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Application of oleanolic acid type saponin compound in preparation of weight-losing and lipid-lowering drugs

A technology of oleanolic acid and saponins, which is applied in the field of pharmaceuticals or health products, and can solve the problems of low safety, many adverse reactions, and limited curative effect of weight-loss drugs

Active Publication Date: 2019-04-19
CHANGSHU INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although so far, 5 drugs have been used in clinical long-term treatment of obesity, but the safety of existing weight-loss drugs is not high, the curative effect is limited, and there are many adverse reactions, which hinder their clinical application.

Method used

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  • Application of oleanolic acid type saponin compound in preparation of weight-losing and lipid-lowering drugs
  • Application of oleanolic acid type saponin compound in preparation of weight-losing and lipid-lowering drugs
  • Application of oleanolic acid type saponin compound in preparation of weight-losing and lipid-lowering drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The instrument used in the present invention is a Bruker AV 600 nuclear magnetic resonance spectrometer (TMS is an internal standard), Buchi medium pressure preparation liquid phase, Agilent preparation chromatograph SD-1 (Agilent Technologies Inc.), and the detection wavelength λ is 215nm.

[0029] D101 macroporous resin, column chromatography silica gel, thin layer chromatography silica gel, acetonitrile and methanol are all commercially available. The medicinal materials used in the experiment were procured from the medicinal materials market.

[0030] Preparation of Compound 1-5

[0031]50kg of thorny dragon bud medicinal material, crushed to a coarse powder, and then refluxed with 70% ethanol to extract 3 times, each time for 2 hours, concentrated under reduced pressure to recover the solvent, and the obtained extract was extracted with ethyl acetate and n-butanol successively to obtain n-butanol Extract 1.2kg. The n-butanol part is separated by 50L D101 column c...

Embodiment 2

[0032] The preparation of embodiment 2 test composition 6-9

[0033] Test composition 6 (60% compound 1+40% fructooligosaccharide)

[0034] Accurately weigh 3.0 g of compound 1 obtained in Example 1, mix with 2.0 g of fructooligosaccharide, grind, stir evenly, and set aside.

[0035] Test composition 7 (80% compound 1+20% fructooligosaccharides)

[0036] Accurately weigh 4.0 g of Compound 1 prepared in Example 1, mix it with 1.0 g of fructo-oligosaccharide, grind it, stir it evenly, and set it aside.

[0037] Test composition 8 (60% compound 3+40% fructooligosaccharide)

[0038] Accurately weigh 3.0 g of Compound 3 prepared in Example 1, mix with 2.0 g of fructooligosaccharide, grind, stir evenly, and set aside.

[0039] Test composition 9 (80% compound 3+20% fructooligosaccharides)

[0040] Accurately weigh 4.0 g of Compound 3 prepared in Example 1, mix it with 1.0 g of fructooligosaccharide, grind, stir evenly, and set aside.

Embodiment 3

[0041] Embodiment 3 preparation of compound tablet of the present invention

[0042] Take compound 1 or its pharmaceutically acceptable salt or ester (3g), lactose (4g), hydroxypropyl cellulose (3g), starch (2g) and mix them with a mixer, pass through a 60 mesh sieve, add micronized silica gel (1g) , magnesium stearate (0.5g) are mixed homogeneously, and the gained mixed product is compressed into tablets with a tablet machine to obtain tablets.

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Abstract

The invention provides an oleanolic acid type saponin compound prepared by arlia elata extraction, separation and purification and having a specific structure. It is found that when the compound is used separately, the compound has remarkable weight-losing and lipid-lowering effects, and the effects are superior to the effect of its aglycone analogue oleanolic acid. When the compound is used withfructo-oligosaccharide, the compound and the fructo-oligosaccharide cooperate with each other and produce a joint action in specific proportion, so that the drug composition has a remarkable weight-losing effect, the weight-losing effect of the composition is superior to the weight-losing effect of a single compound, and the drug composition has a synergistic effect. In addition, the drug composition has the remarkable weight-losing and lipid-lowering effects and has a synergistic effect, the lipid-lowering effect of the drug composition is remarkably superior to the lipid-lowering effect of asingle compound.

Description

technical field [0001] The invention relates to the application of oleanolic acid saponins in the preparation of weight-loss and lipid-lowering medicines, and belongs to the field of medicines or health care products. Background technique [0002] Obesity is a chronic metabolic disease in which excess energy is stored in the body in the form of fat and gradually accumulates to excess due to the body's energy intake exceeding energy consumption. Obesity is a leading cause of death and disease worldwide, and rates have been rising. Obesity increases the risk of metabolic diseases and cardiovascular diseases, and is one of the main causes of cardiovascular diseases. In June 2013, the American Medical Association officially recognized obesity as a disease. Although it is currently possible to reduce the size of the stomach, increase the feeling of fullness, and reduce the amount of food intake through bariatric surgery, so as to achieve the effect of weight loss. But bariatri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K31/702A61P3/04A61P3/06
CPCA61K31/702A61K31/704A61P3/04A61P3/06A61K2300/00
Inventor 张瑞雷丑永新
Owner CHANGSHU INSTITUTE OF TECHNOLOGY
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