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1.发明授权1-hydroxy-oxo-5H-pyrido(3,2-a)phenoxazine-3-carboxylic acid esters 失效1-羟基 - 氧代-5H-吡啶并（3,2-a）吩恶嗪-3-甲酸酯
公开(公告)号：US4820837A
公开(公告)日：1989-04-11
申请号：US68159
申请日：1987-06-30
申请人： Hideo Terayama , Jun Inoue
发明人： Hideo Terayama , Jun Inoue
IPC分类号： C07D498/06 , A61K31/4738 , A61K31/535 , A61K31/538 , A61P27/02 , A61P27/12 , C07D498/04
CPC分类号： C07D498/04
摘要： The compounds represented by the general formula ##STR1## wherein R is an alkyl group having 1-10 carbon atoms are novel compounds which have not been reported in the literature. Since they have excellent affinities for tissues with particular high corneal permeability and show anticataract activity at low concentration, the compounds are of value as prophylactic and therapeutic agents for cataracts.
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公开(公告)号：US4728509A
公开(公告)日：1988-03-01
申请号：US893161
申请日：1986-08-05
IPC分类号： A61K31/435 , A61K9/06 , A61K9/08 , A61K31/455 , A61K47/00 , A61K47/22 , A61K47/32 , A61K47/40 , A61P27/02 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/08 , C07D491/052 , A61K31/44 , A61K31/78
CPC分类号： A61K31/455 , A61K47/22 , A61K47/32 , A61K47/40
摘要： In the aqueous liquid preparation of this invention, which comprises a compound of the formula; ##STR1## wherein R is an alkyl having 1-6 carbon atoms, and at least one species of the solubilizers selected from the group consisting of polyvinylpyrrolidone, cyclodextrin and caffeine, the solubility of the compound in water can be heightened and the aqueous liquid prepared thereby can afford a desired stability and mitigate eye-irritation or nose-irritation.
摘要翻译： 在本发明的含水液体制剂中，其包含下式的化合物： 其中R是具有1-6个碳原子的烷基，以及选自聚乙烯吡咯烷酮，环糊精和咖啡因的至少一种增溶剂，可以提高化合物在水中的溶解度，并且制备含水液体 从而可以提供所需的稳定性并减轻眼刺激或鼻刺激。
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公开(公告)号：US06683070B2
公开(公告)日：2004-01-27
申请号：US10189400
申请日：2002-07-08
IPC分类号： A61K3156
CPC分类号： A61K9/0019 , A61K9/0014 , A61K9/0043 , A61K9/0048 , A61K9/08 , A61K47/32 , A61K47/38 , Y10S514/846 , Y10S514/912 , Y10S514/914 , Y10S514/937
摘要： The aqueous suspension can be prepared by incorporating, in an aqueous suspension of a hardly soluble drug, a water-soluble polymer within the concentration range from the concentration at which the surface tension of the aqueous suspension of the drug begins to decrease up to the concentration at which the reduction in surface tension ceases. The resulting aqueous suspension shows ready redispersibility and will not undergo aggregation of dispersed particles or caking. Because of its good redispersibility, the suspension is useful as a parenteral preparation, eye drops, nasal drops, a preparation for oral administration, a lotion or the like.
摘要翻译： 水性悬浮液可以通过在难溶性药物的水性悬浮液中掺入水溶性聚合物，其浓度范围从药物的水性悬浮液的表面张力开始降低至浓度的浓度 表面张力的降低停止。 所得水悬浮液显示出可再分散性，并且不会发生分散颗粒的聚集或结块。 由于其良好的再分散性，悬浮液可用作肠胃外制剂，滴眼剂，滴鼻剂，口服制剂，洗剂等。
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公开(公告)号：US06448296B2
公开(公告)日：2002-09-10
申请号：US09873348
申请日：2001-06-05
IPC分类号： A61K4700
CPC分类号： A61K9/0019 , A61K9/0014 , A61K9/0043 , A61K9/0048 , A61K9/08 , A61K47/32 , A61K47/38 , Y10S514/846 , Y10S514/912 , Y10S514/914 , Y10S514/937
摘要： The aqueous suspension can be prepared by incorporating, in an aqueous suspension of a hardly soluble drug, a water-soluble polymer within the concentration range from the concentration at which the surface tension of the aqueous suspension of the drug begins to decrease up to the concentration at which the reduction in surface tension ceases. The resulting aqueous suspension shows ready redispersibility and will not undergo aggregation of dispersed particles or caking. Because of its good redispersibility, the suspension is useful as a parenteral preparation, eye drops, nasal drops, a preparation for oral administration, a lotion or the like.
摘要翻译： 水性悬浮液可以通过在难溶性药物的水性悬浮液中掺入水溶性聚合物，其浓度范围从药物的水性悬浮液的表面张力开始降低至浓度的浓度 表面张力的降低停止。 所得水悬浮液显示出可再分散性，并且不会发生分散颗粒的聚集或结块。 由于其良好的再分散性，悬浮液可用作肠胃外制剂，滴眼剂，滴鼻剂，口服制剂，洗剂等。
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公开(公告)号：US06274634B1
公开(公告)日：2001-08-14
申请号：US09423558
申请日：1999-11-10
IPC分类号： A61K3156
CPC分类号： A61K9/0019 , A61K9/0014 , A61K9/0043 , A61K9/0048 , A61K9/08 , A61K47/32 , A61K47/38 , Y10S514/846 , Y10S514/912 , Y10S514/914 , Y10S514/937
摘要： The aqueous suspension can be prepared by incorporating, in an aqueous suspension of a hardly soluble drug, a water-soluble polymer within the concentration range from the concentration at which the surface tension of the aqueous suspension of the drug begins to decrease up to the concentration at which the reduction in surface tension ceases. The resulting aqueous suspension shows ready redispersibility and will not undergo aggregation of dispersed particles or caking. Because of its good redispersibility, the suspension is useful as a parenteral preparation, eye drops, nasal drops, a preparation for oral administration, a lotion or the like.
