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Novel niacin drug salt and preparation method thereof

A technology of niacin and drugs, applied in the field of niacin drug salts and its preparation, to achieve the effects of reduced production costs, high product purity, and mild reaction conditions

Active Publication Date: 2021-10-01
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug co-crystal, drug salt research and solid-state characterization are relatively mature and highly valued fields in the pharmaceutical industry in Europe and America, but it is still in its infancy in the domestic pharmaceutical industry

Method used

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  • Novel niacin drug salt and preparation method thereof
  • Novel niacin drug salt and preparation method thereof
  • Novel niacin drug salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] (1) Liquid auxiliary grinding method

[0052] 1. The preparation method is as follows:

[0053] 1) Take 0.0123 g of smoking acid 0.0123 g, 1,2-diphenyethylenediamine 0.0106 g, mix well;

[0054] 2) Add a mixture into a mortar, 25 μl of ethanol is added thereto, 5 min;

[0055] 3) The resulting solid was dried to give 0.0225 g of the white powder solid 0.025 g, and the yield was 98.2%, the melting point was: 162.2 ° C.

[0056] X-ray diffraction diagram of the product figure 1 As shown in, X-ray powder diffraction angles 2θ in 9.872,11.451,13.731,15.213,15.544,15.934,17.142,18.077,18.955,20.183,20.650,21.5273,22.0145,22.502,22.911,24.880,25.737,26.887,27.628,28.037, 28.739 has a characteristic peak.

[0057] 2, the preparation method is as follows:

[0058] 1) Take 0.0123 g of smoking acid 0.0123 g, 1,2-diphenyethylenediamine 0.0106 g, mix well;

[0059] 2) Add 25 μl of acetonitrile in the process of grinding the mixture, 25 μl of acetonitrile is added thereto.

[0060] The r...

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Abstract

The invention relates to a novel niacin drug salt and a preparation method thereof. The salt is made from niacin and 1,2‑diphenylethylenediamine in a 2:1 molar ratio. The present invention adopts a green synthesis method of micro-liquid assisted grinding and two methods of slow volatilization at room temperature to prepare niacin-1,2-diphenylethylenediamine drug salt with high purity. The solubility of the obtained nicotinic acid drug salt is increased by 3.8 times, 6.7 times and 3.9 times in the buffer solution of pH=1.2, 4.5 and 6.8 respectively, and the crystal form is stable and does not decompose under the condition of normal temperature. The method requires only a trace amount of catalytic amount of organic solvent, has little pollution, mild reaction conditions, simple operation and high product purity.

Description

Technical field [0001] The present invention belongs to the field of pharmaceutical chemistry, and in particular to a nicotinic acid salt and a preparation method thereof. Background technique [0002] Nika-niacin is also a vitamin that is the simplest structure and the stable structure of the structure. It is an indispensable nutrients of the human and animals. It participates in the oxidative process of the organization, which has a metabolic and expanded blood vessels. Function, can promote the growth and development of human and animals. Niacine is contained in the "China Pharmacopoeia" 201 version second, its molecular formula is C 6 Hide 5 NO 2 The chemical structure is: [0003] [0004] Crystal engineering uses the basic principles and methods of super molecules to the growth and design of the crystal, and the structurally controllable and has a new crystal having a specific physical chemical properties by the molecular self-assembly and identification. The route of eut...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/80C07D213/803
CPCC07B2200/13C07D213/80C07D213/803
Inventor 郭放付强
Owner LIAONING UNIVERSITY
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