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1. 发明授权

US4365060A Enterosoluble capsules 失效
标题翻译：肠溶胶囊
公开(公告)号：US4365060A
公开(公告)日：1982-12-21
申请号：US140478
申请日：1980-04-15
申请人： Yoshiro Onda , Hiroaki Muto , Kazumasa Maruyama
发明人： Yoshiro Onda , Hiroaki Muto , Kazumasa Maruyama
IPC分类号： A61K9/22 , A61K9/28 , A61K9/48 , C08B3/16 , C08B13/00
CPC分类号： A61K9/4816 , A61K9/2866
摘要： The invention provides a novel enterosoluble capsule for containing a medicament, which is shaped with a hitherto not used novel cellulose derivative. The cellulose derivative is a mixed ester of an alkyl-, hydroxyalkyl- or hydroxyalkyl alkylcellulose esterified with succinyl anhydride and an aliphatic monocarboxylic acid anhydride. The enterosoluble capsules have excellent enterosolubility behavior as well as sufficient pliability even without the addition of a plasticizer which is almost indispensable in the prior art materials. The cellulose derivative can be shaped into capsules not only by the conventional dipping method but also by the plastic deformation at an elevated temperature under pressure such as compression molding, vacuum forming, matchedmold forming and the like.
摘要翻译：本发明提供了一种用于容纳药物的新型肠溶胶囊，其用迄今为止未使用的新型纤维素衍生物成型。纤维素衍生物是与琥珀酸酐和脂肪族单羧酸酐酯化的烷基 - ，羟基烷基 - 或羟烷基烷基纤维素的混合酯。即使没有添加在现有技术材料中几乎不可缺少的增塑剂，肠溶性胶囊也具有优异的肠溶性行为以及足够的柔韧性。纤维素衍生物不仅可以通过常规的浸渍方法成型为胶囊，而且可以通过压缩模塑，真空成型，匹配成型等压力下的高温下的塑性变形成形。

2. 发明授权

US4385078A Method for providing enteric coating on solid dosage forms and aqueous compositions therefor 失效
标题翻译：在固体剂型及其含水组合物上提供肠溶衣的方法
公开(公告)号：US4385078A
公开(公告)日：1983-05-24
申请号：US71298
申请日：1979-08-30
申请人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki , Kazumasa Maruyama , Atsushi Hatayama
发明人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki , Kazumasa Maruyama , Atsushi Hatayama
IPC分类号： A61K47/38 , A61K9/28 , C08L1/10 , C08L1/14
CPC分类号： A61K9/282 , A61K9/2866
摘要： A novel aqueous coating composition is proposed for providing enteric coating on solid dosage forms such as tablets. The aqueous coating composition of the invention comprises a fine powder of an enterosoluble cellulose derivative such as hydroxypropylmethylcellulose phthalate and hydroxypropylmethylcellulose acetate succinate, which is insoluble in water but can be plasticized and solubilized with certain plasticizing agents, as dispersed in an aqueous dispersing medium and a plasticizing agent having compatibility with the enterosoluble cellulose derivative and dissolved in the aqueous dispersing medium. The particle size of the enterosoluble cellulose derivative and the boiling point of the plasticizing agent is the key parameters and should be finer than 100 .mu.m in an average particle diameter and not lower than 100.degree. C., respectively. Upon application of the aqueous coating composition to the solid dosage forms, water as the dispersing medium is first evaporated leaving the cellulose derivative and the plasticizing agent, which latter solubilizes the former to form a continuous coating layer on the solid dosage forms imparting good and satisfactory enterosolubility thereto.
摘要翻译：提出了一种新颖的水性涂料组合物，用于在诸如片剂的固体剂型上提供肠溶衣。本发明的水性涂料组合物包括不溶于水但可以用某些增塑剂增塑和溶解的分散在水分散介质中的肠溶性纤维素衍生物如羟丙基甲基纤维素邻苯二甲酸酯和羟丙基甲基纤维素乙酸酯琥珀酸盐的细粉末，增塑剂与肠溶性纤维素衍生物具有相容性并溶于水分散介质中。肠溶性纤维素衍生物的粒径和增塑剂的沸点是关键参数，平均粒径分别小于100μm，不低于100℃。当将水性涂料组合物施用于固体剂型时，首先蒸发作为分散介质的水，留下纤维素衍生物和增塑剂，后者溶解前者，在固体剂型上形成连续涂层，赋予良好和令人满意的效果肠溶性。