摘要翻译： 水性悬浮液可以通过在难溶性药物的水性悬浮液中掺入水溶性聚合物，其浓度范围从药物的水性悬浮液的表面张力开始降低至浓度的浓度 表面张力的降低停止。 所得水悬浮液显示出可再分散性，并且不会发生分散颗粒的聚集或结块。 由于其良好的再分散性，悬浮液可用作肠胃外制剂，滴眼剂，滴鼻剂，口服制剂，洗剂等。
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公开(公告)号：US5916550A
公开(公告)日：1999-06-29
申请号：US035094
申请日：1998-03-05
申请人： Katsuhiro Inada , Hideo Terayama
发明人： Katsuhiro Inada , Hideo Terayama
CPC分类号： A61K9/0048 , A61K31/56 , A61K47/183 , A61K9/0043
摘要： The conventional aqueous suspension of loteprednol etabonate is not easily amenable to production pH control and entails a pH depression on long-term storage, thus irritating the eye or the nasal mucosa on instillation.When a C2-7 aliphatic amino acid is added to an aqueous suspension of loteprednol etabonate for topical ophthalmic use, the suspension does not undergo pH depression even on prolonged storage, with the result that no irritable response is elicited in the eye or nasal mucosa.
摘要翻译： 百草酚乙酸酯的常规水悬浮液不易于生产pH控制，并且在长期储存时需要pH抑制，因此在滴注时刺激眼睛或鼻粘膜。 当将C2-7脂肪族氨基酸加入到用于局部眼用药物的百吗泼尼酯的水性悬浮液中时，即使长时间保存，悬浮液也不会经历pH抑制，结果在眼睛或鼻粘膜中不引起易怒的反应。
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公开(公告)号：US4822823A
公开(公告)日：1989-04-18
申请号：US10534
申请日：1987-02-03
申请人： Yujiro Yamamoto , Hideo Terayama , Yasushi Morita
发明人： Yujiro Yamamoto , Hideo Terayama , Yasushi Morita
IPC分类号： A61K9/00 , A61K9/08 , A61K9/70 , A61K31/12 , A61K45/00 , A61K47/00 , A61K47/40 , A61P11/00 , A61P27/02 , A61P27/14 , A61P27/16 , A61P37/08 , A61P43/00 , C07C50/28
CPC分类号： A61K47/40 , A61K31/12 , A61K9/0043 , A61K9/0048 , A61K9/703 , A61K9/7084
摘要： This invention relates to an aqueous preparation comprising a compound (A) represented by the formula: ##STR1## and at least one of cyclodextrins selected from .alpha.-cyclodextrin and dimethyl-.beta.-cyclodextrin; and a method of preparation thereof.According to the aqueous preparation of this invention, coexistence with at least one medicament selected from .alpha.-cyclodextrin and dimethyl-.beta.-cyclodextrin allows to enhance the solubility to water of compound (A) essential in this invention to such a concentration that makes an expected curative effect available and to inpart a desired stability to it. As a consequence, the aforesaid compound (A) can be utilized as a medicament for an aqueous preparation having anti-allergy action.
摘要翻译： 本发明涉及含有由下式表示的化合物（A）的水性制剂和至少一种选自α-环糊精和二甲基-β-环糊精的环糊精; 及其制备方法。 根据本发明的水性制剂，与至少一种选自α-环糊精和二甲基-β-环糊精的药物共存允许增强本发明中必需的化合物（A）对水的溶解度，使其达到预期的浓度 可用的治疗效果和对其的期望的稳定性。 因此，上述化合物（A）可以用作具有抗过敏作用的水性制剂的药物。
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公开(公告)号：US4780465A
公开(公告)日：1988-10-25
申请号：US52576
申请日：1987-05-20
申请人： Kazumi Ogata , Hideo Terayama , Satoshi Takei
发明人： Kazumi Ogata , Hideo Terayama , Satoshi Takei
IPC分类号： A61K31/445 , A61K9/00 , A61K9/08 , A61K31/4427 , A61K31/495 , A61P31/04 , C07D401/04 , A61K31/50
CPC分类号： A61K31/495 , A61K9/0048
摘要： A stable isotonic aqueous solution of the compound 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid, or a pharmaceutically-acceptable salt thereof, having a pH of 3 to 6.5 and isotonized with a polyalcohol or boric acid is disclosed.
摘要翻译： 化合物1-乙基-6,8-二氟-1,4-二氢-7-（3-甲基-1-哌嗪基）-4-氧代喹啉线-3-羧酸的稳定的等渗水溶液， 公开了其pH为3至6.5并与多元醇或硼酸等渗的其可接受的盐。
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