14 results about "Rupatadine" patented technology

The invention relates to a method for detecting genotoxic impurities of rupatadine fumarate, which is characterized in that a phosphate buffer solution is matched with acetonitrile, a high performance liquid chromatography method is adopted, a chromatographic column is a silica gel bonded octadecylsilane column, a gradient program is adopted for elution, and the content of the rupatadine fumarate genotoxic impurities in the rupatadine fumarate genotoxic impurities in the rupatadine fumarate genotoxic impurities is detected. Effective separation between rupatadine fumarate and genotoxic impurities and between genotoxic impurities can be achieved, accurate quantitative analysis can be achieved, and the quality of drugs can be effectively controlled.

The invention discloses a liquid chromatography method for separating rupatadine fumarate and a positional isomer of rupatadine fumarate. According to the method, the rupatadine fumarate and the positional isomer are effectively separated by adopting reversed-phase liquid chromatography, and compared with normal-phase liquid chromatography generally adopted by isomers, the method provided by the invention is quicker, simpler and more convenient, can effectively separate isomer impurities and accurately quantify the content of the isomer impurities, and has the advantages of high accuracy and high efficiency. And the quality of the product is effectively controlled.

The present application relates to a kind of HPLC-MS / MS detection method of detecting in human plasma, desloratadine and 3-hydroxydesloratadine in human plasma, it includes the following steps: (1) human plasma sample pretreatment;(2) liquid chromatography-mass spectrometry detection, using mobile phase A and mobile phase B as mixed mobile phase is carried out gradient elution, wherein: mobile phase A is methanol-acetonitrile mixed solution, in mixed solution methanol and acetonitrile volume ratio is 4-6:6-4;Mobile phase B is 2-20mM ammonium formate aqueous solution;(3) the determination of the concentration of human plasma in lopatadine, desloratadine and 3-hydroxydesloratadine.The present application uses lopatadine-d4, desloratadine-d5, 3-hydroxydesloratadine-d4 as deuterium internal standard, using Agilent, ZORBAX Eclipse XDB-Phenyl is carried out gradient elution, deuterium internal standard and the measured substance has the same retention time, chemical property and matrix effect, the reproducibility, accuracy of determining the concentration of lopatadine, desloratadine and 3-hydroxydesloratadine in plasma are good.The method of the present application can be used to evaluate the bioequivalence of lopatadine.

The application provides fumarate lopanfene hemihydrate and a preparation method thereof, and relates to the technical field of drug synthesis. The fumarate lopanfene hemihydrate is a crystalline compound in orthorhombic system, has high purity, low moisture content, low content of related substances, good fluidity and high stability, and the fumarate lopanfene hemihydrate can be obtained by controlling the water activity of an alcohol solvent during recrystallization, and the preparation method is simple.

The application provides a lurasidone orally disintegrating film composition, a preparation method and application thereof. The lurasidone orally disintegrating film composition comprises an active drug, a film-forming material, a plasticizer, an absorption promoter and a sweetening agent, and the active drug is 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine as shown in formula I and / or a pharmaceutically acceptable salt thereof. The lurasidone orally disintegrating film composition has the advantages of good film-forming property, smooth surface, uniform color, no sand particle feeling, thin thickness, good taste, excellent mechanical property, stable property, no need of drinking water for instant dissolving in the oral cavity, fast oral absorption speed, simple process, high drug loading, good drug content uniformity and good market prospect.

To provide an orally disintegrating tablet that exhibits good dissolution behavior even when a coating layer is applied to mask the bitter taste, and is of a size that is easy to pick up with your fingers. [Solution] The problem is solved by an orally disintegrating tablet containing granules in which a coating layer is provided on a core particle comprising rupatadine or a salt thereof and at least one additive selected from the group consisting of excipients, disintegrants, and binders, characterized in that the mass is 180 to 300 mg.

The invention belongs to the technical field of chemical analysis, and particularly relates to a method for separating and determining related substances in a rupatadine fumarate intermediate Z2. The related substances comprise any one or more of an impurity SM1, an impurity Z1, an impurity Z2a and an enantiomer thereof, an impurity Z2b and an enantiomer thereof, and an impurity Z2e and an enantiomer thereof. According to the self-built high performance liquid chromatography, octadecyl silane bonded silica gel is adopted as a chromatographic column filler, a phosphate solution is adopted as a mobile phase A, acetonitrile is adopted as a mobile phase B, and related substances in the rupatadine fumarate intermediate Z2 are separated through linear gradient elution; then detecting in a detector to obtain a chromatogram; and calculating the content of each impurity by adopting a correction factor-added principal component self-contrast method. The analysis method has the characteristics of short separation time, high sensitivity, strong specificity, good reproducibility, strong durability and simplicity and feasibility in operation.

