The New Indication of Oral Ranitidine in the Treatment of Erosive Esophagitis

A technology for ranitidine and esophagitis, applied in the field of medicine, can solve the problems of no effective treatment for erosive esophagitis, reduce vitamin B12 absorption, affect the health of patients, etc., achieve long drug action time and high bioavailability , to avoid the effect of indigestion

Active Publication Date: 2021-05-18
SHANGHAI JINCHENG PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there is no effective drug for the treatment of erosive esophagitis
[0005] In addition, according to relevant studies, ranitidine has no significant curative effect on some patients with severe gastrointestinal mucosal damage, has low bioavailability, requires a long treatment cycle, and is prone to other complications during treatment. For example, it will continue to reduce the acidity of gastric juice, cause bacteria to multiply in the gastrointestinal tract, and reduce the nitrate in food to nitrite, forming N-nitroso compounds, which will affect the health of patients; it will also reduce the level of vitamin B12 Absorption, resulting in some diseases caused by vitamin B12 deficiency, such as peptic ulcer, slow mucosal healing, etc.

Method used

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  • The New Indication of Oral Ranitidine in the Treatment of Erosive Esophagitis
  • The New Indication of Oral Ranitidine in the Treatment of Erosive Esophagitis
  • The New Indication of Oral Ranitidine in the Treatment of Erosive Esophagitis

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preparation example Construction

[0044] In a second aspect, the present invention provides a method for preparing ranitidine, the method comprising the following steps:

[0045] Step 1, 2-[[[5-(dimethylamino) methyl-2-furan] methyl] thio] ethylamine and N-methyl-1-methylthio-2-nitroethyleneamine respectively Dissolved in a solvent to make a solution, mix the two, and heat to a certain temperature to react.

[0046] According to one and a preferred embodiment of the present invention, the solvent is an organic solvent and / or water.

[0047] In a further preferred embodiment, the solvent is water, preferably distilled water.

[0048] In the present invention, impurity B For the unreacted 2-[[[5-(dimethylamino)methyl-2-furan]methyl]sulfanyl]ethylamine, the inventor found through research that distilled water is selected as the solvent for dissolving raw materials, which is beneficial to The reaction time is shortened, the yield is increased, and the synthesis reaction is fully carried out, so the content of ...

Embodiment approach

[0049] According to a preferred embodiment of the present invention, the 2-[[[5-(dimethylamino)methyl-2-furan]methyl]sulfanyl]ethylamine solution and N-methyl-1-methylthio The molar ratio of the base-2-nitrovinylamine solution is (1.0-3.0):1, preferably (1.1-2.5):1, more preferably (1.2-2.0):1.

[0050] In the present invention, impurity C For unreacted N-methyl-1-methylthio-2-nitroethyleneamine, the inventor found through research that 2-[[[5-(dimethylamino)methyl-2-furan] Methyl]thio]ethylamine and N-methyl-1-methylthio-2-nitroethyleneamine are set to (1.0~3.0):1, preferably (1.1~2.5):1, more preferably (1.2~2.0): The molar ratio of 1 can make the raw material react fully, the surplus is little, effectively reduces the content of impurity B and impurity C, thereby improves the medicine stability of the prepared ranitidine.

[0051] In a further preferred embodiment, the 2-[[[5-(dimethylamino)methyl-2-furan]methyl]thio]ethanamine solution and N-methyl-1-methylthio- 2-Nitro...

Embodiment 1

[0240] The preparation of embodiment 1 ranitidine

[0241] (1) 170g of 2-[[[5-(dimethylamino)methyl-2-furan]methyl]sulfanyl]ethylamine and 90.3g N-methyl-1-methylthio-2-nitro Vinylamine was dissolved in 100ml of distilled water respectively to make a solution. Take the same volume (50mL respectively) of the configured solution, and mix it dropwise at a rate of 2.4mL / min and a stirring rate of 180r / min. Afterwards, the temperature was raised to 42° C. at a heating rate of 2.5° C. / min, and kept for 6 hours until the reaction was completed, and an orange-yellow reaction liquid was obtained;

[0242] (2) Add 50mL, 2mol / L hydrochloric acid to the above reaction solution, then adjust the pH to 3.5, then add 200mL methylene chloride to the reaction solution for extraction, mix well, let stand, and separate to obtain an organic phase and an aqueous phase , wherein the water phase is 180mL; adopt 15% potassium carbonate solution to adjust the pH of the water phase to 9, then add 720...

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Abstract

The invention discloses a ranitidine and a preparation method thereof, as well as a ranitidine preparation, a compound preparation and a preparation method thereof. Among them, ranitidine has low impurity content, high stability and simple preparation method; the ranitidine preparation and compound preparation prepared therefrom have high bioavailability and safety. The ranitidine, the ranitidine preparation and the compound preparation provided by the invention can effectively treat and maintain the treatment of erosive esophagitis.

Description

technical field [0001] The invention belongs to the field of medicine, and specifically relates to ranitidine, a ranitidine preparation, a preparation method and an application thereof. Background technique [0002] Ranitidine, also known as furan nitroamine, chemically named N'-methyl-N-[2-[[[5-[(dimethylamino)methyl]-2-furyl]methyl]thio ]Ethyl]-2-nitro-1,1-ethylenediamine hydrochloride is a potent histamine H2 receptor antagonist. It can effectively inhibit the secretion of gastric acid stimulated by histamine, pentagastrin and carbamylcholine, and reduce the activity of gastric acid and gastric enzymes. It is mainly used for the treatment of hyperacidity and heartburn. Its efficacy in inhibiting gastric acid secretion In moles, it is 5 to 12 times that of cimetidine. [0003] With the development of society and the acceleration of the pace of life, unhealthy lifestyles (such as: staying up late, emotional stress, smoking, drinking, etc.) lead to frequent attacks of gast...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/52A61K31/341A61P1/04
CPCA61K9/0053A61K31/341A61P1/04C07D307/52
Inventor 上官日红戴浙敏陆成
Owner SHANGHAI JINCHENG PHARMACEUTICAL CO LTD
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