Armiharisin succinic mono ester with cholagogic effect, and its salt and medicinal composition

A technology of succinic acid monoester and leucicillin A, applied in the field of medicine, can solve problems such as toxic side effects and lower drug safety

Active Publication Date: 2007-03-28
海南神州康盛医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the addition or improper use of these solubilizers of...

Method used

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  • Armiharisin succinic mono ester with cholagogic effect, and its salt and medicinal composition
  • Armiharisin succinic mono ester with cholagogic effect, and its salt and medicinal composition
  • Armiharisin succinic mono ester with cholagogic effect, and its salt and medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 Preparation of Leucocin A Succinate Monoester (Method 1)

[0018] Add 20g (0.085mol) of Leucocin A, 46.9g (0.34 mol) of anhydrous potassium carbonate, 300ml of ethyl acetate and 100ml of anhydrous N,N-dimethylformamide into a 500ml round bottom flask, oil bath 109 Reflux for 1 hour at °C. A yellow solid gradually precipitated from the reaction liquid. 34g (0.34mol) of succinic anhydride was added, the solid part of the reaction solution was dissolved, and the reaction was refluxed for 30 hours, cooled to room temperature, and filtered with suction. The obtained solid was washed with a small amount of ethyl acetate. The filter cake was dissolved in an appropriate amount of water, and 10% hydrochloric acid was used. Adjust to pH 3.5, stir for 0.5 hours, and filter with suction to obtain part of the product. Concentrate the filtrate to recover ethyl acetate, add 200 ml of water to the concentrate, adjust the pH to 3.5 with 10% hydrochloric acid, stir for 0.5 hours, a...

Embodiment 2

[0089] Example 2 Preparation of Leucocin A Succinate Sodium

[0090] Dissolve 1.67g (5mmol) of Leucocin A succinate monoester in 60ml of methanol, add 0.42g (5mmol) of sodium bicarbonate powder at room temperature while stirring, and after stirring at room temperature for 20 minutes, a large amount of yellow-green solid precipitates out, continue to stir and react 3 After hours, suction filtration, the filter cake was washed with a small amount of methanol, and after vacuum drying, 1.44 g of yellow-green powdery solid was obtained, mp197-198.5°C, and the yield was 81%.

Embodiment 3

[0091] Example 3 Preparation of leucine A succinate monoester lysine salt

[0092] Dissolve 1.67g (5mmol) of Leucocin A succinate monoester in 30ml of tetrahydrofuran, add 0.82g (5mmol) of lysine at room temperature while stirring, and react with stirring for 12 hours at room temperature. Quickly filter with suction to obtain a light yellow solid. Transfer to a vacuum dryer, vacuum drying at 50°C for 4 hours to obtain product 2.2g, mp175-177°C, yield 90%.

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Abstract

The invention relates to an Armillarisinum hemisuccinate and the preparing method and use thereof. And it can be made by acylation reaction of Armillarisinum and succinic anhydride; besides, the invention also relates to its pharmaceutically acceptable salts, such as K salts, Na salts, Ca salts and Mg salts, as well as the salts formed of it and basic amino acid, including lysine and arginine salts. And the pharmacological experiments indicate it has obvious cholagogue effect. And the combination of it or its pharmaceutically acceptable salts as active components and corresponding medicinal dressing can be made into oral and intravenous preparations for curing acute cholecystitis, acute attack of chronic cholecystitis, acute biliary passage infection (including calculus type and parasite type), and acute and chronic hepatitides.

Description

Technical field [0001] The present invention belongs to the field of medicine, and relates to leucin A succinate monoester and its preparation method and use. At the same time, the present invention also relates to a pharmaceutically acceptable salt of leucin A succinate and its preparation method and use, such as potassium Salt, sodium salt, calcium salt, magnesium salt, etc., and the salt formed with basic amino acid include lysine salt and arginine salt. The pharmacological experiment shows that the succinate of leucocetin A succinate has obvious choleretic effect, and the combination of succinate of leucocetin A or its pharmaceutically acceptable salt as the active ingredient and the corresponding medicinal dressing can be made for oral administration. And the preparation for intravenous administration, used for the treatment of acute cholecystitis, acute attack of chronic cholecystitis, acute biliary infection (including stone and parasitic) and acute and chronic hepatitis. ...

Claims

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Application Information

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IPC IPC(8): C07D311/18A61K31/37A61P1/16
Inventor 王绍杰
Owner 海南神州康盛医药科技有限公司
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