3. 发明授权

US4226981A Ether-ester derivatives of cellulose and their applications 失效
标题翻译：纤维素的醚酯衍生物及其应用
公开(公告)号：US4226981A
公开(公告)日：1980-10-07
申请号：US944177
申请日：1978-09-20
申请人： Yoshiro Onda , Hiroaki Muto , Kazumasa Maruyama
发明人： Yoshiro Onda , Hiroaki Muto , Kazumasa Maruyama
IPC分类号： A61K9/28 , A61K9/36 , C08B13/00 , G03C1/835 , B44D1/50 , G03C1/92
CPC分类号： A61K9/2866 , C08B13/00 , G03C1/835
摘要： A novel cellulose derivative provided in this invention is a mixed ester of an alkoxy or hydroxyalkoxy substituted cellulose ether, prepared by the esterification reaction of the ether with succinic anhydride and an anhydride of an aliphatic monocarboxylic acid. The cellulose derivatives are advantageous because of their capability of producing enteric coatings having sufficient flexibility without the use of a plasticizer as well as by their chemical and physical stability against moisture, and also by easy purification after completion of the esterification reaction. The coatings produced from the derivatives have a similar chemical and physical stability. The cellulose derivatives are useful for the enteric coating of pharmaceutical dosage forms and also for providing halation-preventing layers on photographic films.
摘要翻译：本发明提供的新型纤维素衍生物是通过醚与琥珀酸酐的酯化反应和脂族一元羧酸的酸酐制备的烷氧基或羟基烷氧基取代的纤维素醚的混合酯。纤维素衍生物是有利的，因为它们具有在不使用增塑剂的情况下具有足够柔韧性的肠溶衣的能力，以及它们对水分的化学和物理稳定性以及酯化反应完成后容易的纯化。由衍生物生产的涂料具有相似的化学和物理稳定性。纤维素衍生物可用于药物剂型的肠溶包衣以及用于在照相胶片上提供防晕层。

4. 发明授权

US4917885A Hard medicinal capsule 失效
标题翻译：硬药胶囊
公开(公告)号：US4917885A
公开(公告)日：1990-04-17
申请号：US946119
申请日：1986-12-23
申请人： Tohru Chiba , Hiroaki Muto , Soji Tanioka , Yuichi Nishiyama , Noboru Hoshi , Yoshiro Onda
发明人： Tohru Chiba , Hiroaki Muto , Soji Tanioka , Yuichi Nishiyama , Noboru Hoshi , Yoshiro Onda
IPC分类号： A61K9/48 , C08L1/28
CPC分类号： A61K9/4816 , C08L1/28
摘要： In place of gelatin conventionally used as a material for shaping hard medicinal capsules, the invention proposes a hard capsule for medicinal use shaped of a polymer blend of a water-soluble cellulose ether, e.g., alkyl cellulose, hydroxyalkyl cellulose and alkyl hydroxyalkyl cellulose, and a polyvinyl alcohol in a weight ratio of 70:30 to 98:2. The inventive hard medicinal capsules have remarkably low permeability to oxygen and moisture with little influences on the medicament contained therein along with sufficiently high mechanical strengths and are much more stable than conventional gelatin-made capsules against the influences of the ambient conditions, such as, the crack formation unavoidable in a gelatin-made hard capsule when it is kept under an extremely low humidity.
摘要翻译：本发明代替通常用作形成硬药胶囊的材料的明胶，而提出了一种用于医用的硬胶囊，其形式为水溶性纤维素醚，例如烷基纤维素，羟烷基纤维素和烷基羟烷基纤维素的聚合物共混物，以及聚乙烯醇，重量比为70:30至98:2。本发明的硬药物胶囊具有非常低的氧气和水分渗透性，对其中所含的药物几乎没有影响，同时具有足够高的机械强度，并且比常规明胶制成的胶囊比环境条件的影响更稳定，例如当明胶制成的硬胶囊保持在极低的湿度下时，不可避免的裂缝形成。

5. 发明授权

US4322524A Cyanoethylpullulan 失效
标题翻译：氰基乙基
公开(公告)号：US4322524A
公开(公告)日：1982-03-30
申请号：US168269
申请日：1980-07-10
申请人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki
发明人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki
IPC分类号： C08B37/00
CPC分类号： C08B37/0018
摘要： The present invention provides a novel compound cyanoethylpullulan which is a cyanoethylation product of pullulan. Pullulan is readily cyanoethylated by the reaction with acrylonitrile in the presence of an alkali catalyst such as sodium hydroxide.The cyanoethylpullulan having a degree of cyanoethylation of at least 50% has various unique properties in the heat resistance, solubility in organic solvents, film-forming property, adhesive bonding to metals and the like in comparison with related cyanoethylated products such as cyanoethylcellulose and cyanoethylated polyvinyl alcohol.
摘要翻译：本发明提供了作为支链淀粉的氰乙基化产物的新型化合物氰乙基普兰兰。在碱性催化剂如氢氧化钠的存在下，通过与丙烯腈的反应，将支链淀粉容易地氰乙基化。具有至少50％氰基乙基化度的氰乙基普兰兰与相关的氰乙基纤维素和氰乙基化聚乙烯吡咯烷酮相关的氰乙基化产物相比具有各种独特的耐热性，在有机溶剂中的溶解性，成膜性，与金属的粘合性等醇。

