3 results about "Vilazodone" patented technology

The invention discloses a method for continuously synthesizing 2-(4-cyanophenyl)-N-Boc-ethylamine by virtue of photocatalysis. The preparation method comprises the following steps: in the presence of a photocatalyst, enabling 4-chlorobenzonitrile, tert-butyl vinyl carbamate and (tri (trimethylsilyl) silane to react in a solvent through a photoreactor; and after the reaction is finished, extracting, drying and purifying by silica gel column chromatography to obtain a target product. By using the micro-channel photoreactor, efficient mixing, mass transfer enhancement, reaction time shortening and yield and purity improvement can be realized. The whole reaction process is continuous and closed, the liquid holdup is small, and the exposure risk of toxic chemicals is remarkably reduced. The solvent can be recycled, and the COD of the waste liquid is reduced by 70% or above. Equipment is easy to amplify, small in occupied area, energy-saving and economical, the obtained product meets the quality standard of GMP bulk drug intermediates, and the method is suitable for industrial production of vilazodone and other drugs.

A kind of pellet, the pellet includes blank core and drug layer, the drug layer is wrapped in the outer layer of blank core;Wherein, the drug layer includes: vilazodone or its pharmaceutically acceptable salt or ester, and carrier;The carrier includes at least one selected from povidone, copovidone, hypromellose, sucrose and mannitol.The pellet, whether in the environment of pH 6.8 medium, or in the environment of pH 6.8 medium after 0.1M HCl first, has higher solubility, especially can maintain the supersaturated state in the environment of pH 6.8 medium after 0.1M HCl first, therefore, whether with food, or fasting, has higher bioavailability.

A vilazodone pharmaceutical composition, a preparation method therefor and use thereof are provided. The vilazodone pharmaceutical composition are in vilazodone solid particles. The vilazodone solid particles have a Dv(10) particle size not greater than 20 microns, a Dv(50) particle size not greater than 50 microns and a Dv(90) particle size not greater than 100 microns. The vilazodone pharmaceutical composition has significant advantages such as long-acting sustained release, reducing the frequency of administration, and improving patient compliance.