Amantadine hydrochloride and resveratrol pharmaceutical co-crystal and preparation method thereof

A technology of amantadine hydrochloride and resveratrol, which is applied in the field of drug co-crystals, can solve the problems of toxic side effects and drug efficacy reduction, and achieve the effects of reducing toxic side effects, high yield, and mild reaction conditions

Inactive Publication Date: 2021-03-26
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problems in the prior art of amantadine hydrochloride caused by too high solubility of toxic side effects and reduced drug effic

Method used

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  • Amantadine hydrochloride and resveratrol pharmaceutical co-crystal and preparation method thereof
  • Amantadine hydrochloride and resveratrol pharmaceutical co-crystal and preparation method thereof
  • Amantadine hydrochloride and resveratrol pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0029]Example 1: Preparation method of diamine and resveratrol drug eutectic hydrochloride is implemented as follows:

[0030]The methane (56.31 mg) of hydrochloride and resveratrol (34.24 mg) were added to the mortar in the mortar, and 50 ml of isopropyl alcohol was added to dry, and the white powder was obtained after 1 h. The white powder was transferred to a round bottom flask, and 17 mL of acetonitrile was added to a mixed solvent of 1.7 mL of methanol (volume ratio of 10: 1), and then filtered after stirring 4 h, and the filtrate was allowed to wait for a colorless column crystal. Crystals.

[0031]In this example, the drug-modulus of the medicament of the hydrochloride compound prepared by solvent volatile method is a non-chromous crystal, and a single crystal sample selected from which a single crystal sample is selected for X-ray single crystal diffraction determination. The German Stoe's Stadivari diffractometer is used, and the Cu-Kα ray scanned Cu-Kα ray scanned by multilayer ...

Example Embodiment

[0035]Example 2: The preparation method of diamine hydrochloride and resveratrol drug eutectic is implemented as follows:

[0036]In the present embodiment, the difference ratio of the acetonitrile and methanol in the system is 7: 1, and the other steps and parameters are the same as those in the specific embodiment 1.

Example Embodiment

[0037]Example 3: The preparation method of the polycondrioamine hydrochloride and the resveratrol drug eutectic is implemented as follows:

[0038]In the present embodiment, in the first embodiment, the volume ratio of acetonitrile and methanol in the system is 13: 1, and the other steps and parameters are the same as those of the specific embodiment 1.

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Abstract

The invention discloses an amantadine hydrochloride and resveratrol pharmaceutical co-crystal and a preparation method thereof, and relates to the technical field of pharmaceutical co-crystals. The pharmaceutical co-crystal is characterized in that two amantadine hydrochloride molecules and a resveratrol molecule form a basic structural unit, the chemical formula of the pharmaceutical co-crystal is [2C10H18ClN.C14H12O3], the pharmaceutical co-crystal belongs to a monoclinic system, and the space group is P21/c. According to the pharmaceutical co-crystal prepared by adopting a solvent evaporation method and a cooling method, the dissolution rate of amantadine hydrochloride is properly reduced while the solubility of resveratrol is improved, so that the toxic and side effects caused by excessive dissolution of amantadine hydrochloride are favorably reduced; through bidirectional coupling optimization and advantage complementation of the two components in nature, the antiviral activity ofamantadine hydrochloride is significantly improved, and a new thought is provided for development of synergistic antiviral drugs; and the pharmaceutical co-crystal can keep the skeleton structure ofthe crystal unchanged after long-term placement at room temperature, and the preparation method is simple and easy to implement, low in cost and convenient for large-scale production.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to a drug co-crystal of amantadine hydrochloride and resveratrol and a preparation method thereof. Background technique [0002] In the long course of human history, viral diseases have always been one of the main killers of human health, killing hundreds of millions of people in the past few centuries. In order to defeat the virus, the rapid development of antiviral drugs has attracted much attention. As we all know, the creation of new drugs and the transformation of existing drugs are the eternal themes of drug research and development. However, the creation of new drugs has limitations such as long cycle time, high cost, and high failure rate; and viruses have the characteristics of rapid onset, wide infectivity, and high fatality rate, making it difficult for the traditional new drug research and development model to quickly respond to viral diseases in a short period...

Claims

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Application Information

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IPC IPC(8): C07C211/38C07C209/86C07C39/21C07C37/84A61P31/12
CPCA61P31/12C07B2200/13C07C39/21C07C211/38
Inventor 李延团牛圆圆王凌阳赵明钰吴智勇
Owner OCEAN UNIV OF CHINA
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