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公开(公告)号：EP0576675A1
公开(公告)日：1994-01-05
申请号：EP92907107.4
申请日：1992-03-18
CPC分类号： A61K9/5078 , A61K9/1652 , A61K9/1658 , A61K9/5031
摘要： A long-acting pharmaceutical preparation comprising a core part containing a drug and a swelling agent and, formed thereon, a coating film containing a biodegradable high-molecular substance, wherein the swelling agent is contained in an amount sufficient to burst the coating film after a given period of time. This preparation allows the duration of drug release to be controlled arbitrarily and is suitable for not only oral administration but also intramuscular and sub-cutaneous administration.
摘要翻译： 一种长效药物制剂，其包含含有药物和溶胀剂的核心部分，并且在其上形成含有可生物降解的高分子物质的涂膜，其中所述溶胀剂的含量足以使所述涂膜破裂后的量 给定一段时间。 该制剂允许任意地控制药物释放的持续时间，并且不仅适用于口服给药，而且适用于肌内和皮下给药。
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公开(公告)号：EP0943327A1
公开(公告)日：1999-09-22
申请号：EP97946111.8
申请日：1997-12-05
发明人： HATA, Takehisa , TOKUNAGA, Yuji , SHIMOJO, Fumio , KIMURA, Sumihisa , HIROSE, Takeo , UEDA, Satoshi
IPC分类号： A61K9/14 , A61K31/335
摘要： To provide a pharmaceutical composition comprising a water-insoluble active substance, surfactant(s) and solid carrier(s), which is improved in dissolution and oral absorption characteristics.
摘要翻译： 提供包含水溶性活性物质，表面活性剂和固体载体的药物组合物，其溶出度和口服吸收特性得到改善。
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公开(公告)号：EP0669127B1
公开(公告)日：1999-08-11
申请号：EP93924826.6
申请日：1993-11-11
IPC分类号： A61K9/16 , A61K31/395 , C07D498/18
CPC分类号： C07D498/18 , A61K9/1647 , A61K31/436
摘要： A prolonged-action pharmaceutical preparation comprising a macrocyclic compound represented by 17-alkyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04.9]octa-cos-18-ene-2,3,10,16-tetrone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04.9]octa-cos-18-ene-2,3,10,16-tetrone enclosed in a so-called microsphere, i.e., a fine particle of a biodegradable macromolecular substance. When this preparation is administered in the form of a parenteral solution, the macrocyclic compound can very well migrate in the blood. Further it is suited for topical administration.
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公开(公告)号：EP0978288A1
公开(公告)日：2000-02-09
申请号：EP98911222.2
申请日：1998-04-07
发明人： SHIMOJO, Fumio , KIMURA, Sumihisa , HIROSE, Takeo , UEDA, Satoshi , IBUKI, Rinta , OHNISHI, Norio
IPC分类号： A61K47/14
CPC分类号： A61K31/436 , A61K9/4866 , A61K47/14 , A61K47/44
摘要： A medicinal composition excellent in drug release properties and oral absorbability, characterized by comprising a drug sparingly soluble in water and two or more surfactants, at least one of which serves as a solvent in which the drug and the other surfactant(s) have been dissolved.
摘要翻译： 药物释放性和口服吸收性优异的药物组合物，其特征在于含有微溶于水的药物和2种以上的表面活性剂，其中至少一种作为其中溶解有药物和其它表面活性剂的溶剂 。
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公开(公告)号：EP0669127A1
公开(公告)日：1995-08-30
申请号：EP93924826.6
申请日：1993-11-11
IPC分类号： A61K9/16 , A61K31/395 , C07D498/18
CPC分类号： C07D498/18 , A61K9/1647 , A61K31/436
摘要： A prolonged-action pharmaceutical preparation comprising a macrocyclic compound represented by 17-alkyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4.9 ]octa-cos-18-ene-2,3,10,16-tetrone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycycolhexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4- azatricyclo[22.3.1.0 4.9 ]octa-cos-18-ene-2,3,10,16-tetrone enclosed in a so-called microsphere, i.e., a fine particle of a biodegradable macromolecular substance. When this preparation is administered in the form of a parenteral solution, the macrocyclic compound can very well migrate in the blood. Further it is suited for topical administration.
摘要翻译： 包含由17-烷基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基-13代表的大环化合物的长效药物制剂， 19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04.9]八-cos-18-烯-2,3,10,16-四酮或17-乙基-1,14-二氮杂 - （2,2-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基-13,19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[ 1.04.9]八聚-18-烯-2,3,10,16-四酮，其被封入所谓的微球中，即可生物降解的大分子物质的微粒。 当该制剂以肠胃外溶液的形式给药时，大环化合物可非常好地在血液中迁移。 此外，它适用于局部用药。
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公开(公告)号：EP0719561A1
公开(公告)日：1996-07-03
申请号：EP94923065.0
申请日：1994-08-04
发明人： ASAKURA, Sotoo 10-18, Ooenishishinbayashi-cho , KIMURA, Sumihisa , KADO, Kazutake , OHISHI, Yoshiko , HATA, Takehisa
IPC分类号： A61K47/12
CPC分类号： A61K38/12 , A61K9/0014 , A61K38/05 , A61K47/12 , A61K47/14 , Y10S514/944
摘要： A percutaneously absorbable preparation containing a drug and a percutaneous absorption accelerator comprising a monoglyceride and a fatty acid.
摘要翻译： 一种含有包含单酸甘油酯和脂肪酸的药物和经皮吸收促进剂的经皮吸收制剂。
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公开(公告)号：EP0338081A1
公开(公告)日：1989-10-25
申请号：EP88908344.0
申请日：1988-09-21
发明人： UEDA, Yoshio , HATA, Takehisa , KIMURA, Sumihisa , KOHNO, Yutaka
CPC分类号： A61K9/0031
摘要： An oily rectal instillation comprising a water-soluble drug, a dispersing agent and a surfactant with an HLB value of 10 or more. It can prevent sedimentation of a water-soluble drug in an injector even when the concentration of the water-soluble drug or the dispersing agent is high, and is easy to fill in the injector and to inject to patients. In addition, the water-soluble drug and metabolic antagonists thereof have good stability and absorbability.
ABSTRACT
Oily preparation for intrarectal infusion Contains water-soluble drug, dispersing agent and surfactant in which HLB value is 10 or more.
It can prevent the water-soluble drug from precipitating in the container for infusion, even in case that the concentration of the water-soluble drug and/or the dispersing agent is high, and can easily be filled in the container for infusion and can easily be administered to the patient, and further the stability and the bioavailability of the water-soluble drug and its matabolic inhibitor in the preparation are both good.摘要翻译： 包含水溶性药物，分散剂和HLB值为10或更高的表面活性剂的油性直肠滴注剂。 即使当水溶性药物或分散剂的浓度高时，也能够防止注射器中水溶性药物的沉降，并且容易填充注射器并向患者注射。 另外，水溶性药物及其代谢拮抗剂具有良好的稳定性和吸收性。 摘要直肠内输液用油性制剂含有HLB值为10以上的水溶性药物，分散剂和表面活性剂。 即使在水溶性药物和/或分散剂的浓度高，并且容易填充到输液用容器中的情况下，也能够防止水溶性药剂在输液用容器中析出 给予患者，并且制剂中水溶性药物及其代谢抑制剂的稳定性和生物利用度都是好的。
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