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

A technology of succinic acid monoester and leucectin A, applied in the field of medicine, can solve the problems of reducing drug safety, toxic and side effects, etc.

Active Publication Date: 2008-09-24
海南神州康盛医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the addition or improper use of these solubilizers often causes toxic and side effects and reduces the safety of the drug.

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] The preparation (method 1) of embodiment 1 leucidin A succinic acid monoester

[0018] Add 20g (0.085mol) of leucidin A, 46.9g (0.34mol) of anhydrous potassium carbonate, 300ml of ethyl acetate and 100ml of anhydrous N, N-dimethylformamide into a 500ml round-bottomed flask, oil bath 109 °C for 1 hour at reflux. A yellow solid gradually precipitated out of the reaction solution. Add 34 g (0.34 mol) of succinic anhydride, the solids in the reaction solution are partially dissolved, reflux for 30 hours, cool to room temperature, filter with suction, wash the obtained solid with a small amount of ethyl acetate, dissolve the filter cake in an appropriate amount of water, and wash with 10% hydrochloric acid Adjust to pH 3.5, stir for 0.5 hour, and filter with suction to obtain some products. 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 hour, and filter with suction to...

Embodiment 2

[0084] The preparation of embodiment 2 leucidin A succinate monoester sodium

[0085] Dissolve 1.67g (5mmol) succinic acid monoester of leucidin A in 60ml of methanol, add 0.42g (5mmol) sodium bicarbonate powder at room temperature under stirring, and stir at room temperature for 20 minutes to precipitate a large amount of yellow-green solid, continue to stir for reaction 3 After 1 hour, filter with suction, wash the filter cake with a small amount of methanol, and dry in vacuo to obtain 1.44 g of a yellow-green powdery solid, mp 197-198.5° C., yield 81%.

Embodiment 3

[0086] The preparation of embodiment 3 Leucidin A succinic acid monoester lysine salt

[0087] Dissolve 1.67g (5mmol) succinic acid monoester of leucectin A in 30ml tetrahydrofuran, add 0.82g (5mmol) lysine at room temperature under stirring, stir and react at room temperature for 12 hours, quickly filter to obtain a light yellow solid, immediately Transfer to a vacuum dryer, and vacuum-dry at 50°C for 4 hours to obtain 2.2g of the product, 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 invention belongs to the field of medicine, and relates to a succinic acid monoester and its preparation method and use. At the same time, the present invention also relates to a pharmaceutically acceptable salt of a succinic acid monoester and its preparation method and use, such as potassium Salts, sodium salts, calcium salts and magnesium salts, etc., and salts with basic amino acids include lysine salts and arginine salts. Pharmacological experiments show that leucectin A succinate monoester has obvious choleretic effect, and leucectin A succinate monoester or its pharmaceutically acceptable salt is used as the active ingredient in combination with corresponding medicinal dressings and can be made for oral administration And preparations for intravenous administration, for the treatment of acute cholecystitis, acute exacerbation of chronic cholecystitis, acute biliary tract infection (including calculous, parasitic) and acute and chronic hepatiti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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