Pharmaceutical composition having alpha-glucosidase inhibition activity, and applications thereof

A technology of glycosidase inhibition and composition, which is applied in the field of medicine and biology, can solve the problems of high dosage of α-glucosidase inhibitors and large side effects, and achieve good hypoglycemic effect, lower postprandial blood sugar, and improve drug efficacy

Active Publication Date: 2015-10-21
上海皋鱼医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the problems of high dosage of α-glucosidase inhibitors in the prior art and relatively large side effects, the present invention provides a pharmaceutical composition comprising flavonoids and α-glucosidase inhibitors, which can make the combined drug There is a synergistic effect between them to improve the efficacy of the drug, and it can reduce the side effects caused by the large dose of a single α-glucosidase inhibitor, reduce postprandial blood sugar, and prevent or treat diabetes and obesity

Method used

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  • Pharmaceutical composition having alpha-glucosidase inhibition activity, and applications thereof
  • Pharmaceutical composition having alpha-glucosidase inhibition activity, and applications thereof
  • Pharmaceutical composition having alpha-glucosidase inhibition activity, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is maltose)

[0053] SD rats (200-220g) were fasted for 16h, sacrificed under ether anesthesia, and the small intestine was taken out, opened, washed with pre-cooled PBS (0.1M, pH 7.0) buffer solution, and then added at a ratio of 1:10 (W / V) PBS buffer. The small intestine was cut into pieces and homogenized, centrifuged at 10,000 r / min at 4°C for 15 minutes, and the supernatant was taken as the α-glucosidase mother solution for the test.

[0054] The total volume of the enzyme reaction system is 500 μL, including 100 μL each of enzyme solution, baicalin, acarbose, starch solution, and buffer, wherein baicalin is dissolved in 50% DMSO. First, mix the enzyme with the two inhibitors, incubate at 37°C for 30min, and add 100μL of maltose solution to start the reaction. Incubate at 37°C for 30 minutes. The sample was placed in boiling water for 10 minutes to terminate the reaction. ...

Embodiment 2

[0060] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is starch)

[0061] The preparation of α-glucosidase and the assay method of inhibition rate are similar to those in Example 1, except that the substrate is replaced by starch solution. When 37.03, 74.07, 111.11, 148.15μM baicalinin was combined with 0.31, 0.62, 0.93, 1.24μM acarbose respectively, the inhibition rate of combined use at each dose point was significantly higher than that of single use, CI value are 0.45, 0.45, 0.49 and 0.65 ( figure 1 ), the results showed that the combination of baicalin and acarbose had a strong synergistic inhibitory effect on the hydrolysis of starch by α-glucosidase.

Embodiment 3

[0063] Synergistic inhibition of baicalin and acarbose on rat intestinal α-glucosidase (substrate is sucrose)

[0064]The preparation of α-glucosidase and the assay method of inhibition rate are similar to those in Example 1, except that the substrate is changed to sucrose. Combining 74.07, 148.15, 370.37, 740.74 μM baicalin with 0.062, 0.12, 0.31, 0.62 μM acarbose, respectively, the inhibition rate at each dose point was significantly improved, and the CIs were all less than 0.9. And with the increase of the dose of baicalinin, the CI value decreased gradually, and the synergistic effect was enhanced ( figure 2 ). The results showed that the combination of baicalin and acarbose had a strong synergistic inhibitory effect on the hydrolysis of sucrose by α-glucosidase.

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Abstract

The invention relates to a pharmaceutical composition having alpha-glucosidase inhibition activity, wherein the pharmaceutical composition comprises a flavone compound and an alpha-glucosidase inhibitor, the flavone compound is at least one selected from a monomer such as baicalein, quercetin, luteolin, baicalein-7-O-glucoside and catechin, an organic salt of the monomer, and an inorganic salt of the monomer, and the alpha-glucosidase inhibitor is at least one selected from a monomer such as acarbose, voglibose and miglitol, an organic salt of the monomer, and an inorganic salt of the monomer. According to the present invention, the pharmaceutical composition can effectively reduce postprandial blood glucose, can inhibit the activity of alpha-glucosidase adopting starch, maltose and sucrose as substrates, and less uses the alpha-glucosidase inhibitor, such that the efficacy can be improved, the side effect of the alpha-glucosidase inhibitor can be effectively reduced, and hypoglycemia and other problems easily caused by drug combination are effectively solved.

Description

technical field [0001] The invention relates to a pharmaceutical composition with alpha-glucosidase inhibitory activity, which belongs to the field of medicine and biology. Background technique [0002] Diabetes mellitus is an endocrine and metabolic disorder, a chronic disease characterized by hyperglycemia caused by insulin secretion and utilization disorders. According to the statistics of the International Diabetes Federation (IDF), as of 2013, the number of diabetic patients in China was 98.4 million, ranking first in the world. The number of diabetic patients in the world is 382 million, and 5.1 million people die from diabetes-related diseases every year, accounting for 8.39% of the total deaths. According to the forecast of the World Health Organization (WHO), the global medical expenditure on diabetes will reach 53 billion US dollars in 2016, ranking second only to tumors. Therefore, the research and development of diabetes drugs not only has extremely high commer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P3/10A61P3/04
CPCA61K31/133A61K31/352A61K31/353A61K31/445A61K31/7036A61K31/7048A61K45/06A61K2300/00
Inventor 董悦生张博崴孙文龙桑元斌于晓霞修志龙
Owner 上海皋鱼医药科技有限公司
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