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Water-soluble salt of secnidazole and preparation method thereof

A technology of secnidazole and water-soluble salt, applied in the field of secnidazole water-soluble salt and its preparation, can solve the problems of long time, increase of secnidazole water solubility, pain of patients, etc., and achieve the goal of reducing drug pressure Effect

Inactive Publication Date: 2010-10-20
HEFEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, when secnidazole is instilled, the amount of solvent is large and the time is long, which causes unnecessary pain to the patient.
In addition, the large amount of solvent also brings inconvenience to the production and storage process.
[0005] U.S. Patent No. 5,574,167 prepared a series of benzoate and fatty acid esters of secnidazole for the purpose of improving stability and improving adverse reactions, but failed to improve the water solubility of secnidazole

Method used

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  • Water-soluble salt of secnidazole and preparation method thereof
  • Water-soluble salt of secnidazole and preparation method thereof
  • Water-soluble salt of secnidazole and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 Preparation of secnidazole phosphate disodium salt

[0029] Dissolve 4.6g of phosphorus oxychloride in 60mL of DMC at room temperature, put it into a three-necked flask, add 5.5g of secnidazole several times under stirring, stir for 2 hours after the addition, and precipitate a large amount of off-white solid. Raise the temperature to reflux and stir the reaction for more than 10 hours until no more acid gas is released. The liquid was poured out and distilled to dryness under reduced pressure to obtain a red solid residue. 25mL of water was added under stirring, and stirred at 50°C for 1h for hydrolysis. Activated carbon decolorizes and filters, and concentrates to dryness under reduced pressure below 60°C to obtain a reddish-brown clear transparent oil (solid after cooling), which mainly contains secnidazole phosphate. Add an appropriate amount of 90% methanol to fully dissolve, add a slight excess of sodium carbonate several times in a 40°C water bath ...

Embodiment 2

[0031] Embodiment 2 Preparation of secnidazole dipotassium phosphate

[0032] The same operation as in Example 1, but sodium carbonate was changed to potassium carbonate, and the product was vacuum-dried at 160° C., and 5.5 g of secnidazole was added to obtain 5.6 g of anhydrous secnidazole dipotassium phosphate.

Embodiment 3

[0033] Embodiment 3 secnidazole succinic acid monoester

[0034] Cyclohexane 50ml, succinic anhydride 2.5g and pyridine 0.1mL, mix well and heat to 70°C; add 4.625g secnidazole. Reflux for more than 18 hours. Cool the reaction solution to room temperature, thick solids precipitate out at the bottom of the flask, pour out the upper liquid, add an appropriate amount of ether / carbon disulfide (4:1) to the flask, heat and stir to precipitate solids, filter, and dry to obtain secnidazole amber Acid monoester 5.2g, melting point 103-105°C. The solid is soluble in water and ethanol.

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PUM

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Abstract

The invention relates to a water-soluble derivative of a secnidazole medicament for treating amebic dysentery, namely secnidazole phosphate or succinic monoester salt. A compound with the structure is the chemical derivative of secnidazole, and can play the medicinal effect in a range of the secnidazole. The water solubility of the derivative is remarkably superior to that of the secnidazole, so the derivative can be prepared into formulations which cannot be prepared from the secnidazole such as injection powder. The invention also relates to a preparation method for the secnidazole phosphate and the secnidazole succinic monoester salt.

Description

[0001] The present invention is a divisional application, the original application number is 200810023502.0, the application date is 2008.03.28, the applicant is Hefei University of Technology, and the invention name is a water-soluble salt of secnidazole and its preparation method. 1. Technical field [0002] The invention relates to a modified chemical drug and a modification method thereof, in particular to a water-soluble secnidazole salt and a preparation method thereof. 2. Background technology: [0003] Amoeba and protozoa have seriously affected human health. There are as many as 500 million people in the world carrying amoeba histolytica, about 250 million people infected with Giardia, and more than 200 million people infected with Trichomonas. Secnidazole is very effective in the treatment of the above infections. Secnidazole, chemical name: 1-(2-hydroxypropyl)-2-methyl-5-nitroimidazole. It has been reported that a single dose of secnidazole 2g (or 30mg / Kg) is adm...

Claims

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Application Information

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IPC IPC(8): C07D233/94
Inventor 姚日生邹国勇邓胜松朱慧霞何红波
Owner HEFEI UNIV OF TECH
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