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Method for preparing berberinc derivate

The technology of a derivative, berberine, is applied in the field of preparation of berberine derivatives, which can solve the problem that berberine derivatives have no biological activity, and achieve the effects of improving oral glucose tolerance, improving insulin resistance, and promoting insulin secretion

Inactive Publication Date: 2008-04-09
TONGJI HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Some performance research experiments on the berberine derivatives have also been carried out in the paper, but the conclusion is that the berberine derivatives have almost no biological activity

Method used

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  • Method for preparing berberinc derivate
  • Method for preparing berberinc derivate
  • Method for preparing berberinc derivate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the preparation of alcoholic berberine

[0035]Dissolve 5g of berberine bisulfate powder in distilled water to prepare a saturated solution of about 120ml; add dropwise a 20% sodium hydroxide solution until no precipitation occurs; filter the formed turbid solution to obtain the precipitate Dissolve the precipitate in the organic solvent ether, filter the solution, add the resulting filtrate dropwise to 20 g of silica gel G, evaporate the ether to dryness at room temperature, put it into the silica gel G column (silica gel G500 g) by dry method, and elute with ether; Deliquification and concentration under reduced pressure, vacuum low-temperature drying under the conditions of a vacuum degree of less than 150mbar and a temperature of less than 60°C, to obtain 2.21g of a crude product; then recrystallize the crude product with methanol or ethanol, and dry it into a yellow powder, namely 1.78g of pure alcoholic berberine can be obtained.

Embodiment 2

[0036] Embodiment 2: the preparation of the tablet taking alcoholic berberine as active ingredient

[0037] The ratio of alcoholic berberine 10mg, lactose 187mg, cornstarch 50mg, and magnesium stearate 3mg prepared in Example 1 is taken by weighing raw materials, and alcoholic berberine, lactose and cornstarch are mixed uniformly earlier, and the Wet with 70% ethanol, then sieve the wet mixture, granulate, dry, sieve again, add magnesium stearate, and finally compress the mixture into tablets, each tablet weighs 250 mg, and the active ingredient content is 10 mg.

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Abstract

The invention relates to a preparation method of berberine derivative-alcohol form berberine which includes the following steps: the raw materials of berberine hydrogen sulfate are dissolved in water to prepare the saturated solution of berberine hydrogen sulfate; alkaline solution is dropped in the saturated solution of berberine hydrogen sulfate till no generation of the sediment so as to form the turbid solution; the turbid solution is filtered to get the sediments; all the sediments are dissolved in the organic solvent and are carried out the silica gel column chromatography and elution by organic solvent; the crude product can be obtained by concentration under the reduced pressure of the organic solvent elution solution and vacuum low-temperature drying; the obtained crude product is carried out the recrystallization by using methanol or ethanol so as to get enough amount of berberine derivative pure product. The animal experiments find that the prepared berberine derivative has a variety of pharmaceutical activities and shows the great function of regulating the blood glucose and blood lipids of the rats with the type 2 diabetes, compared with the currently recognized berberine hydrochloride compounds which have the function of regulating the blood glucose and blood lipids and the most relevant structure, the efficacy is much better and the effective dose is much less.

Description

[0001] The present invention is a divisional application with the filing date of June 29, 2006, the application number of 200610019492.4, and the title of the invention "Berberine derivatives and their preparation methods, pharmaceutical compositions and uses thereof". technical field [0002] The invention relates to a method for chemically modifying and synthesizing a berberine (BBR) as a matrix, in particular to a method for preparing a berberine derivative. Background technique [0003] At present, diabetes has become a worldwide epidemic. According to statistics, the prevalence of type 2 diabetes in China was 1.0% in 1976, 2.0% in 1989, 3.2% in 1996, and more than 9% in Shanghai and Guangzhou in 2001. %, already higher than the average level of developed countries in Europe and America. Diabetes has become the "third largest killer" of human beings, and the related medical care costs are extremely large, even in economically developed countries. [0004] Berberine (BBR...

Claims

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Application Information

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IPC IPC(8): C07D455/03
Inventor 徐丽君陆付耳魏世超
Owner TONGJI HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI TECH
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