21 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.

The present invention belongs to the field of biomedicine and specifically relates to the use of rupatadine fumarate in the preparation of a drug for inhibiting mycobacteria. The present invention is the first to discover that the commercial second-generation H1-antihistamine rupatadine fumarate exhibits excellent inhibitory effects on both Mycobacterium tuberculosis and non-tuberculosis mycobacteria, with a minimum inhibitory concentration of 4 μg / mL. It also has a synergistic effect in inhibiting mycobacterial activity with existing antibiotics such as pratomanid (PA824), clofazimine, and TB47.

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 present invention provides ruptifene fumarate crystalline form C, and its preparation method and use. The characteristic peaks of the powder X-ray diffraction pattern of crystalline form C of the present invention represented by 2θ (±0.2°) by using Cu-Kα rays are located at 12.3° ± 0.2°, 14.4° ± 0.2°, 17.6° ± 0.2°, and 22.4° ± 0.2°. Crystalline form C has characteristics such as a high melting point, a low residual moisture content, a low residual ethanol content, a stable crystal form, a small number of types of residual solvents and high safety, using a single solvent, a small amount of solvent, being able to effectively save material costs, having less environmental pollution, a high yield, mild conditions, simple operation, and being advantageous for subsequent commercial production.

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 invention provides a method for detecting related substances of rupatadine fumarate, which is suitable for the technical field of detection of impurity control of organic chemical synthesis raw material medicines, in particular to a liquid chromatography detection method for monitoring more than ten oxide impurities and byproducts in the organic synthesis process of the raw material medicines. According to the analysis method, limitation of an existing method is overcome, analysis time is shortened, mobile phase components are simplified, sensitivity and accuracy are improved, high performance liquid chromatography is adopted, chromatographic columns are silica gel bonded octadecylsilane columns and an ultraviolet detector, mobile phases comprise a triethylamine-containing phosphate buffer salt solution and an organic solvent, the mobile phases are simple in composition, and the method is suitable for large-scale industrial production. A conventional chromatographic column is used, the cost is reduced, and a gradient elution mode is adopted for separation and detection. The method for detecting the rupatadine fumarate related substances is good in separation degree, high in specificity, high in precision and good in repeatability, and meets methodological research on determination of the rupatadine fumarate related substances.

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.

The invention belongs to the technical field of pharmaceutical analysis, and particularly relates to a separation, qualitative and quantitative detection method for related substances in rupatadine fumarate. According to the method, main components and related impurities in rupatadine fumarate are separated by adopting a high performance liquid chromatography, and the method comprises the following steps: carrying out gradient elution by taking octadecylsilane chemically bonded silica as a chromatographic column filler, taking a phosphate solution as a mobile phase A and taking acetonitrile as a mobile phase B, and carrying out detection by adopting a detection wavelength of 210 nm and / or 250 nm; and finally, according to the measured chromatogram, calculating the content of each impurity by adopting a correction factor-added principal component self-contrast method. The method solves the problem of separation and determination of main components in rupatadine fumarate and a plurality of impurities such as an impurity G, an impurity D, an impurity E and an impurity F which cannot be solved in the prior art, and has the characteristics of short analysis time, low detection limit, good durability, good reproducibility and the like.

The present invention relates to a composition containing montelukast and rupatadine, having improved stability, and, more specifically, to: a composition containing montelukast or a pharmaceutically acceptable salt, and rupatadine or a pharmaceutically acceptable salt thereof, the composition having a pH of 4 to 5.5 by an added pH regulator; and a preparation method therefor. The composition according to the present invention has a pH of 4 to 5.5 due to a pH regulator, thereby having reduced generation of related substances and having excellent stability.

The present invention provides a semi-solid composition comprising a gel component in an amount sufficient to provide a gel product with binding force, an antihistamine composition comprising an antihistamine agent, and a complexing agent wherein the complexing agent is capable of interacting with the antihistamine agent and forming an antihistamine complex. In one embodiment, the antihistamine agent includes diphenhydramine, cetirizine, levocetirizine, loratadine, desloratadine, fexofenadine, azelastine, bilastine, rupatadine, or a derivative, a salt, or a combination thereof.

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.

The present invention relates to a novel pharmaceutical composition comprising rupatadine or a pharmaceutically acceptable salt thereof and montelukast or a pharmaceutically acceptable salt thereof. The novel pharmaceutical composition can be manufactured by a simple method and exhibits excellent compatibility of the two APIs while allowing the two APIs to have excellent bioavailability.