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公开(公告)号：US09345651B2
公开(公告)日：2016-05-24
申请号：US13981170
申请日：2012-01-24
CPC分类号： A61K8/44 , A61K8/062 , A61K2800/21 , A61Q19/02
摘要： Disclosed is an oil-in-water type emulsion composition containing a physiologically acceptable salt of a tranexamate ester and a method for producing the same. An oil-in-water type emulsion composition containing a physiologically acceptable salt of a tranexamate ester can be obtained by preparing an oil phase including: A) a physiologically acceptable salt of a tranexamate ester; B) an amphiphilic substance; C) an oily substance; and D) water, a water-soluble organic solvent or a mixture thereof wherein the weight ratio of the ingredients A:B is in the range of 1:0.5 to 1:2.5, the weight ratio of the ingredients A:C is in the range of 1:1 to 1:5.0, and the weight ratio of the ingredients A:D is 1:0.2 to 1:5.0, and adding the oil phase to a water phase including E) water, a water-soluble organic solvent or a mixture thereof.
摘要翻译： 本发明公开了一种含有氨基甲酸酯酯的生理学上可接受的盐的水包油型乳剂组合物及其制造方法。 含有氨甲酯酯的生理学上可接受的盐的水包油型乳剂组合物可以通过制备油相得到，该油相包括：A）氨基甲酸酯的生理学上可接受的盐; B）两亲物质; C）油性物质; 和D）水，水溶性有机溶剂或其混合物，其中成分A:B的重量比在1:0.5至1:2.5的范围内，成分A：C的重量比在 范围为1：1至1：5.0，成分A：D的重量比为1:0.2至1:5.0，并将油相加入到包含E）水，水溶性有机溶剂或 它们的混合物。
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公开(公告)号：US08647650B2
公开(公告)日：2014-02-11
申请号：US13514623
申请日：2010-12-03
CPC分类号： A61K8/044 , A61K8/0241 , A61K8/44 , A61K2800/412 , A61K2800/652 , A61Q19/02 , C07C227/42 , C07C2601/14 , Y10T428/2982 , C07C229/46
摘要： A method for producing a composition for external use containing a physiologically acceptable salt of a tranexamate as an active ingredient, which is dispersed in the composition in the state of fine particles, includes dissolving a physiologically acceptable salt of the tranexamate in a solvent to prepare a solution, to which a salting-out agent is added to precipitate the salt. Such salt is so dispersed in a composition for external use in the state of fine particles, that the tranexamate salt can be mixed without using a large amount of an oil component to obtain a composition for external use affording excellent feel of use and stability.
摘要翻译： 包含以细颗粒状态分散在组合物中的含有作为活性成分的作为有效成分的氨基甲酸酯的生理学上可接受的盐的外用组合物的制造方法包括将溶剂中的生理上可接受的盐酸盐溶解在溶剂中， 溶液，加入盐析剂以沉淀盐。 这样的盐分散在细粒状态的外用组合物中，可以在不使用大量油性成分的情况下混合氨甲磺酸盐，得到外用的使用感和稳定性的组合物。
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公开(公告)号：US20130302391A1
公开(公告)日：2013-11-14
申请号：US13981170
申请日：2012-01-24
CPC分类号： A61K8/44 , A61K8/062 , A61K2800/21 , A61Q19/02
摘要： Disclosed is an oil-in-water type emulsion composition containing a physiologically acceptable salt of a tranexamate ester and a method for producing the same. An oil-in-water type emulsion composition containing a physiologically acceptable salt of a tranexamate ester can be obtained by preparing an oil phase including: A) a physiologically acceptable salt of a tranexamate ester; B) an amphiphilic substance; C) an oily substance; and D) water, a water-soluble organic solvent or a mixture thereof wherein the weight ratio of the ingredients A:B is in the range of 1:0.5 to 1:2.5, the weight ratio of the ingredients A:C is in the range of 1:1 to 1:5.0, and the weight ratio of the ingredients A:D is 1:0.2 to 1:5.0, and adding the oil phase to a water phase including E) water, a water-soluble organic solvent or a mixture thereof.
