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    • 1. 发明授权
    • Soluble, gum-containing, coated chewable tablet
    • 可溶,含胶,涂层咀嚼片
    • US06932979B2
    • 2005-08-23
    • US10407134
    • 2003-04-07
    • Gerhard GergelyIrmgard GergelyThomas Gergely
    • Gerhard GergelyIrmgard GergelyThomas Gergely
    • A23G3/00A23G3/02A23G3/38A23G3/42A23G3/54A61K9/00A61K9/20
    • A23G3/42A23G3/0289A23G3/38A23G3/54A61K9/0056
    • The soluble, rubber-containing, coated chewable tablet contains chewable components, syrup components and fat or wax components and optionally fillers. It can be prepared by a process in which pulverulent chewable components are mixed with the molten fat or wax components. The mixture, with the addition of at least one syrup component, then becomes a crumbly material, which is then cooled to below 0° C., then milled to a particle size of not more than 5 mm and, after cooling to below 10° C., compressed to give tablets which are coated in a known manner. The finished product—due to compression of the cooled granules—presumably has a partially granular structure in which the moisture has been initially immobilized by the low temperature. After compression, this moisture becomes mobile as a result of heating (in particular during the coating process) and migrates or diffuses—initially at the surface—into the water-soluble ingredients present. These are partially dissolved and give a highly viscous, thixotropic, chewable material.
    • 可溶的含橡胶的涂覆的咀嚼片含有咀嚼成分,糖浆组分和脂肪或蜡组分以及任选的填充剂。 可以通过将粉状咀嚼成分与熔融脂肪或蜡成分混合的方法来制备。 加入至少一种糖浆组分的混合物然后变成易碎的材料,然后将其冷却至0℃以下,然后研磨至不大于5mm的粒度,冷却至10℃以下 C.压缩得到以已知方式包衣的片剂。 由于冷却的颗粒的压缩,最终产品可能具有部分颗粒状结构,其中水分最初被低温固定。 在压缩之后,由于加热(特别是在涂布过程中),这种水分变得可移动,并且迁移或扩散 - 最初在表面进入存在的水溶性成分。 这些部分溶解并产生高粘度,触变性,咀嚼材料。
    • 2. 发明授权
    • Effervescent base
    • 泡腾基地
    • US06497900B2
    • 2002-12-24
    • US09529343
    • 2000-05-24
    • Gerhard GergelyIrmgard GergelyThomas GergelyStefan Gergely
    • Gerhard GergelyIrmgard GergelyThomas GergelyStefan Gergely
    • A61K946
    • A61K9/0007
    • The effervescent base for the preparation of effervescent tablets and effervescent granules consists of at least one acidic and one gas-evolving component, the former of which is formed by a mixture of (predominantly) monosodium tartrate and (possibly) disodium tartrate, and optionally tartaric acid. The effervescent base is prepared by mixing tartaric acid with sodium bicarbonate and sodium carbonate containing water of crystallization and slowly reacting the mixture at a temperature increasing to about 50° C., after which further sodium carbonate containing water of crystallization is admixed and is allowed to react up to a temperature of about 60° C., and drying is then carried out, preferably in vacuo, the mixture is mixed with further, now anhydrous sodium carbonate and the product is optionally pressed to give tablets. The base may additionally comprise an acid sensitive or an alkali-sensitive pharmaceutically active substance.
    • 用于制备泡腾片和泡腾颗粒的泡腾基底由至少一种酸性和一种气体逸出组分组成,前者由(主要)酒石酸单钠和(可能)酒石酸二钠)和任选的酒石酸 酸。 通过将酒石酸与碳酸氢钠和含有结晶水的碳酸钠混合制备起泡底物,并将混合物在升高至约50℃的温度下缓慢反应,然后混合另外含有结晶水的含碳酸钠,并使其 反应至约60℃的温度,然后进行干燥,优选在真空中,将混合物与另外的无水碳酸钠混合,任选地将产物压制得到片剂。 碱可以另外包含酸敏感或碱敏感的药物活性物质。
    • 5. 发明授权
    • Process and means for the heat treatment of powdery or granulate material
    • 用于粉末或颗粒材料的热处理的方法和方法
    • US4911930A
    • 1990-03-27
    • US297405
    • 1989-01-17
    • Gerhard GergelyIrmgard GergelyThomas Gergely
    • Gerhard GergelyIrmgard GergelyThomas Gergely
    • A61J3/02A61J3/06A61K9/00A61K9/16A61K9/46A61K31/19B01J2/00B01J2/10B01J2/12B01J2/16B01J3/00F26B7/00
    • B01J2/16A61K9/0007B01J2/10F26B7/00
    • Solid, loose particulate materials are treated with vaporizable agent in a process chamber. The materials are combined with a mixture of hot gas and vapor in order to condense finely subdivided amounts of the treatment agent on the material. After a suitable time of reaction, the condensed material is partially removed from the treated material so that the pressure in the process chamber is reduced at least to the point at which the treatment agent partially evaporates, whereupon the portion which has revaporized is extracted from the process chamber. This cycle of introduction and removal of the treating agent is preferably repeated in a program-controlled operation until the desired result is achieved and a product which is suitably agglomerated is obtained. In the present process, particulate material in powder or granule form is agitated and heat-treated in a closed drum, by stirring agents and surface treated by a hot gas flow forced over or through the charge of the material and then extracted intermittently by a vacuum pump. The air is heated and vaporized so that the vapor does not condense on the charge material.
