Melitracen hydrochloride compound

A melitracen hydrochloride compound technology, applied in the field of pharmaceuticals, can solve problems such as risks, large benefits, and few adverse reactions

Active Publication Date: 2016-01-06
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its preparations have few and mild clinical adverse reactions, and the benefits in clinical application outweigh the risks

Method used

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  • Melitracen hydrochloride compound
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  • Melitracen hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1-compound preparation of the present invention

[0017] Melitracen hydrochloride crude product (comparative example 1) 25g, after adding 150ml of acetone, gradually add dropwise 75ml of n-hexane and cyclohexane mixed solvent (the volume ratio of the two is 1:1), fully stir, and precipitate with n-butyl After washing with alcohol for 3 times, the finished melitracen compound was obtained with a yield of 91.7%. Powder X-ray Diffraction: Using Cu-K radiation, the X-ray powder diffraction pattern of this compound is shown in the attached figure 1 . Differential scanning calorimetry analysis: The differential thermal analysis spectrum of this compound is shown in the attached figure 2 .

Embodiment 2

[0018] The formulation of embodiment 2-quality research and quality standard of compound of the present invention

[0019] According to the synthesis process and product characteristics of this product, we have conducted a comprehensive study on the properties, identification, inspection, and content determination of this product with reference to the quality standards for clinical research of this product.

[0020] Properties We have studied the appearance, hygroscopicity and solubility of this product. As a result, the three batches of pilot test samples are white crystalline powder, and this product has no hygroscopicity; according to the results of the solubility investigation of this product, this product is easily Soluble, soluble in methanol or ethanol, slightly soluble in water.

[0021] Inspection In the inspection items, we inspected its acidity, loss on drying, residue on ignition, heavy metals, and the results all met the requirements. According to the synthesis p...

Embodiment 3

[0025] Experimental data of embodiment 3-stability study

[0026] .1. Sample source:

[0027] Influencing factor test sample: batch number: 10021101; batch size: 58g; prepared by Sichuan Haisco Pharmaceutical Co., Ltd.; test time: February 2010. Samples for stability testing: batch numbers: 10022701, 10022702, 10022703. The batches are 99.3g / batch, 99.8g / batch, 103.1g / batch; prepared by Sichuan Haisco Pharmaceutical Co., Ltd.; test time: February 2010.

[0028] .2 Inspection items

[0029] According to the second appendix "Guiding Principles of Drug Stability Test" of the 2010 edition of "Chinese Pharmacopoeia", according to the inspection method stipulated in the quality standard (draft) of this product, the appearance, acidity, loss on drying, related substances, content, etc. of this product were mainly investigated. The project is inspected.

[0030] 3. Illumination test

[0031] Take an appropriate amount of this product (10021101), place it under the condition of 45...

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PUM

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Abstract

The invention provides a melitracen hydrochloride compound. Melitracen hydrochloride can inhibit reuptake of a presynaptic membrane on noradrenaline, so that the content of monoamine neurotransmitters of cynapse is improved. The product is researched by Denmark Lundbeck pharmaceuticals company and is listed in 1968. Melitracen and flupentixol are combined in use to have the function of coordinately adjusting the central nervous system and exert anti-depression, anti-anxiety and anti-excitation characteristics, so that the compound is suitable for acute and chronic schizophrenia, melancholia and depressive psychoneurosis.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a melitracen hydrochloride compound. Background technique [0002] The chemical name of melitracen hydrochloride is: 3-[10,10-dimethyl-9(10H)-anthracene]-N,N-dimethyl-1-propanamine hydrochloride, the English name is MelitracenHydrochloride , the molecular formula is C 21 h 25 N·HCl, molecular weight 327.90. Melitracen hydrochloride can inhibit the reuptake of norepinephrine in the presynaptic membrane and increase the content of synaptic monoamine transmitters. This product was developed by the Danish Lundbeck Pharmaceutical Company and was launched in 1968. The combination of melitracen and flupenthixol has the function of synergistically regulating the central nervous system, exerts antidepressant, anti-anxiety and excitatory properties, and is suitable for acute and chronic schizophrenia, depression and depressive neurosis. [0003] Melitracen hydrochloride b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/31A61K31/135A61P25/24
Inventor 万华冯卫戴志东
Owner SICHUAN HAISCO PHARMA CO LTD
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