Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.

The present invention relates to an improved process for the preparation of 10-oxo-1011-dihydro-5H-dibenz[bf]azepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[bf]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of alpha-hydroxy acids and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

The present invention relates to pharmaceutical combinations of two antiepileptic substances and also to combinations of an antiepileptic and B-complex vitamins, in which the antiepileptic substances are selected from pregabalin and oxcarbazepine, and the vitamins are selected from vitamin B and vitamin B12. The invention also relates to pharmaceutical compositions containing said combinations and to the use of said compositions for treating neuropathic pain (NP).

PROBLEM TO BE SOLVED: To provide controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration.

The present invention relates to a process for the preparation of controlled-release solid oral pharmaceutical formulations of oxcarbazepine, and the pharmaceutical formulations obtainable by said process.

The present invention relates to a process for the preparation of controlled-release solid oral pharmaceutical formulations of oxcarbazepine and the pharmaceutical formulations obtainable by said process.

A process for preparing (S)-(+)-1011-dihydro-10-hydroxy-5H-dibenz/bf/azepine-5-carboxamide or (R)-(−)-1011-dihydro-10-hydroxy-5H-dibenz/bf/azepine-5-carboxamide by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine bromine or iodine and L is an aryl or aryl-aliphatic ligand with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl ...

A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alky...

CONTROLLED RELEASED PREPARATIONS OF OXCARBAZEPINE HAVING SIGMOIDAL RELEASE PROFILE Abstract Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility - and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.