38 results about "Escitalopram Oxalate" patented technology

The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

The invention discloses a tablet containing escitalopram oxalate and a preparation method thereof. According to the invention, the tablet containing escitalopram oxalate uses hydroxy propyl cellulose as an adhesive and uses escitalopram oxalate with median particle size less than or equal to 20mum, and the prepared tablet containing escitalopram oxalate has the advantages of beautiful appearance and stable quality. The invention also provides the preparation method of oral tablet, and has the advantages of simple process and adaptability of commercialized production.

The invention belongs to the field of pharmaceutical analysis and particularly relates to a HPLC (high-performance liquid chromatography) detection method for escitalopram oxalate related substances. The escitalopram oxalate related substances are determined with HPLC, a C18 column is taken as a chromatographic column, a phosphate buffer solution is taken as a mobile phase A, the mobile phase A and an acetonitrile solution are mixed in a certain ratio to form a mobile phase B, the mobile phase A and the acetonitrile solution are mixed in a certain ratio to form a mobile phase C, and the escitalopram oxalate related substances are detected with a gradient elution method. The method can separate impurities, is high in specificity and sensitivity and good in repeatability and durability, can well control known impurities and unknown impurities of escitalopram oxalate and guarantees safety of escitalopram oxalate.

The invention relates to novel synthetic methods for three impurities of escitalopram oxalate. The methods have great significance for synthesis of the escitalopram oxalate with high purity. The invention mainly study syntheses of a citalopram amide impurity 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-isobenzofuran-5-formamide (II), a citalopram lactone impurity 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3-oxo-1,3-dihydro-isobenzofuran-5-carbonitrile (III) and a citalopram-N-oxide impurity 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-isobenzofuran-5-cyano-N-oxide (IV). Specific synthetic routes of the impurities are showed as follows.

The invention relates to an escitalopram oxalate related substance and a preparation method thereof, and particularly, relates to the related substance of an antidepressant drug, the escitalopram oxalate (namely, (S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-formonitrile oxalate), represented as the formula (I) and a preparation method thereof. The escitalopram oxalate, as the target compound, is synthesized through reactions comprising hydrolysis, acylation, condensation, reduction, addition and oxidization to the compound (II) (namely, (S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-formonitrile). According to the method, the compound (I) is chemically synthesized for the first time. By means of the method, the target compound can be obtained through high-efficient and quick separation.

The invention belongs to the field of medicine, and particularly relates to a pharmaceutical composition for treating depression and a preparation method thereof. The preparation is an oral solid preparation and contains an active component with general formula of (S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile oxalate (Escitalopram oxalate), microcrystalline cellulose and a compressible excipient; and the preparation has the characteristic of quick dissolution and is of great significance to the treatment of depression.

Crystalline particles of escitalopram oxalate with a particle size of at least 40 mum is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.

The invention belongs to the technical field of a medicinal preparation. Escitalopram oxalate, as a main drug, is suitable for treating depression and for treating panic disorder accompanies with or not accompanied with agoraphobe. An escitalopram oxalate effervescent tablet adopts a formula which consists of the main drug, a disintegrant, an aromatic and the like, and is subject to a tabletting process that an acid disintegrant and an alkaline disintegrant are respectively granulated. The escitalopram oxalate effervescent tablet, through the formula and the process, is easy to operate, controllable in product quality, good in taste of taking and low in cost.

The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01 % (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate. Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

The invention relates to an escitalopram oxalate tablet composition and a quality control method and in particular relates to a method for controlling quality of an escitalopram oxalate tablet composition. The method comprises the following steps: carrying out limitation test on escitalopram R-enantiomeric impurities in the composition, measuring the content of the escitalopram R-enantiomeric impurities in the composition and testing related substances in the composition. Furthermore, the invention also relates to an escitalopram oxalate tablet composition. The escitalopram oxalate tablet composition comprises an effective dose of escitalopram oxalate, magnesium stearate and optional pharmaceutically acceptable carriers. The method can implement the excellent technical effect as described in the description.

The invention belongs to the technical field of medicine and in particular relates to a synthetic method of a 1-(3-(dimethylamino)propyl)-1-(4'-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran nitrile compound.

