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Use of a non-racemic mixture of bupivacaine enantiomers, for improving the anesthesia profile

机译:布比卡因对映异构体的非外消旋混合物用于改善麻醉状况的用途

摘要

The present invention describes a new method for the separation of bupivacaine enantiomers consisting in a continuous separation process performed without heating, by the selective precipitation of their diastereomeric salts with tartaric acid. This heatless process avoids the degradation of the reagents granting a continuous process feature to the procedure.;Another embodiment of the present invention is related to the enantiomeric manipulation of bupivacaine enantiomers in order to obtain pharmaceutical compositions presenting several enantiomeric excess of levobupivacaine to quantify and determinate the role of the dextrobupivacaine on its anesthetic and cardiotoxic effects. These enantiomeric manipulated compositions showed to present an expressive improvement on its anesthetic properties that had shown to be similar to racemic bupivacaine presenting a cardiotoxic profile similar to enantiomeric pure levobupivacaine.
机译:本发明描述了一种新的布比卡因对映体的分离方法,该方法包括在不加热的情况下通过用酒石酸选择性沉淀其非对映体盐而进行的连续分离过程。该无热过程避免了试剂的降解,从而赋予了该方法连续的过程特征。本发明的另一个实施方案涉及布比卡因对映异构体的对映体操作,以获得具有几种对映体过量的左旋布比卡因的药物组合物以定量和确定右旋布比卡因对其麻醉和心脏毒性作用的作用。这些对映体操纵的组合物显示出其麻醉性能的表达改善,已显示出与外消旋布比卡因相似,表现出与对映体纯左旋布比卡因相似的心脏毒性。

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