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    • 2. 发明授权
    • Pharmacological treatments with N-7-substituted derivatives of
theophylline
    • 用茶碱的N-7-取代衍生物进行药理学处理
    • US4581359A
    • 1986-04-08
    • US602665
    • 1984-04-23
    • James W. Ayres
    • James W. Ayres
    • A61K31/52
    • A61K31/52Y10S514/826
    • Methods for the management of bronchopulmonary insufficiency and other conditions are disclosed. The methods involve administration of an N-7-substituted derivative of theophylline selected from the group consisting of dyphylline, etophylline, proxyphylline and mixtures thereof. The derivative can be administered intravenously, intramuscularly, or in the lungs, concurrently with some form of theophylline or administered alone to a patient whose body has a known or an unknown theophylline content. Theophylline and the derivative can be administered in the same dosage form or in separate dosage forms. They can have the same route of administration or different routes of administration; for example, theophylline can be given orally, while the derivative is given as a zero-order intravenous infusion. A high total plasma concentration of methyl xanthine is achieved safely by using a combination of theophylline and one or more of the derivatives. Rapid injection of a loading dose of the derivative is also disclosed.
    • 公开了治疗支气管肺功能不全等条件的方法。 所述方法包括施用选自由二苯胺,乙酸盐,丙酸盐及其混合物组成的组的茶碱的N-7-取代衍生物。 该衍生物可以与某些形式的茶碱一起静脉内,肌肉内或肺内给药,或单独施用于其身体具有已知或未知的茶碱含量的患者。 茶碱和衍生物可以以相同的剂型或分开的剂型给药。 它们可以具有相同的给药途径或不同的给药途径; 例如,茶碱可以口服给药,而衍生物作为零级静脉输注给药。 通过使用茶碱和一种或多种衍生物的组合,可以安全地实现甲基黄嘌呤的高总血浆浓度。 还公开了快速注射载体剂量的衍生物。
    • 4. 发明授权
    • Compactable self-sealing drug delivery agents
    • 可密封的自密封药物递送剂
    • US5766623A
    • 1998-06-16
    • US621562
    • 1996-03-25
    • James W. AyresSyed A. AltafStephen W. Hoag
    • James W. AyresSyed A. AltafStephen W. Hoag
    • A61K9/00A61K9/20A61K9/22A61K9/50A61K9/16
    • A61K9/2095A61K9/0056A61K9/5078
    • Active agents comprising coated pellets which self seal if they are damaged are described. More specifically, an active agent, or bead coated with an active agent, is coated with a rate-release controlling polymer and a hydrophilic gel-forming material which forms a gel upon hydration. If the bead is compressed into a solid compact which damages the polymer coating, the hydrophilic substance gels upon exposure to an aqueous environment. The gel provides sufficient sealing of the damaged area in the polymer so that a useful control of drug release is retained in spite of the damage to the polymer. The pellets of the invention exhibit improved flow and compactability. The compacts can be formulated to disintegrate in the gastrointestinal tract, and also may result in either controlled release or immediate release of the active agent.
    • 描述了包含自身密封如果它们被损坏的涂覆丸粒的活性剂。 更具体地,用活性剂涂覆的活性剂或珠涂覆有速率释放控制聚合物和在水合时形成凝胶的亲水凝胶形成材料。 如果珠被压缩成破坏聚合物涂层的固体压块,亲水物质在暴露于水性环境中时凝胶化。 凝胶提供了聚合物中损伤区域的足够的密封,使得尽管对聚合物的损害,仍然保留有用的药物释放控制。 本发明的颗粒显示出改善的流动性和可压缩性。 压块可以配制成在胃肠道中分解,并且还可以导致活性剂的受控释放或立即释放。
    • 5. 发明授权
    • Bacterial growth medium and method of use
    • 细菌生长培养基及使用方法
    • US4615978A
    • 1986-10-07
    • US682495
    • 1984-12-18
    • William E. SandineJames W. Ayres
    • William E. SandineJames W. Ayres
    • A23C19/032C12N1/00C12N1/04C12N1/20C12N1/38A23C9/12A23C9/123C12P7/56
    • A23C19/0323C12N1/00C12N1/04C12N1/20C12N1/38
    • An improved powdered bacterial growth medium composition adapted to be admixed with water is described. The powdered growth medium includes an alkaline earth metal cation in a compound A admixed with a compound B containing an anion which reacts with the alkaline earth metal cation in compound A in an aqueous growth medium to form an essentially water insoluble salt or base, including the alkaline earth metal cation and the anion, which is acid neutralizing. The water insoluble salt is thus formed in situ in the aqueous growth medium when compounds A and B are added to the aqueous solution. Also described is an improved method for growing acid producing bacteria in an aqueous growth medium by forming the insoluble salt or base. The resulting growth medium is particularly adapted for neutralizing acids generated during growth of lactic acid producing bacteria which are grown for use in various food fermentations.
