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High content troxerutin medicine and its preparing method

A high-content, drug-based technology, applied to medical preparations containing active ingredients, drug combinations, and pharmaceutical formulas, can solve the problems of drugs affecting the safety of clinical medication, product quality stability, limited use range, and reduced curative effect. Low cost, high product quality, high curative effect

Inactive Publication Date: 2004-12-15
SICHUAN XIELI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] As we all know, the purity of drugs will directly affect the safety of clinical medication and the stability of product quality, especially when injecting drugs, there will often be toxic and side effects and irritation, thus limiting the scope of clinical use of such drugs, At the same time, the efficacy will be significantly reduced

Method used

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  • High content troxerutin medicine and its preparing method
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  • High content troxerutin medicine and its preparing method

Examples

Experimental program
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Effect test

Embodiment 1

[0023] A high-content troxerutin medicine is characterized in that the active substance is a compound represented by structural formula (I) with a liquid chromatography content equal to 90.7%.

[0024] The preparation method of above-mentioned pharmaceutically active substance (I) described in the present invention comprises the hydroxyethylation reaction of reaction stage, the heating, cooling, filtering, drying operation of thermal filtration, concentration and refining stage, concrete process step is as follows:

[0025] A. Reaction stage: 650 grams of rutin, 2700 grams of methanol, and 8 grams of pyridine were added to the reaction kettle, then ethylene oxide was introduced, and the reaction was closed at 40°C for 10 hours, 7 grams of activated carbon was added, and hot filtration was carried out. The filtrate was vacuum-dried to obtain a yellow solid crude product.

[0026] B, refining stage: add 1500 grams of methanol to the crude product obtained in step A, heat and ref...

Embodiment 2

[0028] A high-content troxerutin medicine is characterized in that the active substance is a compound represented by structural formula (I) with a liquid chromatography content equal to 90.6%.

[0029] The preparation method of above-mentioned pharmaceutically active substance (I) described in the present invention comprises the hydroxyethylation reaction of reaction stage, the heating, cooling, filtering, drying operation of thermal filtration, concentration and refining stage, concrete process step is as follows:

[0030] A. Reaction stage: 650 grams of rutin, 3000 grams of methanol, and 12 grams of pyridine were added to the reaction kettle, then ethylene oxide was introduced, and the reaction was closed at 60 ° C for 8 hours, 7 grams of activated carbon was added, and hot filtration was carried out. The filtrate was vacuum-dried to obtain a yellow solid crude product.

[0031] B. Refining stage: add 2000 grams of ethanol to the crude product obtained in step A, heat and re...

Embodiment 3

[0033] A high-content troxerutin medicine is characterized in that the active substance is a compound represented by structural formula (I) with a liquid chromatography content equal to 91.2%.

[0034] The preparation method of above-mentioned pharmaceutically active substance (I) described in the present invention comprises the hydroxyethylation reaction of reaction stage, the heating, cooling, filtering, drying operation of thermal filtration, concentration and refining stage, concrete process step is as follows:

[0035] A. Reaction stage: 650 grams of rutin, 2700 grams of methanol, and 12 grams of pyridine were added to the reaction kettle, and then ethylene oxide was passed into it, and the airtight reaction was carried out at 40°C for 9 hours, and 7 grams of activated carbon was added, followed by hot filtration. The filtrate was vacuum-dried to obtain a yellow solid crude product.

[0036] B, refining stage: add 1500 grams of methanol to the crude product obtained in st...

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Abstract

The present invention discloses a troxerutin medicine with content of active matter 3', 4', 7-trihydroxy rutin over 90%. The active matter has molecular expression of C33H42O19 and molecular weight of 742.68. The preparation process includes the reaction stage comprising hydroxyethylation reaction, hot filtering and concentration; and the refining stage comprising heating, cooling, filtering and drying. The preparation process has high yield, low cost, simple and fast operation and high product quality, and is suitable for preparation of different medicine preparation forms.

Description

Technical field: [0001] The present invention relates to a troxerutin drug and a preparation method thereof, in particular to a troxerutin drug with a high content of active substance 3', 4', 7-trihydroxyethyl rutin greater than 90% and its preparation method. Preparation. technical background: [0002] Troxerutin is a water-soluble product obtained by hydroxyethylation of rutin, which has better absorption in the body and more significant curative effect than rutin. Among them, the 3', 4', 7-trihydroxyethyl rutin obtained by hydroxyethylation of the phenolic hydroxyl groups at the 3', 4', and 7 positions is the main component and has the greatest curative effect. [0003] Troxerutin can maintain the normal permeability of capillaries, and has a good therapeutic effect on edema caused by abnormally increased capillary permeability, increases the rheology of blood cells, reduces blood viscosity, and reduces the aggregation of platelets and red blood cells. It can be used to...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P7/02A61P9/00
Inventor 张光耀
Owner SICHUAN XIELI PHARM CO LTD
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