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Melitracen hydrochloride crystal form A and preparation method thereof

A technology of melitracen hydrochloride and melitracen hydrochloride, applied in the field of medicinal chemistry, can solve problems affecting drug absorption and release, affecting drug efficacy and safety, melting point, solubility, stability, etc.

Pending Publication Date: 2022-02-18
NHWA PHARMA CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It is generally believed that polymorphic drugs, due to different crystal forms, may have different melting points, solubility, stability, etc., which will affect the absorption and release of drugs in the body, thereby affecting the efficacy and safety of drugs

Method used

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  • Melitracen hydrochloride crystal form A and preparation method thereof
  • Melitracen hydrochloride crystal form A and preparation method thereof
  • Melitracen hydrochloride crystal form A and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Weigh 1 g of melitracen hydrochloride sample, put it into an eggplant-shaped bottle, add 10 ml of 95% ethanol, and remove the solvent by rotary evaporation under reduced pressure at a vacuum of 0.09 MPa and 45°C, collect the solid, and dry it overnight at 60°C to obtain melitracen hydrochloride Trisine crystal form A. The purity is 99.8%, X-ray powder diffraction as figure 1 shown.

Embodiment 2

[0053] Weigh 1 g of melitracen hydrochloride sample, put it into an eggplant-shaped bottle, add 10 ml of 90% ethanol, and remove the solvent by rotary evaporation at a vacuum of 0.09 MPa and 60°C, collect the solid, and dry it overnight at 50°C to obtain melitracen hydrochloride. Trisine crystal form A.

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Abstract

The invention provides a novel crystal form A of melitracen hydrochloride. The crystal form A shows characteristic peaks at the positions of 10.467, 11.361, 11.812, 13.895, 15.785, 16.602, 17.419, 18.696, 21.133, 21.691 and 24.370 in an X-ray powder diffraction pattern represented by a diffraction angle of 2 theta + / -0.2 degrees.

Description

Technical field: [0001] The invention relates to the field of medicinal chemistry, in particular to a crystal form A of melitracen hydrochloride and a preparation method thereof. Background technique: [0002] Melitracen hydrochloride (Melitracen hydrochloride) has a chemical name of 3-[10,10-dimethyl-9(10H)-anthracene]-N,N-dimethylpropylamine hydrochloride; 3-[10 ,10-Dimethyl-9(10H)-anthrylene]-N,N-dimethylpropylamine hydrochloride, CAS No.: 10563-70-9. Melitracen hydrochloride can inhibit the reuptake of norepinephrine in the presynaptic membrane and increase the content of synaptic monoamine transmitters. This product was launched in the market in 1968. It is used in combination with flupenthixol. It 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 and depression. [0003] The structural formula is as follows: [0004] [0005]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/31C07C209/84
CPCC07C209/84C07B2200/13C07C211/31C07C2603/24
Inventor 郝超王国海陈亮张桂森
Owner NHWA PHARMA CORPORATION