38 results about "Escitalopram Oxalate" patented technology

Crystalline particles of escitalopram oxalate with a particle size of at least 40 μm 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 medicinal preparation and particularly relates to an escitalopram oxalate oral dissolution film agent and a preparation method thereof. The escitalopram oxalate oral dissolution film agent comprises an antioxygen, a high polymer film-forming material and the like. The film agent provided by the invention is novel in appearance and excellent in taste, can be dissolved in an oral cavity quickly, can be taken without water, and can be accepted and adopted by patients easily; in addition, compared with common drugs, the film agent provided by the invention is different in appearance and taste, not only can relieve mental stress of patients, but also can protect patients' privacy. The product adopts the process of low temperature drying, is used together with the antioxygen, and ensures excellent product stability. The preparation process is environmentally friendly, low in cost, and has excellent environmental benefits and economic benefits.

The invention discloses an oxalic acid esmolol citalopram oral solid preparation and a preparation method. The oral solid preparation comprises raw materials of: 2-40 parts by weight of oxalic acid esmolol citalopram, 5-60 parts by weight of starch, 5-200 parts by weight of microcrystalline cellulose, 5-60 parts by weight of lactose, 0.05-5 parts by weight of binding agent and 0.05-3 parts by weight of lubricant; the binding agent is one or a plurality of mixed aqueous solutions or alcoholic solutions from the group consisting of polyvinyl pyrrolidone, hydroxyethyl methylcellulose, methylcellulose, hydroxypropyl cellulose and ethyl cellulose, the concentration of the binding agent is 0.1-10.0%; and the lubricant is stearic acid, magnesium stearate, calcium stearate, talcum or superfine silica gel powder.

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

The invention discloses a preparation method for escitalopram oxalate, which is characterized in that D-toluoyl tartrate of S-diol is dissolved into water, and sodium hydroxide is used for neutralization to obtain free S-diol; then, the temperature is controlled to be 0 to 10 DEG C, paratoluensulfonyl chloride is added, then, inorganic alkaline solution is dripped, and the ring closure reaction is carried out after the reaction for 2 to 4 hours; after the reaction is completed, the pH value is regulated to 12 to 13, and then, the extraction, the water washing and the liquid separation are carried out; and after oxalic acid is added for salt forming, the temperature reduction, the filtering and the drying are carried out, and products are obtained. In the ring closure reaction, water is adopted as solvents, the condition is mild, the environment is friendly, byproducts of each step of reaction in the synthesis method are few, the yield is high, in addition, products in each step of reaction are easy to separate and purity, raw materials used in the synthesis method are easy to obtain, the operation is simple, and the industrial production is easy.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to escitalopram oxalate tablets and a preparation method thereof capable of ensuring stable quality. According to the preparation method, an escitalopram oxalate raw material with the median diameter of not less than 300 microns is used, and auxiliary materials include magnesium stearate and other components, wherein the weight percentage of magnesium stearate in the tablets is less than 0.1%. The preparation method effectively solves the problems of poor raw material fluidity, high sticking tendency and non-uniform mixing of materials, and also solves the problem that compatibility between magnesium stearate and active ingredients is poor, causing increase of related substances. The method has the advantages of easy operation and easy industrialization, and the obtained tablets are high in content uniformity and stable in quality within the valid period.

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 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 present invention relates to a pharmaceutical composition comprising a tablet core comprising a combination of actives selected from the group consisting of bupropion hydrochloride and escitalopram oxalate, bupropion hydrobromide and citalopram hydrochloride, bupropion hydrobromide and escitalopram oxalate, and bupropion hydrobromide and quetiapine fu-marate, and at least one pharmaceutically acceptable excipient, and a control-releasing coat surrounding the tablet core, wherein said composition surprisingly provides for a synchronous release of the combination of active agents in-vitro. The once-daily pharmaceutical composition surprisingly also provides for enhanced absorption of bupropion hydrobromide when administered to a subject in need of such administration.

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 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 discloses a preparation method of escitalopram oxalate intermediate S-configuration diol, comprising: (1) preparing racemic diol (4-(4-dimethylamino-1-p-fluorobenzene Base-1-hydroxybutyl)-3-(hydroxymethyl) benzyl cyanide) hydrobromide basification to obtain free racemic diol; (2) free racemic diol with D-(+)- Chiral resolution and crystallization of di-p-toluoyl tartaric acid in isopropanol by static resolution to obtain the crude product of the S-configuration diol of the escitalopram oxalate intermediate, and the crude product was carried out in an organic solvent The escitalopram oxalate intermediate with high optical purity was obtained through recrystallization and purification. The method of the invention has high resolution efficiency and high product yield, and the prepared diol intermediate has high optical purity and can meet the needs of industrial production.