The application provides a hydrated compound and a preparation method thereof, and relates to the technical field of compound preparation. The hydrated compound is fumaric acid rupatadine monohydrate, which has a crystal structure. The preparation method of the hydrated compound is as follows: fumaric acid rupatadine is added into a reaction solvent containing at least a first organic solvent, heated, stirred and refluxed until the fumaric acid rupatadine is completely dissolved, the concentration of the fumaric acid rupatadine in the reaction system is not less than 70% of the saturated solution concentration of the fumaric acid rupatadine in the reaction system, the refluxing is continued for 1 min to 24 h, the temperature is lowered to not more than 8 DEG C and crystallization is performed, the crystals are collected, washed and dried, and the hydrated compound is obtained.

To provide a lupatadine solid preparation having favorable dissolution characteristics even when provided with a coating layer.SOLUTION: The foregoing problem is solved by a lupatadine solid preparation comprising granules in which core particles containing lupatadine or a salt thereof are provided with a coating layer containing an aminoalkyl methacrylate copolymer and methylcellulose. It is preferable that, within the coating layer, the mass ratio of methylcellulose to the aminoalkyl methacrylate copolymer [methylcellulose / aminoalkyl methacrylate copolymer] is from 0.1 to 2.SELECTED DRAWING: None

The present invention relates to the technical field of drug synthesis, and in particular to a method for preparing rupatadine fumarate. The method for preparing rupatadine fumarate of the present invention comprises the following steps: S1, reacting nitrogenmethylloratadine, phenyl chloroformate, and an organic amine in an organic solvent to obtain compound I; the structural formula of compound I being: #imgabs0#; S2, reacting compound I with a base in an organic solvent to obtain desloratadine; S3, reacting desloratadine, 3-chloromethyl-5-methylpyridine hydrochloride, and an organic amine in an organic solvent to obtain rupatadine; and S4, reacting rupatadine with fumaric acid in a salt-forming solvent to obtain rupatadine fumarate. The method for preparing rupatadine fumarate of the present invention has mild reaction conditions, short reaction time, a short route, simple operation, high yield, high product purity, and is suitable for large-scale industrial production.

The invention relates to the field of compounds, in particular to application of a small molecule compound in preparation of a CXCR7 agonist. The invention provides an application of a small molecule compound or a pharmaceutically acceptable salt thereof in preparation of a CXCR7 agonist, and is characterized in that the small molecule compound comprises one or more of JMS-17-2, rupatadine, ibutamolam mesylate, asenapine, alverine and vilanterol. The small molecule compound can specifically activate an intracellular beta-arrest signal channel instead of being coupled with a G protein signal channel, so that the small molecule compound can be used as a novel CXCR7 agonist.

The invention belongs to the technical field of analytical chemistry, and particularly relates to an HPLC (High Performance Liquid Chromatography) method for separating and determining rupatadine fumarate SM2 and impurities thereof. The method comprises the following steps: by taking octadecylsilane chemically bonded silica as a chromatographic column filler, a phosphate solution as a mobile phase A and methanol as a mobile phase B, separating rupatadine fumarate SM2 and related impurities thereof through linear gradient elution, and detecting by adopting a detector to obtain a chromatogram; and each impurity is quantified according to a correction factor-added principal component self-contrast method and a limit method. The method realizes effective detection of 15 impurities, namely SM2f, SM2j, SM2k, SM2a, SM2b / SM2d, SM2c, SM2e, SM2g, SM2h, SM2i, SM2l, SM2m, SM2n and SM2o, in rupatadine fumarate SM2, and has the characteristics of short separation time, strong specificity, high sensitivity, good reproducibility and strong durability.

Provided is a technique for suppressing discoloration that occurs when at least one selected from the group consisting of rupatadine, a salt thereof and a solvate thereof is enclosed in an airtight package.SOLUTION: A pharmaceutical product comprising a pharmaceutical composition packaged in an airtight package, the pharmaceutical composition comprising the following components (A) and (B-2): (A) one or more selected from the group consisting of rupatadine, a salt thereof and a solvate thereof; and (B-2) one or more selected from glycyrrhetinic acids.SELECTED DRAWING: None

The invention discloses a method for detecting related substances of a rupatadine fumarate intermediate, which is characterized in that a high performance liquid chromatography method is adopted, a chromatographic column is a silica gel bonded octadecylsilane column, a chromatographic column is a silica gel bonded octadecylsilane column, a chromatographic column is a silica gel bonded octadecylsilane column, a chromatographic column is a silica gel bonded octadecylsilane column, a chromatographic column is a silica gel bonded octadecylsilane column, and a chromatographic column is a silica gel bonded octadecylsilane column. A certain proportion of inorganic salt buffer solution-organic phase is used as a mobile phase, and a gradient elution mode is adopted for separation and detection. According to the method for preparing the related substances of the rupatadine fumarate intermediate, the quality of a medicine can be effectively controlled, and the safety of the medicine is ensured.