9 results about "Vilazodone" patented technology

Provided are pharmaceutical compositions which include an amorphous solid dispersion comprising i) a lipophilic active pharmaceutical ingredient such as abiraterone, alectinib, pazopanib, cabozantinib, venetoclax, lurasidone, or vilazodone or a salt thereof, ii) a hydrophilic polymer, iii) optionally a surfactant, iv) optionally an adsorbent, and v) optionally an acid. Also described are methods for preparing such pharmaceutical compositions and treating a subject in need thereof. In one aspect, disclosed herein is an amorphous solid dispersion comprising an active pharmaceutical ingredient.

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.

The invention provides a novel crystal form of votioxetine pamoate, and in addition, the invention also relates to application of the crystal form of votioxetine pamoate in treatment and / or prevention of nervous system diseases. According to the crystal form of the vosulfur oxetine pamoate, the action time of vosulfur oxetine in vivo is greatly prolonged, the release rate of vosulfur oxetine is delayed, and the vosulfur oxetine pamoate is more stable in release and better in safety.

The present invention relates to a new vilazodone derivative (3-(4-(4-(2-chloro-6-methoxyphenyl)piperazine-1-yl)butyl)-cyano-indole) and a synthesis method and application thereof. The vilazodone derivative is 3-(4-(4-(2-chloro-6-methoxyphenyl)piperazine-1-yl)butyl)-cyano-indole, and its chemical structure is as follows: The compound has a significant growth inhibitory effect on a variety of human tumor cells and has excellent inhibitory activity on tumors such as leukemia, lymphoma, breast cancer, melanoma, ovarian cancer, colorectal cancer, cervical cancer, lung cancer, prostate cancer, esophageal cancer, glioma, kidney cancer, pancreatic cancer, nasopharyngeal cancer, liver cancer, and gastric cancer. The IC50 effective concentration of the compound on tumor cells such as breast cancer, colorectal cancer, lung cancer, glioma, pancreatic cancer, and nasopharyngeal cancer is lower than that of cisplatin. Experiments show that the vilazodone derivative has a broad-spectrum anti-tumor activity and is expected to become a new anti-tumor drug.

The invention belongs to the technical field of biological medicine, and particularly relates to a hydrobromic acid potioxetine sustained-release microsphere, a preparation thereof, a preparation method and application thereof. Compared with the prior art, the preparation method provided by the invention has the advantages that the drug loading capacity can be improved, the drug encapsulation efficiency can be improved, and the dosage of auxiliary materials is obviously reduced.

The invention relates to the technical field of medicines, in particular to a vothioxetine ester pharmaceutical composition as well as a preparation method and application thereof. The pharmaceutical composition disclosed by the invention has the characteristic of high drug loading capacity, and the drug loading capacity is as high as 100 mg / mL to 400 mg / mL. The pharmaceutical composition disclosed by the invention has the characteristic of high stability, can be prepared by various methods, and is easy to realize industrial production. After intramuscular injection, about 50-1300mg of a drug reservoir can be formed at an injection site, slow and continuous release can be realized in the drug reservoir, the fluctuation of blood concentration is small, continuous and effective drug release as long as 2-24 weeks can be realized, frequent administration is reduced, and the pharmaceutical composition is used for treating adult depression and increasing the compliance of drug use.

The present invention belongs to the field of pharmaceutical technology, and particularly relates to a long-acting prodrug derivative of vilazodone, its pharmaceutical composition and uses. The long-acting prodrug derivative of vilazodone includes a compound having the structure shown in formula (I). The long-acting prodrug derivative of vilazodone of the present invention is metabolized by enzymes in vivo to produce vilazodone, so that the fluctuation of the blood drug concentration of vilazodone is small, the effective blood drug concentration is maintained for a long time, the administration frequency can be reduced, and the compliance of patients and the therapeutic effect of diseases can be improved.

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.