    • 描述了适于与水混合的改进的粉状细菌生长培养基组合物。 粉末状生长培养基包括与含有阴离子的化合物B混合的化合物A中的碱土金属阳离子,所述阴离子与水性生长培养基中化合物A中的碱土金属阳离子反应,形成基本上不溶于水的盐或碱,包括 碱土金属阳离子和阴离子,它是酸中和的。 因此当化合物A和B添加到水溶液中时,水不溶性盐在水性生长培养基中原位形成。 还描述了通过形成不溶性盐或碱,在水性生长培养基中生长生酸细菌的改进方法。 所得的生长培养基特别适用于中和生长用于各种食物发酵的乳酸生产细菌生长期间产生的酸。
    • 7. 发明授权
    • Coated, platform-generating tablet
    • US06720005B1
    • 2004-04-13
    • US09887318
    • 2001-06-21
    • James W. Ayres
    • James W. Ayres
    • A61K936
    • A61K9/2846A61K9/2059A61K9/2072A61K9/2866
    • An expanding tablet is described comprising a drug release controlling membrane material. After swallowing, the tablet hydrates and expands such that the membrane ruptures to directly expose some surfaces of the core tablet to hydrating and eroding liquids, thus generating in situ a tablet which is platform supported on non-exposed surfaces, and which releases active ingredient in approximately zero order fashion. More particularly, the dosage form is adapted for controlled release of various pharmaceuticals. A working embodiment of the tablet was a spray-coated tablet comprising a core having greater than 25% of an expandable material which expands upon exposure to an aqueous environment and at least one active ingredient, e.g., glipizide, and an outer rupturable coating surrounding the core comprising a rate release modifying membrane and a water-soluble modifier. A method for administering an active ingredient also is described. The method comprises (1) providing a tablet according to the invention, and (2) administering the tablet to a patient.
    • 8. 发明授权
    • Process for separating radioactive and hazardous metal contaminants from
soils
    • 将放射性和有害金属污染物与土壤分离的过程
    • US4783253A
    • 1988-11-08
    • US853995
    • 1986-04-21
    • James W. AyresAlfred W. Western
    • James W. AyresAlfred W. Western
    • B07C5/346B09C1/02B07C5/34B03B5/16
    • B07C5/346B09C1/02
    • A process for treating radioactive contaminated soils to remove radioactive metal oxide contaminants therefrom comprises creating a suspension of particles of the soil in a column of water, alternately forcing fresh water in the column upwardly to force ligher soil particles upwardly in the column and allowing heavier particles to gravitationally settle in the bottom of the water column. The heavy particles comprising radioactive metal oxides are collected and handled for radioactive waste material storage. The aqueous slurry of lighter soil particles is directed to a separator for removing substantial amounts of water after which the particles are directed to a conveyor and spread out to a substantially uniform thickness and detected for any radioactivity. Portions of material in which radioactive particles are detected ar diverted and the uncontaminated soil material is recovered.
    • 用于处理放射性污染土壤以除去其中的放射性金属氧化物污染物的方法包括在水柱中产生土壤颗粒的悬浮液,交替地迫使柱中的淡水向上施力以迫使土壤颗粒在柱中向上并允许较重的颗粒 重力沉降在水柱的底部。 收集并处理包含放射性金属氧化物的重粒子用于放射性废物储存。 较轻土壤颗粒的含水浆液被引导到用于除去大量水的分离器,之后将颗粒引导到输送机上并展开至基本上均匀的厚度并且检测任何放射性。 检测到放射性粒子的部分材料被转移,未被污染的土壤物质被回收。
    • 9. 发明授权
    • Two-membrane medicated device for rate-controlled administration of
prostaglandins
    • 用于速率控制前列腺素给药的双膜药物装置
    • US4237888A
    • 1980-12-09
    • US23126
    • 1979-03-23
    • Theodore J. RosemanOsmer C. CarpenterRichard W. BakerJames W. Ayres
    • Theodore J. RosemanOsmer C. CarpenterRichard W. BakerJames W. Ayres
    • A61F13/20A61K9/00A61K31/557
    • A61F13/28A61F13/2051A61F13/2068A61F13/2074A61K31/557A61K9/0036A61F13/2011A61F2013/8414
    • The present specification describes a medicated device adapted for a single, acute, and rate-controlled rectal or vaginal administration to a mammal of a lipophilic prostaglandin. The device accomplishes drug administration at an essentially time-independent rate of dosage. Further, the device advantageously results in the substantial exhaustion of the prostaglandin from the device at the conclusion of the single, acute use. The device comprises three elements:(A) an inert resilient support means contoured for easy vaginal or rectal insertion;(B) a first flexible polymer film layer affixed to the support means and containing the prostaglandin dispersed therethrough, this first polymer film not being rate limiting as to the release of drug from the device; and(C) a second polymer film, laminated onto the first polymer film and providing a release rate therefrom of prostaglandin, which is rate limiting both as to the release of prostaglandin from the device and absorption rate by the rectal or vaginal tissues.
    • 本说明书描述适用于对亲脂性前列腺素的哺乳动物的单次,急性和速率控制的直肠或阴道给药的药物装置。 该装置以基本上时间独立的剂量速率实现药物给药。 此外,该装置有利地导致在单次急性使用结束时来自装置的前列腺素的显着耗尽。 该装置包括三个元件:(A)易于阴道或直肠插入的惰性弹性支撑装置; (B)固定在支撑装置上并含有分散在其中的前列腺素的第一柔性聚合物膜层,该第一聚合物膜不限制药物从装置中的释放; 和(C)第二聚合物膜,层压在第一聚合物膜上并提供前列腺素的释放速率,前列腺素的释放速率限于前列腺素从装置中的释放和由直肠或阴道组织吸收的速率。