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US 2005/0239831 A1Published application
Bupivacaines
AssigneeCristalia Productos Quimicos Farmaceuticos Ltda
InventorsRoberto Sudo, Valter Russo, Elisa Russo
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AssigneeCristalia Productos Quimicos Farmaceuticos Ltda
InventorsRoberto Sudo, Valter Russo, Elisa Russo
Estimating the term…
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.
A continuous process for preparing bupivacaine enantiomers in a high yield with a minimum of impurities, characterized by reacting racemic bupivacaine with a resolution agent within a medium of organic solvent at low concentration and at room temperature, wherein said resolution agent is used in an amount not lower than 0.6 molar equivalent per racemic bupivacaine molar equivalent.
Pharmaceutical compositions comprising levobupivacaine and dextrobupivacaine in a weight ratio of from 60:40 to less than 90:10.
Pharmaceutical compositions of claim 13 characterized by the fact of being used in medicine and veterinary.
A pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of from 65:35 to less than 90:10.
A pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of less than 90:10.
A pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of about 75:25.
A continuous process for producing levobupivacaine from racemic bupivacaine comprising the steps of:
A method for blocking a nerve by contacting the nerve with a pharmacologically effective amount of a pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of from 65:35 to less than 90:10.
A method for blocking a nerve by contacting the nerve with a pharmacologically effective amount of a pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of less than 90:10.
A method for blocking a nerve by contacting the nerve with a pharmacologically effective amount of a pharmaceutical composition comprising levobupivacaine and dextrobupivacaine in a weight ratio of about 75:25.
Dependencies are inferred from the claim text.