6. 发明授权

US4091205A Method for preparing low-substituted cellulose ethers 失效
标题翻译：制备低取代纤维素醚的方法
公开(公告)号：US4091205A
公开(公告)日：1978-05-23
申请号：US635286
申请日：1975-11-26
申请人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki
发明人： Yoshiro Onda , Hiroaki Muto , Hiroshi Suzuki
IPC分类号： A61J3/06 , A61K9/20 , A61K47/38 , C08B11/00 , C08B11/20 , A61K31/72 , C08B11/02 , C08B11/08 , C08B11/12 , C08B11/193
CPC分类号： A61K9/2054 , C08B11/00 , C08B11/20 , Y10S514/951
摘要： In the process for the preparation of low-substituted cellulose ethers comprising the successive steps of etherification of alkali cellulose, neutralization of the crude cellulose ether, washing, drying and pulverization, the neutralization step is carried out in two stages, i.e., by first employing 5 to 80% of an acid stoichiometrically required and then adding an additional amount of the acid to complete neutralization. The cellulose ethers thus prepared can readily be pulverized into fine powder having a very good flowing property and yet an excellent binding force, and work as a suitable disintegrator in tablets.
摘要翻译：在制备低取代纤维素醚的方法中，包括碱纤维素醚化，中和粗纤维素醚，洗涤，干燥和粉碎的连续步骤，中和步骤分两个阶段进行，即首先采用按化学计量要求的5至80％的酸，然后加入额外量的酸以完全中和。如此制备的纤维素醚可以容易地粉碎成具有非常好的流动性能和优异的粘合力的细粉末，并且作为片剂中合适的崩解剂起作用。

7. 发明授权

US4993137A Method of manufacturing hard capsules 失效
标题翻译：制造硬胶囊的方法
公开(公告)号：US4993137A
公开(公告)日：1991-02-19
申请号：US449354
申请日：1989-12-13
申请人： Hiroaki Muto , Yuichi Nishiyama , Toru Chiba , Kiyoshi Araume
发明人： Hiroaki Muto , Yuichi Nishiyama , Toru Chiba , Kiyoshi Araume
IPC分类号： A61J3/07 , A61K9/48
CPC分类号： A61J3/077 , A61K9/4816 , Y10S264/37 , Y10S425/804 , Y10T29/49872
摘要： A method for manufacturing capsules causes the solution of thermo-gelling material to gelatinize once, and then drys the gel. Therefore the process of manufacturing capsules is less affected by drying conditions, thus providing capsules of uniform wall thickness without wrinkle. In the apparatus, circulating capsule pins are dipped in the solution of thermo-gelling material, thus the solution adheres to the pins. The pins are rotated upside down, thus thickness of the solution adhering to the pins becoming uniform. Then the pins are retained in the vessel maintained at a higher temperature than the gelling temperature of the solution, and the solution adhering to the pins is gelatinized. The thus-formed gel is dried through a drying device, and the dried gel, i.e. capsules, is removed from capsule pins.
摘要翻译：制造胶囊的方法使得热凝胶材料的溶液凝胶化一次，然后干燥凝胶。因此，制造胶囊的过程较少受干燥条件的影响，从而提供均匀的壁厚而没有皱纹的胶囊。在该装置中，将循环的胶囊销浸渍在热凝胶材料的溶液中，从而使溶液粘附到销上。销被倒置旋转，因此粘附在销上的溶液的厚度变得均匀。然后将销保持在保持在比溶液的胶凝温度更高的温度的容器中，并且粘附到销的溶液凝胶化。将如此形成的凝胶通过干燥装置干燥，并将干燥的凝胶，即胶囊从胶囊销中取出。

