Abstract: The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1% by weight as determined by high performance liquid chromatography (HPLC).
Abstract: The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.
Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
Type:
Application
Filed:
November 6, 2009
Publication date:
March 4, 2010
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
Abstract: The present invention relates to the process for the preparation of compounds of formula (I) having an ACE inhibitory action wherein carboxy group of stereospecific amino acid is activated with an uranium salt in the presence of an aprotic solvent and an activated amino acid is further transformed with appropriate amine into ACE inhibitor or its precursor.
Abstract: The present invention provides a stable pharmaceutical composition comprising an inclusion complex of perindopril, a microcrystalline cellulose having a low moisture content and/or a silicified microcrystalline cellulose having a low moisture content, and optionally other pharmaceutically acceptable excipients.
Abstract: In the present invention, a new pharmaceutical formulation of bursting pellets comprising in the core a high dose of a low potency active substance which is poorly soluble in water is described. Release of the active substance from the core takes place within minutes.
Type:
Application
Filed:
December 21, 2006
Publication date:
February 11, 2010
Applicant:
LEK Pharmaceuticals D.D.
Inventors:
Polonca Kuhar, Peter Svete, Judita Sirca
Abstract: The invention relates to the synthetic gene coding for hG-CSF which enables expression in E. coli with an improved expression level of the recombinant hG-CSF regarding the total cellular proteins after expression.
Abstract: There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
Abstract: The present invention relates to a new process for the preparation of pure perindopril erbumine. The present invention also relates to a new process for the preparation of crystalline form D of perindopril erbumine.
Abstract: 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2?-cyanobiphenyl or 4?-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
Type:
Application
Filed:
March 30, 2006
Publication date:
December 24, 2009
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Anton Copar, Ljubomic Antoncic, Matej Antoncic
Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8?-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction.
Type:
Grant
Filed:
December 11, 2003
Date of Patent:
December 15, 2009
Assignee:
Lek Pharmaceuticals d.d.
Inventors:
Igor Krisch, Marko Zivin, Natasa Milivojevic, Rudolf Rucman, Breda Bole-Vunduk, Uros Urleb
Abstract: The present invention relates to multiple unit tablets comprising multiple units compacted together with at least two tablet filler-binders and optionally other pharmaceutically acceptable excipients, wherein at least one of said tablet filler-binder is a tablet filler-binder having mean particle size-to-mean multiple unit size ratio from 10% to 40%, and at least one of said tablet filler-binder is a tablet filler-binder having mean particle size-to-mean multiple unit size ratio from 1% to 10%. The present invention further relates to process for the preparation of multiple unit tablets.
Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, and some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The aforementioned active substances may be destabilized by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions.
Abstract: A pharmaceutical composition comprising an ester of 4-(1-hydroxy-1-methylethyl)-2 propyl-1-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid characterized in that when exposed to 75% relative humidity at 40° in open dish for one month the total amount of related substances does not increase more than 1% is described.
Type:
Application
Filed:
May 2, 2007
Publication date:
September 24, 2009
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Matej Avanzo, Tanja Rozman Peterka, Igor Legen
Abstract: A novel process for the preparation of 1?-hydroxy-2?-substituted cyclohexyl azetidin-2-one compound of formula 2, which is important intermediate in the synthesis of trinems, is described by epoxide ring opening of (3S,4R)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-4-[(1?R,2?S,3?R)-1?,2?-epoxycyclohexan-3?-yl]azetidin-2-one of formula 1 with the nucleophile compound of formula RYH, where nucleophile may act as solvent itself if the nucleophile is in the liquid form, in a suitable solvent and in the presence of a suitable catalyst from the group of salt of trifluoromethane sulfonic acid, preferably ytterbium (III) trifluoromethanesulfonate, stannous (II) trifluoromethanesulfonate or dysprosium (III) trifluoromethanesulfonate, under a) ultrasonic irradiation or b) under microwave irradiation of the reaction mixture following by isolation and purification of the desired compound.
Abstract: The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent. The present invention also relates to novel crystalline omeprazole sodium form E and crystalline omeprazole sodium form F as well to the processes for their preparation as well, both with considerably low levels of residual solvents. Omeprazole sodium form A and both novel crystalline forms omeprazole sodium form E and form F are useful for the treatment of gastrointestinal disorders.
Type:
Application
Filed:
June 7, 2006
Publication date:
September 3, 2009
Applicant:
LEK Pharmaceuticals D.D
Inventors:
Lidija Vranicar Savanovic, Zoran Ham, Janez Rzen
Abstract: A sustained release pharmaceutical composition comprising coating comprising at least one water-insoluble permeable polymer and at least one water soluble polymer and homogenous cores containing only tolterodine or a salt thereof and microcrystalline cellulose is described.
Abstract: New form of irbesartan having favourable chargeability is prepared from the alcoholic/etheric or ketonic solution of irbesartan after slow cooling with sporadic or light agitation and alternatively new crystalline form of an acid addition salt of irbesartan is prepared from the aqueous solution of a sodium salt of irbesartan after strongly acidifying aforesaid solution and subsequently adjusting pH with an alkali. Those are used in manufacturing a pharmaceutical composition.