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Preparation method and application of compound salt formed by glucuronic acid or glucurolactone and sophocarpidine and/or oxymatrine

A technology of glucuronic acid and glucuronide is applied in the field of preparation of double salts, can solve problems such as reduction, and achieve the effects of simple preparation method, reduced dosage of medicines, and reduced stimulation of medicines

Inactive Publication Date: 2018-12-14
刘兆平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the deficiency of existing single compound glucuronolactone or glucuronic acid and matrine, matrine in the clinical curative effect and therapeutic range, and to provide a kind of liver disease therapeutic effect better than sodium glucuronate, sodium glucuronate, A double salt of glucuronic acid or glucuronolactone, matrine and / or matrine of any single compound in glucuronolactone, matrine, and matrine and a preparation method thereof, and the double salt is characterized in that Reduce the pH value of matrine and matrine, reduce drug stimulation, and play a synergistic and complementary role between the raw materials for preparing the double salt

Method used

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  • Preparation method and application of compound salt formed by glucuronic acid or glucurolactone and sophocarpidine and/or oxymatrine
  • Preparation method and application of compound salt formed by glucuronic acid or glucurolactone and sophocarpidine and/or oxymatrine
  • Preparation method and application of compound salt formed by glucuronic acid or glucurolactone and sophocarpidine and/or oxymatrine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A kind of preparation method of the double salt that is formed by glucuronic acid and matrine as follows, concrete steps are as follows:

[0030] (1) Add 5 g of a mixture of glucuronic acid and matrine in an equimolar ratio to a 100 ml reaction flask, then add 50 ml of methanol, stir and reflux in a water bath at 20° C. until clarification;

[0031] (2) evaporating and concentrating the clear liquid obtained in step (1) at 40°C;

[0032] (3) cooling the concentrated product, refrigerating and crystallizing for 12-24 hours, filtering, washing, and vacuum drying;

[0033]

[0034] where x=1, y=1, z=0.

Embodiment 2

[0036] A kind of preparation method of the double salt that following formula is formed by glucuronic acid and matrine, concrete steps are as follows:

[0037] (1) Add 5 g of a mixture of glucuronic acid and matrine in an equimolar ratio to a 100 ml reaction flask, then add 50 ml of acetone, stir and reflux in a water bath at 40 ° C until clarification;

[0038] (2) evaporating and concentrating the clear liquid obtained in step (1) at 60°C;

[0039] (3) cooling the concentrated product, refrigerating and crystallizing for 12-24 hours, filtering, washing, and vacuum drying;

[0040]

[0041] where x=1, y=0, z=1.

Embodiment 3

[0043] A kind of preparation method of the double salt that following formula is formed by glucuronic acid, matrine and matrine, concrete steps are as follows:

[0044] (1) Add 5 g of a mixture of glucuronic acid, matrine and matrine in an equimolar ratio to a 100 ml reaction bottle, then add 50 ml of ethanol, stir and reflux in a water bath at 60 ° C until clarification;

[0045] (2) evaporating and concentrating the clear liquid obtained in step (1) at 80°C;

[0046] (3) cooling the concentrated product, refrigerating and crystallizing for 12-24 hours, filtering, washing, and vacuum drying;

[0047]

[0048] where x=1, y=1, z=1.

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Abstract

The invention discloses a preparation method of compound salt formed by glucuronic acid or glucurolactone and sophocarpidine and / or oxymatrine. The preparation method comprises specific steps as follows: water and an organic solvent are added to a mixture of glucuronic acid or glucurolactone and sophocarpidine and / or oxymatrine, and a mixed solution is stirred and subjected to refluxing under thewater-bath condition at 20-60 DEG C until the mixed solution is clear; an obtained clear liquid is evaporated and concentrated at 40-80 DEG C; a concentrated product is cooled, refrigerated and then filtered, and washing and vacuum drying are performed. The invention further discloses pharmaceutical composition containing the compound salt and pharmaceutically acceptable auxiliary materials and used for treating hepatic diseases. Animal experiments prove that glucuronic acid or glucurolactone and sophocarpidine and / or oxymatrine have synergistic effects and do not have toxic or side effects onanimals.

Description

technical field [0001] The invention relates to a preparation method and application of a double salt, in particular to a preparation method and application of a double salt formed of glucuronic acid or glucuronolactone, matrine and / or matrine, and belongs to the field of medicinal chemistry. Background technique [0002] Matrine and matrine are alkaloids isolated from the roots of the leguminous plant Sophora flavescens or the root of the flat family plant broad bean. In recent years, domestic and foreign studies on matrine and matrine have found that matrine not only has anti-hepatitis virus, anti-hepatic fibrosis, immune regulation, anti-tumor, anti-inflammation, anti-allergic and many other effects. Pharmacological activity, also has obvious cardiotonic, anti-arrhythmia, lowering blood pressure, relieving asthma, scavenging free radicals, anti-radiation, sedative and analgesic effects, in addition, it is still used for the treatment of vaginitis, parasitic diseases (such...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H13/02C07H7/033C07D471/22C07H1/00A61K31/7048A61K31/4375A61K31/7012A61P1/16
CPCC07H13/02A61P1/16C07D471/22C07H1/00C07H7/033
Inventor 刘兆平
Owner 刘兆平
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