization, drying and screening to obtain pellets, said pellets being further coated with one or more layers of film coating to achieve taste masking.
    • 稳定的掩味的药物组合物,其包含多个涂覆的,不分散的离散剂量单位,所述单元由包含一种或多种头孢菌素如头孢呋辛酯和头孢泊肟酯的核心和一个或多个涂层组成。 头孢呋辛酯是α-晶型和无定形形式,其中至少30%的头孢呋辛酯为α-结晶形式,其中α-晶型的粒度分布使得100%的颗粒具有颗粒 尺寸低于250μ。 结晶部分与无定形部分的比例为0.3:0.7至0.99:0.01。 头孢泊肟酯的粒径使得90%的颗粒小于15μ。 包衣,非崩解丸剂的制备方法包括以下步骤:减少一种或多种头孢菌素的粒度,与其它赋形剂混合,湿法制粒,挤出,滚圆,干燥和筛选以获得丸粒,所述丸粒进一步 涂覆一层或多层薄膜包衣以达到掩味。