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Composition containing alisol A and application of composition containing alisol A on medicine

A technology of alisol and its composition, which is applied in the field of compositions containing alisol A, can solve the problems that the quality stability is not good enough, and the aortic inner wall thickness and inflammatory indicators of rabbits with atherosclerosis cannot be significantly improved, etc. , to achieve the effects of long-term use, increased stability, and less toxic and side effects

Active Publication Date: 2013-04-24
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, the quality stability of the technology provided by the CN 101411711A patent is not good enough, especially it cannot significantly improve the thickness of the inner wall of the atherosclerotic rabbit aorta and the inflammatory indicators

Method used

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  • Composition containing alisol A and application of composition containing alisol A on medicine
  • Composition containing alisol A and application of composition containing alisol A on medicine
  • Composition containing alisol A and application of composition containing alisol A on medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Effects of different compositions on the stability of alisol A-23-acetate

[0028] Stability of the compound alisol A-23-acetate when alisol A and alisol A-24-acetate co-exist in solution.

[0029] Take the following samples, dissolve them in 1000ml of 50% ethanol solution, ultrasonically dissolve, measure the concentration of alisitol A-23-acetate in the solution by HPLC, heat in a water bath at 60°C, and measure the concentration of alisol A-23-acetate in the solution at 1h, 2h and 5h respectively. Concentrations of alisol A-23-acetate. Each sample was run in 3 parallels.

[0030] No. 1 Alisitol A-23-Acetate 100mg

[0031] No.2 Alisitol A+Alisol A-23-Acetate+Alisol A-24-Acetate, 1:0.05:0.5, 3100mg

[0032] No.3 Alisitol A+Alisol A-23-Acetate+Alisol A-24-Acetate, 1:0.3:0.05, 450mg

[0033] No.4 Alisitol A+Alisol A-23-Acetate+Alisol A-24-Acetate, 1:0.1:0.2, 1300mg

[0034] No. 5 alisol A + alisol A-23-acetate + alisol A-24-acetate, 1:0.05:0.05, 2200mg

[0035] No....

Embodiment 2

[0044] Comparison of lipid-lowering effects of different compositions on hyperlipidemic rats

[0045] Get the SD male rats of body weight 190-210g, 222, get 10 at random and give conventional feed as blank control group, all the other 210 give high-fat feed (cholesterol 1%, lard 20%, bile salt 0.2%, conventional feed 78.8%), the serum total cholesterol (TC), serum triglyceride (TG) and low-density lipoprotein (LDL-C) of each rat fed with high-fat diet were measured after 2 weeks. According to the elevated values ​​of TC, TG and LDL-C, the top 120 rats with elevated TC, TG and LDL-C were selected and randomly divided into 12 groups, with 10 rats in each group, respectively:

[0046] Model control group (purified water),

[0047] Simvastatin group (Harbin Pharmaceutical Group Sanjing Pharmaceutical Co., Ltd., batch number: 0608206, 10mg / tablet, 2mg / kg)

[0048] Fenofibrate group (Shanghai Hengshan Pharmaceutical Co., Ltd., batch number: 071001, 100mg / tablet, 80mg / kg)

[0049]...

Embodiment 3

[0087] Effects of Different Compositions of A on Lowering Blood Lipid and Anti-Atherosclerosis in Rabbits with Atherosclerosis

[0088] 3.1 Dose and grouping

[0089] Animal species: Japanese big-eared white rabbit.

[0090] Animal level: normal level.

[0091] Sex and number of animals: 180, male.

[0092] Animal age: 5-6 months old.

[0093] Animal weight: 2-3kg.

[0094] Animals are grouped into:

[0095] Blank control group (purified water)

[0096] Model control group (purified water),

[0097] Simvastatin group (1.5mg / kg)

[0098] Fenofibrate group (60mg / kg)

[0099] Group M (Alisol A, 60mg / kg)

[0100] Group N (Alisol A+Alisol A-23-acetate, 1:1, 60mg / kg)

[0101] Group O (Alisol A+Alisol A-24-acetate, 1:1, 60mg / kg)

[0102] Group P (Alisol A+Alisol A-23-acetate+Alisol A-24-acetate, 1:0.05:0.5, 60mg / kg)

[0103]Group Q (Alisol A+Alisol A-23-acetate+Alisol A-24-acetate, 1:0.3:0.05, 60mg / kg)

[0104] Group R (Alisol A+Alisol A-23-acetate+Alisol A-24-acetate, 1...

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Abstract

The invention discloses a composition containing alisol A and an application of the composition containing alisol A on medicine, and the composition containing alisol A comprises the following ingredients by weight, alisol A: alisol A-23-acetate: alisol A-24-acetate is 1: 0.05-0.3: 0.05-0.5. The composition has the advantages of stable quality and high security, compared with single administration of alisol A or alisol A-23-acetate or alisol A-24-acetate, the composition containing alisol A with long-time administration has better hypolipemic effect by using same dosage with the alisol A or alisol A-23-acetate or alisol A-24-acetate, and in-vitro hepatotoxicity test results display that compared with single administration of alisol A or alisol A-23-acetate or alisol A-24-acetate with same dosage, the composition presents weak performance on cytotoxicity of hepatocyte. The alisol A-23-acetate combines with alisol A or alisol A-24-acetate to obtain the composition, the stability of alisol A-23-acetate is obviously increased, and the druggability is enhanced.

Description

technical field [0001] The present invention relates to a high-efficiency blood lipid-lowering composition, in particular to a composition containing alisol A and its preparation for treating hyperlipidemia, atherosclerosis caused by hyperlipidemia, and fatty liver caused by hyperlipidemia. application in medicine. technical background [0002] At present, the blood lipid-lowering drugs mainly include HMG-CoA reductase inhibitors, fibrates, nicotinic acid, and unsaturated fatty acids, among which statins and fibrates are the first-line blood lipid-lowering drugs, but because these drugs are metabolized by the liver During the process, it can cause liver toxicity such as cholestasis and elevated transaminases, leading some patients to be forced to stop taking the drug. [0003] Therefore, it has been a long-term goal of pharmaceutical workers to research and develop a new type of blood lipid-lowering drug that has little liver toxicity and is suitable for long-term use. [...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/06A61P9/10A61P1/16
Inventor 侯惠民程志红
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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