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    • 12. 发明授权
    • Method for automatic dosing of drugs
    • 药物自动给药方法
    • US5782799A
    • 1998-07-21
    • US797296
    • 1997-02-07
    • Stephen C. JacobsenGaylen M. Zentner
    • Stephen C. JacobsenGaylen M. Zentner
    • A61D7/00A61M31/00
    • A61M31/002A61D7/00
    • The method for automatic dosing of drugs utilizes a microdelivery device which may be implanted in or otherwise administered to an animal or human. A microdelivery device is configured to have a plurality of compartments, each containing at least one drug so that a plurality of doses of the drug(s) are held within the device. In accordance with the present invention, the microdelivery device selectively actuates the compartments to selectively release doses of the drug(s) to provide an efficacious dosing pattern. One primary function of the present invention is to release two or more pesticides in such a pattern that parasites are effectively controlled while preventing the development of tolerance to the drugs within the parasites. Preferably, the microdelivery device is programmable to effectuate the release of the drug(s) at a desired time to maintain efficacious levels of the drug while minimizing the amount of drug which must be used.
    • 用于药物自动给药的方法使用可以植入或以其它方式施用于动物或人的微量输送装置。 微量输送装置被配置为具有多个隔室,每个隔间包含至少一种药物,使得多个剂量的药物保持在该装置内。 根据本发明,微量输送装置选择性地致动隔室以选择性地释放药物的剂量以提供有效的给药模式。 本发明的一个主要功能是以这样的模式释放两种或更多种杀虫剂,即在有效地控制寄生虫的同时防止对寄生虫内的药物的耐受性的发展。 优选地,微量输送装置是可编程的,以在期望的时间实现药物的释放,以保持药物的有效水平,同时最小化必须使用的药物的量。
    • 16. 发明授权
    • Solubility modulated drug delivery system
    • 溶解调制药物输送系统
    • US4946686A
    • 1990-08-07
    • US348099
    • 1989-05-01
    • Gregory A. McClellandGaylen M. Zentner
    • Gregory A. McClellandGaylen M. Zentner
    • A61K9/00A61K9/22
    • A61K9/0004
    • A drug delivery device for the controlled release of a therapeutically active ingredient into an environment of use is disclosed which comprises:(A) a core composition comprising(a) a plurality of controlled release solubility modulating units comprising solubility modulating agents each of which is a complexing agent or a surfactant and which is either (i) surround by a water insoluble cost containing at least one pore forming additive dispersed throughout said coat, or (ii) dispersed in an individual matrix substrate, and(b) A therapeutically active ingredient; and(B) a water insoluble microporous wall surrounding said core composition comprising:(i) a polymer material that is permeable to water but substantially impermeable to solute and(ii) 0.1 to 75% by weight, based on the total weight of (i) and (ii), of at least one water leachable pore forming additive dispersed throughout said wall.
    • 公开了用于将治疗活性成分控制释放到使用环境中的药物递送装置,其包括:(A)核心组合物,其包含(a)多个控释溶解度调节单元,其包含溶解性调节剂,其各自为 络合剂或表面活性剂,其(i)通过不溶于水的成本包围,其包含分散在所述涂层中的至少一种成孔添加剂,或(ii)分散在单独的基质底物中,和(b)治疗活性成分; 围绕所述芯组合物的水不溶性微孔壁包括:(i)可渗透水但基本上不可渗透溶质的聚合物材料,和(ii)基于(i)的总重量为0.1-75重量% )和(ii)分散在整个所述壁上的至少一种可浸出水的成孔添加剂。
    • 18. 发明授权
    • Biodegradable low molecular weight triblock poly(lactide-co- glycolide) polyethylene glycol copolymers having reverse thermal gelation properties
    • 具有反向热凝胶化特性的可生物降解的低分子量三嵌段聚(丙交酯 - 共 - 乙交酯)聚乙二醇共聚物
    • US06201072B1
    • 2001-03-13
    • US09396589
    • 1999-09-15
    • Ramesh C. RathiGaylen M. ZentnerByeongmoon Jeong
    • Ramesh C. RathiGaylen M. ZentnerByeongmoon Jeong
    • C08G6391
    • C08G63/664A61K9/0024A61K9/1075A61K47/34C08L71/02C08L2666/18
    • A water soluble, biodegradable ABA- or BAB-type tri-block polymer is disclosed that is made up of a major amount of a hydrophobic A polymer block made of a biodegradable polyester and a minor amount of a hydrophilic polyethylene glycol(PEG) B polymer block, having an overall average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the tri-block polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the tri-block polymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, inhalation, transdermal, vaginal, transurethral, rectal, nasal, oral, pulmonary or aural delivery means and is a gel at body temperature. The composition may also be administered as a gel. The drug is released at a controlled rate from the gel which biodegrades into non-toxic products. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic component content, polymer concentration, molecular weight and polydispersity of the tri-block polymer. Because the tri-block polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition.
    • 公开了一种水溶性,可生物降解的ABA或BAB型三嵌段聚合物,其由主要量的由可生物降解聚酯和少量亲水性聚乙二醇(PEG)B聚合物制成的疏水性A聚合物嵌段 具有约2000和4990之间的总平均分子量,并具有反向热凝胶化性质。 三嵌段聚合物和药物的有效浓度可以均匀地包含在水相中以形成药物递送组合物。 在低于三嵌段聚合物的凝胶化温度的温度下,组合物是液体,并且在等于或高于凝胶化温度的温度下,组合物是凝胶或半固体。 组合物可以通过胃肠外,眼部,局部,吸入,透皮,阴道,经尿道,直肠,鼻腔,口腔,肺或听觉递送装置作为液体施用于温血动物,并且是体温下的凝胶。 组合物也可以作为凝胶施用。 药物以可控制的速率从生物降解成无毒产品的凝胶释放。 可以通过改变三嵌段聚合物的各种参数如疏水/亲水组分含量,聚合物浓度,分子量和多分散性来调节药物的释放速率。 因为三嵌段聚合物是两亲性的,所以其作用是增加药物在组合物中的溶解度和/或稳定性。