The invention discloses a preparation method of an escitalopram oxalate intermediate S-configuration diol. The preparation method comprises the following steps: (1) carrying out hydrobromic acid salinization on racemic diol (4-(4-dimethylamino-1-p-fluorophenyl-1-hydroxybutyl)-3-(hydroxymethyl)benzonitrile) to obtain free racemic diol; and (2) carrying out chiral resolution on the free racemic diolby using (+)-di-p-toluoyl-D-tartaric acid in isopropanol by adopting a standing resolution mode, and conducting crystallization to obtain an escitalopram oxalate intermediate S-configuration diol crude product, and carrying out recrystallization refining on the crude product in an organic solvent to obtain the escitalopram oxalate intermediate with high optical purity. The method disclosed by theinvention is high in resolution efficiency and high in product yield, and the prepared diol intermediate is high in optical purity and can meet the requirements of industrial production.

The invention discloses an oral disintegrating tablet containing escitalopram oxalate. The preparation is composed of a filling agent, especially referring to mannitol with good taste, microcrystalline cellulose having a certain disintegration function, an adhesive, a disintegrating agent, a flavoring agent and a lubricating agent. Silicon dioxide is added, so that the taste is effectively improved. When a patient takes the escitalopram oxalate oral disintegrating tablet disclosed by the invention, no water or less water is required and no chewing is required; when the drug is placed into the oral cavity, the drug is quickly dissolved or disintegrated after meeting saliva, and then the drug enters the digestive system following the autonomous or heteronomous swallowing action of the patient and then is absorbed and becomes effective. The oral disintegrating tablet is suitable for the acute and maintenance treatment for major depressive disorder of an adult and the acute treatment for generalized anxiety disorder of the adult. The invention also provides a preparation method which is simple in technique, is low in cost and belongs to the field of pharmaceutical technology.

The invention discloses pharmaceutical composition containing escitalopram oxalate and a preparation method of the pharmaceutical composition. The pharmaceutical composition is tablets prepared from polyethylene glycol 6000 as a lubricant through fluidized bed granulation. The method well solves the problems of poor material flowability and non-uniform tablet content.

The invention discloses escitalopram oxalate inclusion compound oral liquid and a preparation method of the escitalopram oxalate inclusion compound oral liquid. In order to overcome the defect of a conventional flavor correction process of escitalopram oxalate, the preparation method disclosed by the invention has the advantages that the flavor is corrected commonly by adopting an inclusion technology and a flavor correction agent, so that a bitter taste of the escitalopram oxalate is covered, and an oral liquid preparation having an appropriate mouth feel is developed, and thus, the medicineapplication compliance of patients is improved.

The invention relates to the technical field of medicine, in particular to a preparation method of an escitalopram oxalate drop. The escitalopram oxalate drop is composed of escitalopram oxalate, a pH buffer agent, a flavoring agent, a solvent and a preservative. The escitalopram oxalate contained in the drop prepared by the invention is racemic citalopram-S-enantiomer, and the action mechanism of the escitalopram oxalate may be related to the behavior of enhancing serotonin activation by inhibiting the 5-hydroxytryptamine reabsorption of neurons of a central nervous system. The escitalopram oxalate drop is clinically used for treating severe depression and general anxiety; compared with other dosage forms, the escitalopram oxalate drop has the advantages of being convenient to take, accurate in dosage, convenient to carry and transport and the like; and when the escitalopram oxalate drop is taken, a matched dropper is used for sucking liquid to a specified scale line, and the escitalopram oxalate drop is directly dropped into a mouth or added into other food to be taken.

The invention discloses a synthetic method of an escitalopram impurity J, belonging to the technical field of medicaments. The synthetic route comprises the steps of using escitalopram oxalate as a raw material, adding an acid-binding agent into a solvent in the presence of hydrogen peroxide, and performing hydrolysis reaction to generate the escitalopram impurity J. The method disclosed by the invention uses escitalopram oxalate as a starting material; compared with a raw material required by a conventional method, escitalopram oxalate has the advantages of low cost and easy purchase; the synthetic route is simple, only needs a one-step reaction, is mild in reaction conditions and small in pollution caused by a reagent and the solvent adopted in the reaction, and has the characteristic of environmental friendliness; the escitalopram impurity J synthesized by the synthetic method is high in purity and yield.