Use of a non-racemic mixture of bupivacaine enantiomers, for improving the anesthesia profile
US7700629B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 1, 2007 |
| Grant date | Apr 20, 2010 |
| Priority date | — |
| Expiry date | Jun 1, 2027 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P23/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.