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Potassium tiopronin as well as preparation and uses thereof

A technology of tiopronin potassium and tiopronin, which is applied in the field of medicine, can solve the problems of increasing the risk of clinical use, cumbersome operation process, easy to be infected with bacteria, etc., and achieve the effect of good medicinal effect, high purity and good stability

Inactive Publication Date: 2008-06-25
CHANGZHOU NO 4 PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The operation process is cumbersome, and it is easy to be infected with bacteria during use
It is also reported in the literature that tiopronin is easily decomposed in the process of being neutralized by acid to neutral in the water phase to produce a large number of by-products, which will cause harm to the human body and increase the risk of clinical use.

Method used

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  • Potassium tiopronin as well as preparation and uses thereof
  • Potassium tiopronin as well as preparation and uses thereof
  • Potassium tiopronin as well as preparation and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1. Tiopronin potassium and preparation method thereof

[0026] Weigh 99.88g (0.612mol) of tiopronin, put it in a three-neck flask, add 280ml of analytical pure methanol, put it in a water bath at 15°C, add 1.0g of mercaptoprotectant 2-mercaptoethanol, and stir for 20 minutes. Weigh 28.02g of NaOH, and add it into the methanol solution in 4 times (7g each time), with an interval of 1.5 hours between each time; after adding NaOH for the 4th time, continue to react in a 15°C water bath for 1 hour while stirring. Then, the reaction bottle was moved into a 25°C water bath and stirred for 1 hour. Suction filtration, the filtrate was added in 800ml of ethyl acetate, fully shaken to mix evenly; a large amount of white precipitate appeared in the reaction solution, suction filtration, and the filter cake was dried at 80°C to obtain 87.71g of tiopronin potassium, with a yield of 71.20% .

[0027] Elemental analysis result (%): C29.69, H3.98, N6.81, K19.38, theoretica...

Embodiment 2

[0029] Embodiment two. tiopronin potassium crystalline hydrate and preparation method thereof

[0030] Take 99.92 g (0.612 mol) of tiopronin, place it in a three-necked flask, add 200 ml of analytically pure isobutanol, and stir in a water bath at 15° C. for 20 minutes. Take by weighing 2-ethylhexanolate potassium 118g, add in the isobutanol liquid (each adding 29.5g) in 4 times, every interval 1.5 hours; After adding 2-ethylhexanolate potassium for the 4th time, continue to °C for 1 hour under stirring in a water bath. Then, the reaction bottle was moved into a 25°C water bath and stirred for 1 hour. Filtrate with suction, add 800ml of water to the filtrate, shake fully to make the mixture uniform; when a large amount of white precipitate appears in the reaction solution, filter with suction, and vacuum dry the filter cake at 60°C for 5 hours to obtain 96.53g of off-white solid, yield 71.92%. According to thermogravimetric and differential thermal analysis, it contains a m...

Embodiment 3

[0032] Embodiment three. the preparation of tiopronin potassium tablet

[0033] Get 123 grams of tiopronin potassium prepared in Example 1, add an appropriate amount of carrier auxiliary materials (such as starch, lactose, mannitol, dextrin, hydroxypropyl cellulose, povidone, magnesium stearate, etc.), wet granulation , drying, and tableting with a tablet machine, each tablet has a specification of 100 mg (calculated as tiopronin), for oral use.

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PUM

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Abstract

The invention relates to a medicine-potassium tiopronin used for curing acute and chronic hepatopathy, a method for manufacturing the same and the application in medication. The tiopronin is prepared into potassium salt so as to increase the potassium salt supplement for hepatopaths, and thus the electrolyte balance disorder of hepatopaths is adjusted. The manufacturing method comprises the following steps of: adding tiopronin and potassic inorganic base in organic solvent to undergo the acids-bases salifying reaction with sulfhydryl protecting group assisted in the reaction process; adding precipitator in the system to precipitate at the end of reaction; filtering and drying; finally obtaining potassium tiopronin.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a potassium salt compound of tiopronin, a preparation method thereof and an application thereof in medicine. Background technique [0002] Tiopronin (English name Tiopronin, chemical name: mercaptopropionylglycine) is a metabolism-improving antidote, its molecular formula: C5H9NO3S, molecular weight: 163.19, and its structural formula is as follows: [0003] [0004] Tiopronin is mainly used for the improvement of liver function in acute and chronic liver diseases. Currently on the market there are oral formulations of tiopronin, freeze-dried powder injections and water injections. Tiopronin is strongly acidic, and most of the existing preparations are formulated as neutral for use. For example, tiopronin freeze-dried powder injection is prepared with a special solvent, sodium bicarbonate aqueous solution. In clinical use, tiopronin is dissolved in aqueous sodi...

Claims

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Application Information

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IPC IPC(8): C07C319/12C07C319/28C07C323/52A61K31/198A61P1/16
CPCY02P20/55
Inventor 庄苏静屠永锐
Owner CHANGZHOU NO 4 PHARMA FACTORY
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