    • 固体,松散的颗粒材料在处理室中用可蒸发剂处理。 将这些材料与热气体和蒸气的混合物组合以便将精细细分的量的处理剂冷凝在材料上。 在适当的反应时间之后,将冷凝材料从经处理的材料中部分地除去,使得处理室中的压力至少降低到处理剂部分蒸发的程度,随后从其中提取已再汽化的部分 处理室。 处理剂的引入和除去的这个循环优选在程序控制操作中重复,直到达到所需的结果,并且获得适当聚集的产物。 在本方法中,粉末或颗粒形式的颗粒材料在封闭的鼓中通过搅拌剂进行搅拌和热处理,并通过强制的热气流进行表面处理,或通过该材料的电荷进行表面处理,然后通过真空间歇地提取 泵。 空气被加热和蒸发,使得蒸气不会在充电材料上冷凝。
    • 6. 发明授权
    • Effervescent composition and method of making same
    • 泡腾组合物及其制造方法
    • US4678661A
    • 1987-07-07
    • US880081
    • 1986-06-30
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • A23L2/40A61K9/46A61K33/10
    • A61K9/0007A23L2/40A61K33/10Y10S514/819
    • Effervescent granulates, particularly for the manufacture of effervescent tablets, comprising at least one solid, crystalline edible organic acid and at least one carbonate which releases carbon dioxide upon reaction with the organic acid, the acid crystals comprising a coating which contains calcium carbonate adhering to the surface of the acid crystals by means of a bonding layer formed by a reaction at the interface with the crystal of a calcium carbonate coating material. The coating is built up in multi-layers and includes at least two carbonate layers, the layer which is bonded essentially to the acid crystal being composed of calcium carbonate with the succeeding layers adhering to the carbonate layer by means of a bonding layer formed by reaction of the acid and the carbonate. The invention also deals with methods of manufacture as well as fields of use for the new effervescent granulates.
    • 泡腾颗粒,特别是用于制造泡腾片剂,其包含至少一种固体,结晶可食用有机酸和至少一种与有机酸反应释放二氧化碳的碳酸盐,所述酸晶体包含含有碳酸钙的涂层, 通过在与碳酸钙涂层材料的结晶的界面处的反应形成的结合层,形成酸晶体的表面。 该涂层是多层构成的,并且包括至少两个碳酸盐层,该层基本上与由碳酸钙组成的酸性晶体结合,后续层通过由反应形成的粘合层粘附到碳酸盐层 的酸和碳酸盐。 本发明还涉及新的泡腾颗粒的制造方法和使用领域。
    • 7. 发明授权
    • Pharmaceutical formulation in the form of an effervescent and/or
disintegrating tablet or of instant granulate, and process for their
preparation
    • 以泡腾和/或崩解片剂或即时颗粒形式的药物制剂及其制备方法
    • US5587179A
    • 1996-12-24
    • US256503
    • 1994-07-13
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • A61K9/16A61K9/22A61K9/46A61K47/38A61K47/44
    • A61K9/0007A61K9/1676
    • The pharmaceutical formulation in the form of an effervescent and/or disintegrating tablet or of instant granules contains at least one active ingredient having an irritating taste and at least one matrix which delays the release of the active ingredient and is present as an intimate mixture with the active ingredient particles or covers said particles and is applied to a carrier. The formulation releases at most 65%, preferably at most 50%, of the active ingredient in aqueous solution at room temperature within about 2 min but more than 70%, preferably at least 80%, of the active ingredient within max. 20 min, preferably max. 15 min, in 0.1N HCl at 38.degree. C. The matrix preferably contains at least one fatty ester and/or one wax, preferably having a melting point between 30.degree. and 45.degree. C., in particular between 32.degree. and 35.degree. C., and/or at least one cellulose derivative and/or at least one polymethacrylate. In particular, the active ingredient is present in an amount of less than 60 mg, preferably less than 10 mg, and the matrix is present in an amount of 1 to 10, preferably 3 to 5, times the amount of active ingredient per tablet or granule dose. For the treatment of diarrhoea by means of loperamide, the matrix additionally contains a mixture which serves to compensate for the electrolyte loss in the body and an amount of alkali metal and/or alkaline earth metal salts, preferably of organic salts, and of chlorides.
