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公开(公告)号:US4695465A
公开(公告)日:1987-09-22
申请号:US720401
申请日:1985-04-05
CPC分类号: A61K9/7053 , A61K9/7007 , A61K9/7061 , A61K9/7069 , Y10S514/946 , Y10S514/947
摘要: Drug preparations for external application having a stick-itself-to-the-skin property, so-called "soft patch", are provided. The preparations contain a drug, a water-soluble protein having an absorption-promoting effect, a polyhydric alcohol a tackifier, and an oleaginous substance, and ensure an improved percutaneous absorption and bioavailability of the drugs, thus permitting an accurate control of drug dosage.
摘要翻译: 提供了具有粘贴本身对皮肤特性的外部应用的药物制剂,即所谓的“软贴剂”。 该制剂含有药物,具有吸收促进作用的水溶性蛋白质,多元醇增粘剂和油性物质,并且确保药物的经皮吸收和生物利用度得到改善,从而可以准确控制药物剂量。
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公开(公告)号:US4024082A
公开(公告)日:1977-05-17
申请号:US605950
申请日:1975-08-19
IPC分类号: C07D221/28 , C07D237/00 , C07D471/08
CPC分类号: C07D471/08
摘要: dl-N-Cyclopropylmethyl-3-hydroxy-9-azamorphinan is a compound known to possess analgesic activity that is about twice as potent as pentazocine. Resolution of the compound into its levorotatory and dextrorotatory isomers and subsequent animal testing revealed that l-N-cyclopropylmethyl-3-hydroxy-9-azamorphinan was much more potent than the dl-mixture.
摘要翻译: dl-N-环丙基甲基-3-羟基-9-阿卡波霉素是已知具有止痛活性的化合物的化合物的剂量为约他卡他敏的两倍。 将化合物分解成其左旋和右旋异构体并随后进行的动物试验显示,1-N-环丙基甲基-3-羟基-9-阿魏霉素比dl-混合物更有效。
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公开(公告)号:US4572832A
公开(公告)日:1986-02-25
申请号:US540161
申请日:1983-10-07
申请人: Kazuo Kigasawa , Hiroaki Shimizu , Toshihiro Hayashi , Kazuo Watabe , Akira Tanizaki , Osamu Koyama , Kikuo Wakisaka , Yasuaki Ogawa
发明人: Kazuo Kigasawa , Hiroaki Shimizu , Toshihiro Hayashi , Kazuo Watabe , Akira Tanizaki , Osamu Koyama , Kikuo Wakisaka , Yasuaki Ogawa
CPC分类号: A61K9/2004 , A61K9/006
摘要: A soft buccal containing (1) a medicament to be absorbed through the oral mucosa, (2) a water-soluble protein, (3) a polyhydric alcohol, and (4) a fatty acid ester or/and a carboxyvinyl polymer, has various advantages such as good feeling in use, good retainability within the mouth, slow release, improved absorbability of drug through the mucosa, improved bioavailability, etc., and therefore can be used an excellent pharmaceutical preparation for administration to the mucous membrane of the mouth.
摘要翻译: 一种软颊含有(1)通过口腔粘膜吸收的药物,(2)水溶性蛋白质,(3)多元醇,和(4)脂肪酸酯或/和羧乙烯基聚合物,各种各样的 口感好,口内保留性好,缓释,药物通过粘膜吸收性好,生物利用度提高等优点,因此可用于向口腔粘膜施用的优良药物制剂。
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公开(公告)号:US4528372A
公开(公告)日:1985-07-09
申请号:US385379
申请日:1982-05-21
申请人: Kazuo Kigasawa , Mineharu Hiiragi , Kikuo Wakisaka , Keiko Ichikawa , Kikuo Nakazato , Taiji Okada
发明人: Kazuo Kigasawa , Mineharu Hiiragi , Kikuo Wakisaka , Keiko Ichikawa , Kikuo Nakazato , Taiji Okada
IPC分类号: C07D239/545 , A61K31/505 , A61K31/513 , A61P35/00 , C07D307/88 , C07D405/04 , C07D405/14
CPC分类号: C07D405/04
摘要: The present invention relates to novel N-phthalidyl-5-fluorouracil derivatives represented by the general formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents phthalidyl group ##STR2## (wherein R.sub.3 is a hydrogen atom, a halogen atom or a group selected from alkoxyl groups or alkyl groups) and the other represents a hydrogen atom, an acyl group or a cyclic ether group; ##STR3## (wherein n is 1 or 2) or R.sub.1 and R.sub.2 represent the same phthalidyl group; ##STR4## (wherein R.sub.3 has the same meaning as that defined above) and provides a compound which has antitumor activity and less toxicity and can be used as a cancerocidal agent.
