7 results about "Vortioxetine Hydrobromide" patented technology

This application discloses coated granules, solid dispersions, combinations and formulations for oral taste masking, which have been shown to improve the taste masking effect of vortioxetine hydrobromide and increase patient compliance and tolerability.

This application discloses an analytical method for N-nitrosamine vortioxetine in vortioxetine hydrobromide tablets, belonging to the field of pharmaceutical impurity analysis. The method employs high-performance liquid chromatography (HPLC), with the following chromatographic conditions: a 4.6 mm × 250 mm column packed with octadecylsilane-bonded silica gel, with a particle size of 5 μm; mobile phase A is a 90:10 water-acetonitrile mixture containing 0.025%–0.035% trifluoroacetic acid (v / v); mobile phase B is acetonitrile; gradient elution; column temperature 38–42 °C; flow rate 0.9–1.1 ml / min; injection volume 50 μl; and detection wavelength 226 nm. This analytical method effectively eliminates excipient interference and exhibits excellent detection performance (specificity, sensitivity, linearity, precision, accuracy, and robustness), accurately detecting the content of N-nitrosamine vortioxetine in vortioxetine hydrobromide tablets, meeting quality control requirements.

The invention discloses a preparation method of hydrobromic acid vortioxetine, and belongs to the technical field of organic synthesis. The method comprises the following steps: by taking o-aminothiophenol and Boc2O as initial raw materials, carrying out amino protection to obtain an intermediate 1; reacting the intermediate 1 with 2, 4-dimethyl bromobenzene under an alkaline condition to form a thioether bond, and acidifying to obtain an intermediate 2; carrying out high-temperature cyclization on the intermediate 2 and bis (2-bromoethyl) amine hydrobromide in mesitylene, so as to obtain a crude product of the hydrobromic acid vortioxetine; and recrystallizing the crude product with 95% ethanol to obtain a high-purity final product. The route is simple, only three-step reaction is needed, a noble metal catalyst is not needed in the whole process, and the problem of metal residues is fundamentally avoided; the selected raw materials are easy to obtain, the reaction condition is mild, the operation is simple and convenient, the process is stable, the total yield is good, the product purity is as high as 99.9%, and the method is suitable for large-scale production.

The application relates to a preparation method of a high-fluidity alpha crystal form of vortioxetine hydrobromide. The technical scheme of the application is that vortioxetine hydrobromide is dissolved in 5-10 times the volume of an organic solvent, and after the insoluble substances are filtered out, 1-2.5 times the mass of polyvinylpyrrolidone is added to the filtrate. The above solution is flowed into pre-cooled purified water containing crystal seeds to crystallize, is filtered, and is dried to constant weight to obtain vortioxetine hydrobromide. 2 The vortioxetine hydrobromide obtained by the method is in an alpha crystal form, is spherical in shape, has a particle size less than 15 mu m, a specific surface area higher than 1600 m 2 / g, a fast dissolution rate, good fluidity, high yield, and is easy to realize industrialization.

A coated granule, a solid dispersion, a composition, and a preparation for oral masking, which improve the taste masking effect of vortioxetine hydrobromide, and improve the patient adherence and compliance.

The invention discloses a lyotropic liquid crystal long-acting injection as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The preparation consists of a raw material medicine, a lipid material, an organic solvent and a release regulator, and hexagonal phase liquid crystal gel can be spontaneously formed after injection so as to realize long-acting slow release. The preparation can be prepared by stirring and mixing at room temperature, and has the advantage of simple and convenient preparation process. Experiments show that the effective blood concentration in the body can be maintained for more than 14 days after single hypodermic injection, the half-life period of the medicine is prolonged to 187 hours from about 66 hours of oral administration, and the burst release phenomenon is avoided. The invention effectively solves the clinical pain points of frequent administration, large blood concentration fluctuation, poor patient compliance and the like of the existing oral preparation of the hydrobromic acid vortioxetine.

The invention discloses a 3D printing technology-based vortioxetine hydrobromide implant as well as a preparation method and application thereof, and relates to the technical field of pharmaceutical preparations, a melt extrusion deposition printing technology is adopted, polylactic acid with excellent biocompatibility is taken as a drug carrier material, vortioxetine hydrobromide is taken as a model drug, and a customized three-dimensional model is constructed, so that the vortioxetine hydrobromide implant is prepared. And the auxiliary material system and the drug loading capacity are subjected to adaptive screening, meanwhile, key 3D printing process parameters such as the filling distance, the layer thickness, the printing needle diameter and the printing path are optimized, and accurate forming of the implant is achieved. The preparation method has the advantages of simplicity and convenience in operation, low energy consumption, short production cycle, controllable process and the like, and the prepared implant has good biocompatibility, can realize long-term (40-80 days) stable release of drugs, and improves the medication compliance of patients.