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Silymarin Methylglucamine clathrate compound and its preparation method

A technology for silymarin meglumine and silymarin, which is applied in the field of inclusion complexes of silymarin meglumine and can solve the problems of insoluble matter, easy deliquescence, instability and the like

Inactive Publication Date: 2005-01-19
烟台同和医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, this product only has two dosage forms of tablet and hard capsule on the market, which is difficult to meet the needs of patients with different clinical conditions at different levels. On the other hand, due to the following three reasons of silymarin meglumine, its application in medicine Application of silymarin meglumine: (1) silymarin meglumine is unstable in aqueous solution, decomposes quickly, and is more unstable under light conditions; (2) silymarin meglumine is hygroscopic, easy to deliquescence, and has a bitter taste; (3) silymarin meglumine In addition to silymarin, the main raw material silymarin also contains isosilymarin, silymarin, silymarin and other impurities, which makes its synthetic product silymarin meglumine not fully soluble in aqueous solution, and there is always a small amount of insoluble matter

Method used

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  • Silymarin Methylglucamine clathrate compound and its preparation method

Examples

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Effect test

example 1

[0020] Dissolve 2.5 grams of 2,6 dimethyl β-cyclodextrin in 100 grams of water, add 1.5 grams of silymarin meglumine, stir for 1 hour, filter the solution, evaporate to dryness under reduced pressure or lyophilize to obtain the package of silymarin meglumine compound.

example 2

[0022] Dissolve 2.6 grams of 2,6-trimethyl-β-cyclodextrin in 100 grams of water, add 1.5 grams of silymarin meglumine, stir for 1 hour, filter the solution, evaporate to dryness under reduced pressure or lyophilize to obtain the package of silymarin meglumine compound.

example 3

[0024] Dissolve 3.5 g of hydroxypropyl β-cyclodextrin in 100 g of water, add 1.5 g of silymarin meglumine, stir for 1 hour, filter the solution, evaporate to dryness under reduced pressure or lyophilize to obtain the inclusion compound of silymarin meglumine.

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PUM

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Abstract

The invention relates to a silymarin meglumine inclusion compound, which is prepared form hepadestal aminomethane and different materials through enclosing technology, the invention also discloses a Silymarin Methylglucamine clathrate compound preparation method.

Description

(1) Technical field: [0001] The invention relates to silymarin meglumine and different inclusion materials, a silymarin meglumine inclusion compound prepared by inclusion technology, and a preparation method of the silymarin meglumine inclusion compound. (two) background technology: [0002] Silymarin meglumine is also called silibinamine. It is a product synthesized from natural extraction drug silymarin (main component is silymarin) and meglumine. Its chemical name is 2-[2,3-dihydro-2-(4- Hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-1,4-benzodioxan-6-yl]-2,3-dihydro-3,5,7-trihydroxy- 4H-1-Benzopyran-4-one meglumine salt; English name: Silybin Meglumine; Molecular formula: C 32 h 39 o 15 N; structural formula: [0003] [0004] It has pharmacological effects such as direct elimination of active oxygen, protection of liver cell membrane, promotion of DNA and structural protein synthesis of damaged liver cells, immune regulation and anti-hepatic fibrosis. It is mainly su...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/357A61P1/16A61P31/12
Inventor 吴新华张传林张晓亮孙兰亭
Owner 烟台同和医药科技有限公司
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