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Vilazodone hydrochloride and composition thereof

A technology of vilazodone and a composition, applied in the application field of medicine, can solve the problems of adverse reactions, insufficient curative effect and the like

Active Publication Date: 2011-10-19
天津汉一医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, SSRIs are less effective than TCAs in the treatment of major depressive disorder and, because they nonselectively stimulate various subtypes of 5-HT receptors, have some associated adverse effects

Method used

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  • Vilazodone hydrochloride and composition thereof
  • Vilazodone hydrochloride and composition thereof
  • Vilazodone hydrochloride and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] In a 1000ml reaction bottle equipped with stirring, thermometer and condenser, add 30g of vilazodone and 180ml of dimethylformamide, start stirring, heat up to 48°C-50°C, filter, and cool the filtrate to 10°C- 12°C, add ether hydrochloride to pH 2-3, then cool to 0°C-4°C, keep stirring for 11 hours. The precipitated crystals were filtered, washed with 30ml of anhydrous ether in three equal parts, placed indoors for 1 hour, then moved to a vacuum drying oven, and dried in vacuum at room temperature for 3 hours to obtain 26.1 grams of vilazodone dihydrochloride in white crystalline form. The powder has a melting point of 286-288°C and a purity of 99.84% (HPLC normalization method).

[0044] Elemental Analysis Results:

[0045] Measured value (calculated value), C:60.63(60.70),H:5.62(5.68),N:13.68(13.61),

[0046] Cl: 13.75 (13.78);

[0047] The X-ray diffraction pattern of this crystalline powder is shown in figure 1 . Instrument model and measurement conditions: Rig...

Embodiment 2

[0049] Granules containing a new crystal form of vilazodone dihydrochloride

[0050] Prescription: 10 grams of new crystal form vilazodone dihydrochloride, 650 grams of lactose, 30 grams of microcrystalline cellulose, 68 grams of crospovidone, 80 grams of PEG-4000, 110 grams of hydroxypropyl methylcellulose grams, appropriate amount of distilled water, made into 1000 bags.

[0051] Process: PEG-4000 and the new crystal form of vilazodone dihydrochloride are crushed together, passed through an 80-mesh sieve, mixed with other materials, made into soft materials with distilled water, granulated, dried at low temperature, and then packed into granules.

Embodiment 3

[0053] Capsules containing a new crystalline form of vilazodone dihydrochloride

[0054] Prescription: 40 grams of vilazodone dihydrochloride in new crystal form, 16 ml of propylene glycol, 120 grams of starch, 26 grams of magnesium stearate, 35 grams of colloidal silicon dioxide, made into 1000 capsules.

[0055] Process: Wet the new crystal form of vilazodone dihydrochloride, starch, magnesium stearate, and colloidal silicon dioxide with 15% propylene glycol aqueous solution, mix well, sieve and granulate, dry at 60°C, and prepare Capsules, filled capsules.

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PUM

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Abstract

The invention relates to a crystal form of vilazodone dihydrochloride and a preparation method thereof, and also relates a medicinal composition containing vilazodone in the crystal form and application of the crystal form to the preparation of medicaments for treating melancholia.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing vilazodone dihydrochloride crystal form, a preparation method and an application of the crystal form in the manufacture of medicine for treating depression. Background technique [0002] Depression is a disorder caused by biochemical changes in the brain whose signs and symptoms include: depressed mood, loss of interest in usual activities, significant changes in weight or appetite, insomnia or excessive sleepiness (hypersomnia), restlessness / pacing (psychomotor Agitation), increased fatigue, feelings of guilt or inferiority, slow thinking or inattention, and in severe cases, self-harm and suicidal impulses. Seriously affects people's ability to work, sleep, study, eat and enjoy pleasurable activities. [0003] Low content of monoamine neurotransmitters such as central norepinephrine (NE), 5-hydroxytryptamine (5-HT), dopamine (DA) and low receptor function are considered to be the cause ...

Claims

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Application Information

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IPC IPC(8): C07D407/12A61K31/496A61P25/24
Inventor 严洁黄欣
Owner 天津汉一医药科技有限公司
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