首页> 外国专利> Process for obtaining the enantiomers of racemic bupivacaine, process for obtaining pharmaceutical compositions based on levobupivacaine: pharmaceutical compositions based on levobupivacaine formulated in basic forms or pharmaceutically acceptable salts and use of pharmaceutical compositions based on levobupivacaine formulated in basic forms or pharmaceutically salts acceptable

Process for obtaining the enantiomers of racemic bupivacaine, process for obtaining pharmaceutical compositions based on levobupivacaine: pharmaceutical compositions based on levobupivacaine formulated in basic forms or pharmaceutically acceptable salts and use of pharmaceutical compositions based on levobupivacaine formulated in basic forms or pharmaceutically salts acceptable

机译：获得外消旋布比卡因对映异构体的方法，获得基于左旋布比卡因的药物组合物的方法：基于左旋布比卡因的药物组合物，其以基本形式或药学上可接受的盐配制，以及基于左旋布比卡因的药物组合物的用途，其以基本形式或药学上可接受的盐配制

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"Process of obtaining the ENANTIÈMEROS OF racemic bupivacaine, PROCESS compositions of obtaining pharmaceutical BASE levobupivacaine; Pharmaceutical Compositions levobupivacaine BASE MADE IN BASIC OR SALTS FORMS pharmaceutically acceptable AND USAGE OF PHARMACEUTICAL COMPOSITIONS levobupivacaine BASE MADE IN Basic Shapes OR SALTS PHARMACEUTICALLY ACCEPTABLE ". The present invention describes a novel method of separating bupivacaine enantiomers which consists of a continuous cold separation procedure via selective precipitation of its tartaric acid diastereomers. This cold processing avoids the degradation of the reagents giving continuous processing character to the procedure. Another object of the present invention relates to enantiomeric manipulation of bupivacaine enantiomers in order to obtain pharmaceutical compositions having varying enantiomeric excesses of levobupivacaine in order to quantify and determine the participation of dextroisomer in anesthetic and cardiotoxic effects. These enantiomerically engineered compositions have been shown to show significant improvement in anesthetic properties, which have been shown to be similar to racemic bupivacaine, having a cardiotoxic profile similar to that of enantiomerically pure levobupivacaine.

机译：“获得外消旋布比卡因的ENANTIÈMEROS的过程，获得药物左旋布比卡因碱的过程组合物;以基本或盐形式制成的药物组合物左旋布比卡因碱可药用，并以基本形状或盐形式制成的药物组合物左旋布比卡因碱的用法。本发明描述了分离布比卡因对映体的新方法，该方法包括通过选择性沉淀其酒石酸非对映体而进行的连续冷分离方法。这种冷处理避免了试剂的降解，从而使程序具有连续的处理特性。本发明的另一个目的涉及布比卡因对映异构体的对映体操纵，以获得具有不同对映体过量的左旋布比卡因的药物组合物，以便定量和确定右旋异构体参与麻醉和心脏毒性作用。这些对映体工程组合物已显示出麻醉性能的显着改善，已显示与外消旋布比卡因相似，其心脏毒性特征与对映体纯左旋布比卡因相似。

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公开/公告号BR0002246A

专利类型
公开/公告日2003-04-15

原文格式PDF
申请/专利权人 CRISTALIA PRODUTOS QUIMICOS FARMACEUTICOS LTDA;
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申请/专利号BR20000002246
发明设计人 ROBERTO TAKASHI SUDO;MARIA DOS PRAZERES BARBALHO SIMONETTI;VALTER FREIRE TORRES RUSSO;ELISA MANNOCHIO DE SOUZA RUSSO;
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申请日2000-04-06
分类号A61K31/445;A61K31/4453;A61K31/4458;C07D211/30;C07D211/32;
国家 BR
入库时间 2022-08-22 00:03:56

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