摘要翻译： 本发明公开了一种含有氨基甲酸酯酯的生理学上可接受的盐的水包油型乳剂组合物及其制造方法。 含有氨甲酯酯的生理学上可接受的盐的水包油型乳剂组合物可以通过制备油相得到，该油相包括：A）氨基甲酸酯的生理学上可接受的盐; B）两亲物质; C）油性物质; 和D）水，水溶性有机溶剂或其混合物，其中成分A:B的重量比在1:0.5至1:2.5的范围内，成分A：C的重量比在 范围为1：1至1：5.0，成分A：D的重量比为1:0.2至1:5.0，并将油相加入到包含E）水，水溶性有机溶剂或 它们的混合物。
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4.发明申请METHOD FOR PRODUCING COMPOSITION FOR EXTERNAL USE CONTAINING PHYSIOLOGICALLY ACCEPTABLE SALT OF TRANEXAMATE 有权用于生产含有生理学上可接受的盐酸盐的外用组合物的方法公开(公告)号：US20130142741A1
公开(公告)日：2013-06-06
申请号：US13814549
申请日：2011-07-15
CPC分类号： A61K8/8152 , A61K8/0295 , A61K8/41 , A61K8/73 , A61K8/84 , A61K2800/49 , A61K2800/805 , A61Q19/02
摘要： A composition for external use containing a tranexamate as an active ingredient with suppressed sticky or oily feeling but having a fresh feel of use, and a method for producing the same. A tranexamate salt can be dispersed stably in an aqueous medium by (a) dissolving the tranexamate salt and an amphiphilic polymer in water, a water-soluble organic solvent or a mixture thereof; and (b) adding a mixed solution obtained in the step (a) to an aqueous medium, and thus keeping the tranexamate salt in molecular assembly particles formed of the amphiphilic polymer.
摘要翻译： 一种外用组合物及其制造方法，其中含有以氨基甲酸酯为活性成分的具有抑制的粘稠或油腻感，但具有清新的使用感的组合物。 （a）将氨甲酯盐和两亲性聚合物溶于水，水溶性有机溶剂或其混合物中，稳定地分散在水性介质中; 和（b）将在步骤（a）中获得的混合溶液加入到水性介质中，从而将氨甲酯盐保持在由两亲性聚合物形成的分子组装颗粒中。
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公开(公告)号：US09833401B2
公开(公告)日：2017-12-05
申请号：US13814549
申请日：2011-07-15
CPC分类号： A61K8/8152 , A61K8/0295 , A61K8/41 , A61K8/73 , A61K8/84 , A61K2800/49 , A61K2800/805 , A61Q19/02
摘要： A composition for external use containing a tranexamate as an active ingredient with suppressed sticky or oily feeling but having a fresh feel of use, and a method for producing the same. A tranexamate salt can be dispersed stably in an aqueous medium by (a) dissolving the tranexamate salt and an amphiphilic polymer in water, a water-soluble organic solvent or a mixture thereof; and (b) adding a mixed solution obtained in the step (a) to an aqueous medium, and thus keeping the tranexamate salt in molecular assembly particles formed of the amphiphilic polymer.
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公开(公告)号：US20120244204A1
公开(公告)日：2012-09-27
申请号：US13514623
申请日：2010-12-03
IPC分类号： A61K31/215 , C07C211/17 , A61Q19/08 , A61K8/04 , A61Q19/00
CPC分类号： A61K8/044 , A61K8/0241 , A61K8/44 , A61K2800/412 , A61K2800/652 , A61Q19/02 , C07C227/42 , C07C2601/14 , Y10T428/2982 , C07C229/46
摘要： A method for producing a composition for external use containing a physiologically acceptable salt of a tranexamate as an active ingredient, which is dispersed in the composition in the state of fine particles, includes dissolving a physiologically acceptable salt of the tranexamate in a solvent to prepare a solution, to which a salting-out agent is added to precipitate the salt. Such salt is so dispersed in a composition for external use in the state of fine particles, that the tranexamate salt can be mixed without using a large amount of an oil component to obtain a composition for external use affording excellent feel of use and stability.
摘要翻译： 包含以细颗粒状态分散在组合物中的含有作为活性成分的作为有效成分的氨基甲酸酯的生理学上可接受的盐的外用组合物的制造方法包括将溶剂中的生理上可接受的盐酸盐溶解在溶剂中， 溶液，加入盐析剂以沉淀盐。 这样的盐分散在细粒状态的外用组合物中，可以在不使用大量油性成分的情况下混合氨甲磺酸盐，得到外用的使用感和稳定性的组合物。
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