摘要翻译: PCT No.PCT / JP81 / 00260 Sec。 371日期1982年5月21日 102(e)日期1982年5月21日PCT提交1981年9月30日PCT公布。 出版物WO82 / 01370 1982年4月29日。本发明涉及由通式“IMAGE”表示的新型N-邻苯二甲酰基-5-氟尿嘧啶衍生物,其中R 1和R 2中的一个表示苯酞基(其中R 3为氢原子, 卤素原子或选自烷氧基或烷基的基团),另一个表示氢原子,酰基或环醚基; (其中n为1或2)或R 1和R 2表示相同的苯酞基; (其中R3具有与上述相同的含义),并提供具有抗肿瘤活性和较低毒性并可用作杀癌剂的化合物。
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公开(公告)号:US4952560A
公开(公告)日:1990-08-28
申请号:US183307
申请日:1988-04-11
CPC分类号: A61K9/0014 , A61K47/10 , A61K47/42 , Y10S514/801 , Y10S514/947 , Y10S514/969
摘要: An ointment base for external use is provided which contains a water-soluble protein and monohydric alcohol or/and oleginous substance and additionally contains a wetting agent. The present ointment base offers a markedly improved percutaneous absorption of drugs, as compared with the conventional ointment bases.
摘要翻译: 提供了一种外用软膏基质,其含有水溶性蛋白质和一元醇或/和油酸物质,另外含有润湿剂。 与常规软膏基质相比,本发明的软膏基质提供了显着改善的药物经皮吸收。
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公开(公告)号:US4500511A
公开(公告)日:1985-02-19
申请号:US531745
申请日:1983-09-13
IPC分类号: A61K9/06 , A61K31/19 , A61K47/10 , A61K47/14 , A61K47/22 , A61K47/32 , A61K47/36 , A61K47/38 , A61P29/00
CPC分类号: A61K31/19 , A61K47/10 , A61K47/14 , A61K47/22 , A61K47/32 , A61K47/36 , A61K47/38 , A61K9/0014
摘要: An antiinflammatory and analgesic gel composition for external use which comprises 0.03 to 1.5 percent by weight of clidanac or a pharmacologically acceptable salt thereof as a pharmacologically active ingredient and 0.5 to 5.0 percent by weight of gelling agent, 0.3 to 4.0 percent by weight of a neutralizer, 30 to 60 percent by weight of a solubilizer and 35 to 65 percent by weight of water, has an excellent antiinflammatory and analgesic effect.
摘要翻译: 一种外用抗炎和止痛凝胶组合物,其包含0.03至1.5重量%的氯吡旦或其药理学上可接受的盐作为药理活性成分和0.5-5.0重量%的胶凝剂,0.3-4.0重量%的中和剂 ,30〜60重量%的增溶剂和35〜65重量%的水,具有优异的抗炎和镇痛作用。
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公开(公告)号:US4166125A
公开(公告)日:1979-08-28
申请号:US862206
申请日:1977-12-19
IPC分类号: C07D209/46 , C07D209/48 , A61K31/40
CPC分类号: C07D209/48 , C07D209/46
摘要: 2-Oxo-phenylbutanoic acid derivatives of the general formula (I) ##STR1## wherein X is amino, hydroxy or lower alkoxy, which have an anti-inflammatory activity and low toxicity, a method for the production of the said derivatives, a pharmaceutical composition containing a therapeutically effective amount of at least one compound of the said derivatives, and the use of such compounds and compositions in therapeutics.
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