公开(公告)号：WO2010000879A3

公开(公告)日：2010-04-08

申请号：PCT/EP2009064555

申请日：2009-11-03

申请人： EVULTIS SA ,  MAZZOLA ALESSANDRO ,  MOIANA SILVIA

发明人： MAZZOLA ALESSANDRO ,  MOIANA SILVIA

IPC分类号： C07C51/47 ,  C07C66/02 ,  C07C69/157

CPC分类号： C07C51/47 ,  C07C51/412 ,  C07C67/56 ,  C07C66/02 ,  C07C69/017 ,  C07C69/16

摘要： The present invention is directed to a process for producing non-genotoxic Diacetylrhein (Diacerein), comprising: i) transformation of raw Diacerein (or raw Rhein), into a water-soluble salt; ii) adsorption of the salt Diacerein (or Rhein) solution on a hydrophobic resin; iii) washing with an appropriate solvent to eliminate the impurities (in particular the genotoxic impurities); iv) elution to recover Diacereinor Rhein; v) if the process is applied to Rhein, its transformation to Diacerein by acetylation; vi) acidification of purified Diacerein and its recovery, and drying. The invention is also directed to non-genotoxic Diacerein obtained by the process of the invention, in which the total content of genotoxic impurities is below 1ppm, and suitable for the preparation of pharmaceutical formulations, in particular capsules, for human and veterinary use, in agreement with the current Health Authorities request.

摘要翻译： 本发明涉及生产无基因毒性的二乙酰纤维素（双醋瑞因）的方法，包括：i）将原始双醋瑞因（或生大黄酸）转化为水溶性盐; ii）盐双醋瑞因（或大黄酸）溶液在疏水性树脂上的吸附; iii）用合适的溶剂洗涤以消除杂质（特别是遗传毒性杂质）; iv）洗脱以回收Diacereinor Rhein; v）如果该过程应用于Rhein，则其通过乙酰化转化为双醋瑞因; vi）纯化的双醋瑞因的酸化及其回收和干燥。 本发明还涉及通过本发明方法获得的非基因毒性的双醋柳黄素，其中基因毒性杂质的总含量低于1ppm，并且适用于制备用于人和兽医用途的药物制剂，特别是胶囊 与当前的卫生当局请求达成一致。

公开(公告)号：WO2012156533A1

公开(公告)日：2012-11-22

申请号：PCT/EP2012/059404

申请日：2012-05-21

申请人： FRIULCHEM SPA ,  MAZZOLA, Disma ,  MOIANA, Silvia ,  COPPI, Germano

发明人： MAZZOLA, Disma ,  MOIANA, Silvia ,  COPPI, Germano

IPC分类号： C07D498/22 ,  A61K31/437 ,  A61P31/04

CPC分类号： C07D498/22

摘要： Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo- crystalline form of rifaximin with fewer impurities obtained thereby.

摘要翻译： 用于制备利福昔明，假结晶利福昔明和利福昔明的新型假晶体形式的方法，由此获得的杂质较少。

公开(公告)号：WO2012155981A1

公开(公告)日：2012-11-22

申请号：PCT/EP2011/058171

申请日：2011-05-19

申请人： FRIULCHEM SPA ,  MAZZOLA, Disma ,  MOIANA, Silvia ,  COPPI, Germano

发明人： MAZZOLA, Disma ,  MOIANA, Silvia ,  COPPI, Germano

IPC分类号： C07D498/22 ,  A61K31/437 ,  A61P31/04

CPC分类号： C07D498/22

摘要： Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby.

摘要翻译： 用于制备利福昔明，假结晶利福昔明和新型假结晶形式的利福昔明的方法，由此获得的杂质较少。

公开(公告)号：WO2010000879A2

公开(公告)日：2010-01-07

申请号：PCT/EP2009/064555

申请日：2009-11-03

申请人： EVULTIS SA ,  MAZZOLA, Alessandro ,  MOIANA, Silvia

发明人： MAZZOLA, Alessandro ,  MOIANA, Silvia

CPC分类号： C07C51/47 ,  C07C51/412 ,  C07C67/56 ,  C07C66/02 ,  C07C69/017 ,  C07C69/16

摘要： The present invention is directed to a process for producing non-genotoxic Diacetylrhein (Diacerein), comprising: i) transformation of raw Diacerein (or raw Rhein), into a water-soluble salt; ii) adsorption of the salt Diacerein (or Rhein) solution on a hydrophobic resin; iii) washing with an appropriate solvent to eliminate the impurities (in particular the genotoxic impurities); iv) elution to recover Diacereinor Rhein; v) if the process is applied to Rhein, its transformation to Diacerein by acetylation; vi) acidification of purified Diacerein and its recovery, and drying. The invention is also directed to non-genotoxic Diacerein obtained by the process of the invention, in which the total content of genotoxic impurities is below 1ppm, and suitable for the preparation of pharmaceutical formulations, in particular capsules, for human and veterinary use, in agreement with the current Health Authorities request.

摘要翻译： 本发明涉及一种生产非遗传毒性的二乙酰胆碱（Diacerein）的方法，其包括：i）将生的双醋瑞因（或生的大黄酸​​）转化成水溶性盐; ii）盐将双醋瑞因（或大黄酸）溶液吸附在疏水性树脂上; iii）用适当的溶剂洗涤以除去杂质（特别是基因毒性杂质）; iv）洗脱以恢复大鼠精氨酸酯; v）如果该过程适用于莱茵，则其通过乙酰化转化为双醋瑞因; vi）纯化的Diacerein的酸化及其回收，并干燥。 本发明还涉及通过本发明方法获得的非遗传毒性双醋瑞因，其中基因毒性杂质的总含量低于1ppm，并且适用于制备用于人和兽医用途的药物制剂，特别是胶囊 与当前卫生当局的要求达成一致。