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Preparation of zinc linolenate and application thereof in preparation of drugs for resisting helicobacter pylori

A technology of zinc linolenic acid and linolenic acid, applied in the field of medicine, can solve the problems such as failure of radical cure and drug resistance of triple or quadruple therapy, and achieve the effects of alleviating the problem of drug resistance, not easy to resist drug resistance, and high yield

Active Publication Date: 2018-10-09
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the long-term use of antibiotics, H. pylori develops resistance to antibiotics to varying degrees, resulting in the failure of triple or quadruple therapy.

Method used

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  • Preparation of zinc linolenate and application thereof in preparation of drugs for resisting helicobacter pylori
  • Preparation of zinc linolenate and application thereof in preparation of drugs for resisting helicobacter pylori
  • Preparation of zinc linolenate and application thereof in preparation of drugs for resisting helicobacter pylori

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The first step: activate zinc chloride: dissolve 1.36g (1mol / L) of zinc chloride in 10mL of sterile water in the reaction kettle, put the reaction kettle into a drying oven and heat at 160°C, react for 30min, and cool down to room temperature naturally .

[0019] The second step: activated linolenic acid: 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) 766mg, N-hydroxysulfosuccinimide (NHS) 460mg and 560mg of α-linolenic acid (α-LLA) were dissolved in 5mL of EMS solvent, stirred and mixed evenly in a nitrogen atmosphere and activated for 30min.

[0020] The third step: complexation reaction: add activated zinc chloride 1mL (136mg or 1mM) and linolenic acid 5mL (560mg or 2mM) in the reaction kettle, make up 4mL of sterile water, and the liquid is 10mL in total. Mix evenly on the container, control the temperature at 60°C, and react for 3 hours. After the reaction is completed, let it stand and cool overnight.

[0021] The fourth step: dialysis washin...

Embodiment 2

[0024] Step 1: Activation of zinc chloride: Dissolve 1.36g (1mol / L) of zinc chloride in 10mL of sterile water in a reaction kettle, put the reaction kettle into a drying oven and heat at 165°C, react for 30min, and cool naturally.

[0025] The second step: activated linolenic acid: 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) 766mg, N-hydroxysulfosuccinimide (NHS) 460mg and 560mg of α-linolenic acid (α-LLA) were dissolved in 5mL of EMS solvent, stirred and mixed evenly in a nitrogen atmosphere and activated for 30min.

[0026] Step 3: Complexation reaction: Add 1mL (136mg or 1mM) of activated zinc chloride and 4.5mL of linolenic acid (504mg or 1.8mM) to the reaction kettle, add 4.5mL of sterile water, and the liquid is 10mL in total. Mix evenly on a type magnetic stirrer, control the temperature at 70°C, and react for 3 hours. After the reaction is completed, let it stand and cool overnight.

[0027] The fourth step: dialysis washing: put the complexatio...

Embodiment 3

[0030] Step 1: Activate zinc chloride: dissolve 1.36g (1mol / L) of zinc chloride in 10mL of sterile water in the reactor, put the reactor into a drying oven and heat at 170°C, react for 30min, and cool naturally.

[0031] The second step: activated linolenic acid: 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) 766mg, N-hydroxysulfosuccinimide (NHS) 460mg and 560mg of α-linolenic acid (α-LLA) were dissolved in 5mL of EMS solvent, stirred and mixed evenly in a nitrogen atmosphere and activated for 30min.

[0032] The third step: complexation reaction: add 1mL (136mg or 1mM) of activated zinc chloride and 5mL of linolenic acid (504mg or 1.8mM) to the reaction kettle, add 4mL of sterile water, and the liquid is 10mL in total. Mix evenly on a stirrer, control the temperature at 80°C, and react for 2 hours. After the reaction is completed, let it stand and cool overnight.

[0033] The fourth step: dialysis washing: put the complexation reaction solution into a di...

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Abstract

The invention provides preparation of zinc linolenate and application thereof in preparation of drugs for resisting helicobacter pylori. The preparation of the zinc linolenate comprises the steps of dissolving zinc chloride with sterile water, heating and activating a zinc chloride solution by using a reactor, and then naturally cooling the zinc chloride solution to the room temperature; dissolving 1-ethyl-3-(3-dimethyl aminopropyl) carbodiie hydrochlide, N-hydroxysulfosuccinimide sodium salt and linolenic acid in an EMS solvent, and activating in nitrogen; carrying heating reaction on activated zinc chloride and activated linolenic acid, and standing for cooling after reaction is finished; carrying out dialysis in pure water through a dialysis bag until the pure water is clear and transparent; and drying with a vacuum freeze dryer to obtain the zinc linolenate. The zinc linolenate is prepared successively, the yield is high, and the helicobacter pylori inhibiting effect of the zinc linolenate is excellent.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the preparation of zinc linolenate and its application in the preparation of anti-helicobacter pylori drugs. Background technique [0002] Helicobacter pylori (Hp) is a Gram-negative bacterium with a helical shape, microaerophilicity, and harsh growth conditions. Studies have shown that Hp infection can lead to acute and chronic gastritis, gastric and duodenal ulcers, and lymphoproliferative gastric lymphoma, and is related to gastric cancer, liver cancer outside the intestine, and diabetes. In 1994, the World Health Organization classified Hp as a class I carcinogen, which plays a leading role in the development of gastric cancer. At present, the treatment plan for Hp infection is triple or quadruple therapy, that is, taking proton pump inhibitors (omeprazole, etc.) plus two antibiotics (clarithromycin, amoxicillin, tetracycline, metronidazole, etc.) ) or bismuth (bismuth p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C51/41C07C57/12A61K31/202A61P31/04A61P1/04
CPCA61P1/04A61P31/04A61K33/30C07C51/412C07C57/12
Inventor 毕洪凯黄衍强杭旭东曾利平贾佳
Owner NANJING MEDICAL UNIV
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