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2. 发明申请

WO2017005483A1 PROCESS FOR PREPARING POLY(GLYCOLIDE-CO-LACTIDE) COPOLYMER MICROPARTICLES 审中-公开
标题翻译：制备聚（丙二醇共聚物）共聚物微球的方法
公开(公告)号：WO2017005483A1
公开(公告)日：2017-01-12
申请号：PCT/EP2016/064270
申请日：2016-06-21
申请人： EVONIK RÖHM GMBH , KIRCHNER, Andreas , LIZIO, Rosario , ROSSMEISSL, Markus Rolf , LULEY, Wolfgang , VORHOLZ, Johannes , GRIMM, Silko , SCHNEIDER, Marc
发明人： KIRCHNER, Andreas , LIZIO, Rosario , ROSSMEISSL, Markus Rolf , LULEY, Wolfgang , VORHOLZ, Johannes , GRIMM, Silko , SCHNEIDER, Marc
IPC分类号： C08G63/88 , C08J9/14 , C08J9/20
CPC分类号： C08J3/12 , A61K9/146 , A61K47/34 , C08G63/88 , C08J3/095 , C08J2367/04
摘要： The invention refers to a process for preparing poly(lactide-co-glycolide) copolymer particles with an average particle size in the range of 50 - 800 nm comprising the steps: a) transfer of ethanol and a poly(lactide-co-glycolide) copolymer with a content of polymerized monomer units of 55 - 80 mol% lactide and 20 to 45 mol% of glycolide and a molecular weight M w of 1.000 - 25.000 into a first reactor with a stirring equipment, b) feeding carbon dioxide into the first reactor so that carbon dioxide is from 65 to 85 % by weight and the ethanol is 15 to 35 % by weight wherein carbon dioxide and ethanol add up to 100%, c) mixing the poly(lactide-co-glycolide) copolymer, the ethanol and the carbon dioxide by stirring and adjusting or maintaining the mixture in the first reactor to a temperature of at least 31 and up to 70 °C and a pressure of at least 7.38 and up to 50 MPa, d) stirring the mixture from step c) for 1 to 5 hours, whereby at least a part of the poly(lactide-co-glycolide) copolymer becomes dissolved in the mixture of carbon dioxide and ethanol, e) transfer of the mixture from step d) into a second reactor under rapid reduction of the pressure and expansion with phase separation into a gas phase, an aerosol and an ethanolic suspension containing poly(lactide-co-glycolide) copolymer particles, f) removing the carbondoxide gas and the ethanol aerosol from the reactor g) obtaining the poly(glycolide-co-lactide) copolymer particles with an average particle size in the range of 50 - 800 nm in the form of an ethanolic suspension or in dry form from the second reactor.
摘要翻译：本发明涉及一种制备平均粒度在50-800nm范围内的聚（丙交酯 - 共 - 乙交酯）共聚物颗粒的方法，包括以下步骤：a）乙醇和聚（丙交酯 - 共 - 乙交酯）共聚物，其中具有55-80摩尔％丙交酯和20至45摩尔％乙交酯的聚合单体单元的含量，并且使用搅拌设备将第二反应器的分子量Mw为1.000-25.10000，b）将二氧化碳进料到第一反应器使得二氧化碳为65至85重量％，乙醇为15至35重量％，其中二氧化碳和乙醇加至100％，c）将聚（丙交酯 - 共 - 乙交酯）共聚物，乙醇和通过搅拌并将第一反应器中的混合物调节或维持至至少31℃至70℃的温度和至少7.38至高达50MPa的压力，d）搅拌并搅拌来自步骤c）的混合物， 1至5小时，由此至少一部分聚（丙交酯 - 共 - 乙交酯） olymer溶解在二氧化碳和乙醇的混合物中，e）将混合物从步骤d）转移到第二反应器中，在快速降低压力和膨胀的同时将相分离成气相，气溶胶和含有聚（丙交酯 - 共 - 乙交酯）共聚物颗粒，f）从反应器中除去碳氧烷气体和乙醇气溶胶g）获得平均粒度在50-800nm范围内的聚（乙交酯 - 共 - 丙交酯）共聚物颗粒以乙醇悬浮液的形式或来自第二反应器的干燥形式。

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