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Composition containing alisol A and alisol A 24-acetic ester and use

A technology of alisitol and acetate, which is applied in the direction of medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., can solve problems such as poor stability, unsuitable for making medicines with stable quality, and low development feasibility , to achieve the effect of less toxicity

Active Publication Date: 2009-04-22
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported in the literature that the stability of alisitol B 23-acetate is poor, and it is prone to structural transformation at room temperature, so it is not suitable for making medicines with stable quality; 0.03%, and the difficulty of synthesis is relatively high, and the development feasibility is small

Method used

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  • Composition containing alisol A and alisol A 24-acetic ester and use
  • Composition containing alisol A and alisol A 24-acetic ester and use
  • Composition containing alisol A and alisol A 24-acetic ester and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Extraction of medicinal materials:

[0053] Method 1: Take 1 kg of dried tubers of Alisma orientalis (Sam.) Juzep., a plant of the family Alismaceae, make decoction pieces, and reflux extract with 7000ml of ethyl acetate twice, each time for 0.5 hours. The extracts were combined, and the solvent was recovered under reduced pressure to obtain 35 g of dark brown extract.

[0054] Method 2: Take 3 kilograms of dried tubers of Alisma orientalis (Sam.) Juzep., grind them into coarse particles, leak them with 70% ethanol, combine the leaked fluids, recover the solvent under reduced pressure, and obtain dark brown soaked tubers. Cream 115g.

[0055] Method 3: Take 2 kg of dry tubers of Alisma orientalis (Sam.) Juzep., crush them into coarse particles, and place them in CO 2 In supercritical extractor, extraction condition: CO 2 The pressure is 25-36MPa, the extraction temperature is 40-55°C, and the extraction time is 1.5h to obtain 61g of dark brown extract.

[0056] Meth...

Embodiment 2

[0058] Preparation of alisol A:

[0059] Method 1: Weigh 50 g of the extract of Example 1, put it on a silica gel column (450 g), elute with petroleum ether-ethyl acetate (3:1), 500 ml is 1 fraction, detect with HPLC, collect the target fraction, 1.0 g of solid was obtained, and the purity was greater than 50% (by weight) as determined by the area normalization method.

[0060] Method 2: Weigh 10 g of the extract from Example 1, put it on D101 macroporous adsorption resin, elute with 20% ethanol for 10 column volumes, then use 70% ethanol to elute for 5 column volumes, and collect 70% ethanol to elute The solvent was recovered under reduced pressure to obtain 2 g of yellow oil; 2 g of yellow oil was dissolved in 65% methanol, and the target compound was separated by preparative HPLC. The separation conditions are: C18 column, mobile phase is 65% methanol, flow rate is 50ml / min, detection wavelength is 208nm. 100 mg of alisol A with a purity of 95% by weight was obtained.

Embodiment 3

[0062] Preparation of Alisitol A 24-acetate:

[0063] Method 1: Weigh 50 g of the extract of Example 1, put it on a silica gel column (450 g), elute with petroleum ether-ethyl acetate (5:1), 300 ml is 1 fraction, detect with HPLC, collect the target fraction, 0.4 g of solid was obtained, and the purity was greater than 55% (by weight) as determined by the area normalization method.

[0064] Method 2: take by weighing 20 g of the extract of Example 1, put on AB-8 type macroporous adsorption resin, elute 10 column volumes with 30% ethanol, then use 80% ethanol to elute 5 column volumes, collect 80% ethanol The eluate was recovered under reduced pressure to obtain 1.5 g of yellow oil; 1.5 g of yellow oil was dissolved in 68% methanol, and the target compound was separated by preparative HPLC. The separation conditions are: C18 column, mobile phase is 68% methanol, flow rate is 50ml / min, detection wavelength is 208nm. This gave 60 mg of alisol A 24-acetate with a purity of 95% b...

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Abstract

The invention provides a composition consisting of alisol A and alisol A24-acetic ester and application thereof, wherein weight ratio of the composition consisting of the alisol A and the alisol A24-acetic ester is between 1: 0.02 and 1: 50. The invention provides a medicine for treating hyperlipidemia diseases, atherosclerosis diseases or fatty liver diseases by modern medical theory so as to satisfy needs for clinical application. The invention has the advantages that people taking the composition consisting of the alisol A and the alisol A24-acetic ester for a long time do not have abnormal rise of liver transaminase, intrahepatic fat deposit, or increase of liver volume and / or weight. The creativity of the invention lies in that through a systematically study of the specific mixture ratio of the alisol A and the alisol A24-acetic ester, the curative effect of decreasing blood-fat, resisting atherosclerosis and treating fatty liver can be improved, and toxic and side effect can be reduced.

Description

technical field [0001] The invention relates to a composition of Alisma alisma and its application in medicine. Background technique [0002] With the improvement of people's living standards, the incidence of hyperlipidemia, atherosclerosis and fatty liver is also increasing. In 2004, the "Nutrition and Health Status of Chinese Residents" issued by the Ministry of Health and the National Bureau of Statistics clearly pointed out that dyslipidemia in my country deserves attention. The prevalence of dyslipidemia in adults is 18.6%. It is estimated that there are 160 million people with dyslipidemia nationwide. There is no feeling in the early stage of dyslipidemia, and it is not easy to be detected, and the awareness rate is only 25%. [0003] The mechanism of dyslipidemia causing atherosclerosis is a hotspot of current research. Existing research results have confirmed that the most important hazard of hypercholesterolemia is that it is easy to cause coronary heart disease ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P3/06A61P9/10A61P1/16
Inventor 侯惠民程志红于垂亮吴闻哲
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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