    • PCT No.PCT / EP93 / 00055 Sec。 371日期:1994年7月13日 102(e)日期1994年7月13日PCT提交1993年1月12日PCT公布。 公开号WO93 / 13760 PCT 日期1993年7月22日泡腾和/或崩解片剂或速溶颗粒形式的药物制剂含有至少一种具有刺激性味道的活性成分和至少一种延迟活性成分释放并且以 与活性成分颗粒的紧密混合物或覆盖所述颗粒并施加到载体上。 该制剂在室温下在约2分钟内释放活性成分的至多65%,优选至多50%,在约2分钟内释放大于70%,优选至少80%的活性成分。 20分钟,最好最大 15分钟,在38℃的0.1N HCl中。基质优选含有至少一种脂肪酯和/或一种蜡,优选熔点在30-45℃之间,特别是在32-35℃之间 和/或至少一种纤维素衍生物和/或至少一种聚甲基丙烯酸酯。 特别地,活性成分的存在量小于60mg,优选小于10mg,并且基质的存在量为每片或每片或更多的活性成分的量的1至10,优选3至5倍 颗粒剂量 为了通过洛哌丁胺治疗腹泻,基质还含有一种混合物,其用于补偿身体中的电解质损失以及一定量的碱金属和/或碱土金属盐,优选有机盐和氯化物。
    • 8. 发明授权
    • Particles of hydrophobic or sparingly soluble substance
    • 疏水或微溶物质的颗粒
    • US5158779A
    • 1992-10-27
    • US266350
    • 1988-11-02
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • Gerhard GergelyThomas GergelyIrmgard Gergely
    • A61K9/00A61K9/16A61K9/50B01J2/00
    • A61K9/1676A61K9/5015A61K9/5026A61K9/5089
    • The surface of micronized and hydrophilized powder particles of a hydrophobic or sparingly soluble substance is covered with a cohesive layer of not more than 0.1 part by weight of surfactant in not more than 10 parts by weight of a binder (based on 100 parts by weight of the substance). A sparingly soluble or insoluble antibiotic is converted to instant granules or instant tablets, while a hydrophobic, moderately soluble to readily soluble pharmaceutical substance, such as, for example, acetylsalicylic acid or paracetamol, is converted to effervescent granules or effervescent tablets. The particles are preferably applied to carbohydrate crystals by means of a binder. The preparation is carried out by a method in which a solution which contains at least one surfactant in an amount of 0.01 to 0.1% by weight, based on the weight of the particles to be hydrophilized, and a binder in an amount corresponding to 5 to 10 times the weight of the surfactant used is sucked through a bed of the particles under a pressure of less than 800, preferably less than 100, mbar.
    • 疏水性或微溶性物质的微粉化和亲水化粉末颗粒的表面被不超过10重量份粘合剂的0.1重量份表面活性剂的内聚层覆盖(基于100重量份的粘合剂 物质)。 将微溶或不溶性抗生素转化为速溶颗粒剂或速溶片剂,而将疏水的,适度溶解的易溶于药物的物质例如乙酰水杨酸或对乙酰氨基酚转化为泡腾颗粒剂或泡腾片剂。 颗粒优选通过粘合剂施用于碳水化合物晶体。 该制备方法通过以下方法进行:将含有至少一种表面活性剂的溶液的量为0.01〜0.1重量%,相对于待亲水化的颗粒的重量为5〜 使用的表面活性剂的重量的10倍在小于800,优选小于100毫巴的压力下通过颗粒床吸入。
    • 10. 发明授权
    • Effervescent formulation containing plant extract
    • 含有植物提取物的泡腾制剂
    • US06190697B1
    • 2001-02-20
    • US09178639
    • 1998-10-26
    • Gerhard GergelyIrmgard GergelyThomas GergelyStefan Gergely
    • Gerhard GergelyIrmgard GergelyThomas GergelyStefan Gergely
    • A61K946
    • A61K9/0007A61K36/00A61K2300/00
    • The effervescent formulation elation in the form of granules or of a tablet contains, in addition to the effervescent base, at least one water-soluble or at least suspendable plant extract whose particles are coated with at least one oily, fatty or waxy substance. At least one emulsifier and/or at least one antifoam may be present in the coating and/or as a further component of the mixture, in particular applied as a further component of the mixture to a pharmaceutically permissible filler as carrier. The individual phases are prepared by a procedure in which the plant extract or the filler is heated—preferably in a granulator, in particular in a vacuum granulator—and wet or mixed with a melt or solution of the oily, fatty or waxy substance or at least one emulsifier and/or at least one antifoam and then dried—preferably in a vacuum—and sieved to the desired particle size.
    • 颗粒或片剂形式的泡腾剂配方除了泡腾基质之外还含有至少一种水溶性或至少可悬浮的植物提取物,其颗粒被至少一种油性,脂肪或蜡状物质包被。 至少一种乳化剂和/或至少一种消泡剂可以存在于涂层和/或作为混合物的另外的组分中,特别是作为混合物的另外的组分被用作药学上允许的填料作为载体。 各个阶段通过其中植物提取物或填料加热的方法制备,优选在造粒机中,特别是在真空制粒机中,并且与油,脂肪或蜡质物质的熔体或溶液一起湿润或混合,或在 至少一种乳化剂和/或至少一种消泡剂,然后干燥,优选在真空中并筛分至所需粒度。