8. 发明授权

US4948622A Method for the preparation of coated solid medicament form 失效
标题翻译：涂覆固体药物形式的制备方法
公开(公告)号：US4948622A
公开(公告)日：1990-08-14
申请号：US224772
申请日：1988-06-09
申请人： Hiroyasu Kokubo , Hiroaki Muto , Tohru Chiba
发明人： Hiroyasu Kokubo , Hiroaki Muto , Tohru Chiba
IPC分类号： A61K47/44 , A61K9/28 , A61K9/34 , A61K9/50 , A61K9/52 , A61K9/60 , A61K47/00 , A61K47/38
CPC分类号： A61K9/5047 , A61K9/2866 , A61K9/2886 , A61K9/5073
摘要： Solid medicament forms, such as granules, beads, tablets, are first coated with a hot aqueous dispersion of a cellulose ether, which is soluble in cold water but insoluble in hot water, and then subjected to a wax treatment with heating to form a masking layer of the wax. Different from the coating film of a cellulose ether formed by using an aqueous or organic solution of the cellulose ether, the coating film formed by using the aqueous dispersion of the cellulose ether has a porous structure so that the amount of the wax deposited in the wax treatment is much larger than in the prior art methods to exhibit a high effect of masking the bitterness of the ingredient contained in the medicament form.
摘要翻译： PCT No.PCT / JP88 / 00483 Sec。 371日期：1988年6月9日 102（e）日期1988年6月9日PCT提交1988年5月23日PCT公布。出版物WO89 / 05635 日期：1989年6月29日。固体药物形式，例如颗粒剂，珠粒，片剂，首先用纤维素醚的热水分散体包衣，纤维素醚可溶于冷水但不溶于热水，然后经受蜡加热处理以形成蜡的掩蔽层。与通过使用纤维素醚的水溶液或有机溶液形成的纤维素醚的涂膜不同，通过使用纤维素醚的水分散体形成的涂膜具有多孔结构，使得沉积在蜡中的蜡的量处理比现有技术方法中大得多，以显示掩蔽药物形式中所含成分的苦味的高效果。

9. 发明授权

US5372998A Powdery material for preparing drug-coating solution 失效
标题翻译：用于制备药物涂层溶液的粉状材料
公开(公告)号：US5372998A
公开(公告)日：1994-12-13
申请号：US31347
申请日：1993-03-12
申请人： Hiroyasu Kokubo , Yuichi Nishiyama , Hiroaki Muto
发明人： Hiroyasu Kokubo , Yuichi Nishiyama , Hiroaki Muto
IPC分类号： A61K47/38 , A61K9/28 , A61K9/36 , A61K9/62 , A01N43/04
CPC分类号： A61K9/2866
摘要： The present invention provides a powdery starting material for preparing a drug-coating solution, which has high safety as a drug component and is very rapidly dissolved in room temperature water upon preparation of a coating solution. The powdery starting material for preparing a drug-coating solution comprises hydroxypropylmethyl cellulose and/or methyl cellulose particles having an average particle size ranging from 200 to 1000 .mu.m and whose content of particles having a particle size of 75 .mu.m or smaller is not more than 30% by weight. More preferably, the viscosity of a 2% by weight aqueous solution of the powdery starting material as determined at room temperature ranges from 2 to 60 cP and preferably 2 to 20 cP.
摘要翻译：本发明提供了一种制备药物涂层溶液的粉末状原料，其作为药物成分具有高安全性，并且在制备涂布溶液时非常快速地溶解在室温水中。用于制备药物包衣溶液的粉末状原料包括平均粒度为200-1000μm的羟丙基甲基纤维素和/或甲基纤维素颗粒，其粒径为75μm或更小的颗粒的含量不多超过30重量％。更优选地，在室温下测定的粉末原料的2重量％水溶液的粘度为2至60cP，优选为2至20cP。

10. 发明授权

US5086077A Endermic medicament with a gel base 失效
标题翻译：具有凝胶基质的终末药物
公开(公告)号：US5086077A
公开(公告)日：1992-02-04
申请号：US604921
申请日：1990-10-29
申请人： Sakae Obara , Hiroaki Muto , Sumiko Mizuno , Tohru Chiba , Izumi Saitoh , Kaori Ikeda
发明人： Sakae Obara , Hiroaki Muto , Sumiko Mizuno , Tohru Chiba , Izumi Saitoh , Kaori Ikeda
IPC分类号： A61K9/06 , A61K47/38 , C08B11/02
CPC分类号： A61K9/0014 , A61K47/38 , Y10S514/944 , Y10S514/946 , Y10S514/947
摘要： A novel endermic medicament having a consistency of a gel is proposed which is formulated, as a gel base, with non-ionic water-soluble cellulose ether, e.g., methyl cellulose and hydroxypropyl methyl cellulose, modified with a modification agent containing, in the molecule, an alkyl group having 6 to 26 carbon atoms and a functional group having reactivity with the hydroxyl group in the cellulose ether, e.g., stearyl glycidyl ether, decyl glycidyl ether and cetyl epoxide. The endermic medicament formulated with the modified cellulose ether is stable by virtue of the very little interaction between the active ingredients and the gel base and also can exhibit high percutaneous absorptivity of the active ingredients through the human skin.

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