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Combination product containing limonoid and alpha-glucosidase inhibitor

A technology of glycosidase inhibitors and limonoids, which is applied in the field of medicine and can solve problems such as elevated liver enzymes, aggravated diseases, and injuries

Active Publication Date: 2019-10-15
NATURAL MEDICINE INST OF ZHEJIANG YANGSHENGTANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the decomposition and absorption of carbohydrates in the small intestine, the bacteria in the colon act on the unabsorbed carbohydrates to cause flatulence, such as abdominal distension, diarrhea and abdominal pain; 2. Systemic adverse reactions
It has been reported that the drug can cause hepatocellular liver injury, accompanied by jaundice and elevated transaminases, which can be relieved by stopping the drug; 3. Especially when used in large doses, asymptomatic liver enzymes will occur. For people with normal liver function, After stopping the drug, the liver enzyme value will return to normal, but for patients with liver insufficiency, it will aggravate the condition and cause damage

Method used

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  • Combination product containing limonoid and alpha-glucosidase inhibitor
  • Combination product containing limonoid and alpha-glucosidase inhibitor
  • Combination product containing limonoid and alpha-glucosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Effects of limonoids, acarbose or their combination on blood glucose in mouse islet β-cell injury model

[0036] In this example, ICR mice were modeled with streptozotocin (STZ) to obtain a mouse islet β-cell injury model (Li Nan et al., The protective effect of pine pollen on kidney damage in mice with diabetic nephropathy, Science and Technology Herald, 2014, 32 (4 / 5): 95-99), completed the animal hypoglycemic efficacy evaluation experiment (this model can simulate type I and type II diabetes islet β cell damage state). Limonoid compounds choose limonin, isocitrinic acid, limonin glycoside, and isocitrolactone glycoside, and set up separate acarbose administration group, limonin administration group, and isocitrolactone administration group. Acid administration group, limonin glycoside administration group, isocitrolactone glycoside administration group and combined administration group compounded with acarbose.

[0037] Experimental feeding conditions: ICR mice (20±...

Embodiment 2

[0047] Effects of limonoids, acarbose, or their combination on blood glucose and leptin in a mouse model of type II diabetes

[0048] In this embodiment, db / db mice (strain name BKS.Cg-Dock7 m+ / + Lepr db / Nju) completed the animal hypoglycemic efficacy evaluation experiment (blood sugar level and leptin). For the limonoid compounds, choose phellodendron, isofortone acid, and phellodendron glucoside, and set up separate acarbose administration groups, phellodendron administration groups, isofortone acid administration groups, and phellodendron glucoside administration groups. And the combined administration group with acarbose respectively.

[0049] Experimental feeding conditions: as type II diabetes model mice, 6-week-old SPF-grade db / db mice were purchased from the Nanjing Institute of Model Organisms, and the experimental feeding was carried out after 7 days of preparatory feeding. It should be noted that the feeding conditions of the mice were temperature of 23±1°C, hum...

Embodiment 3

[0060] Effects of limonoids, acarbose or their combination on blood glucose in mouse islet β-cell injury model

[0061] In this example, ICR mice were modeled with streptozotocin (STZ) to obtain a mouse islet β-cell injury model (Li Nan et al., The protective effect of pine pollen on kidney damage in mice with diabetic nephropathy, Science and Technology Herald, 2014, 32 (4 / 5): 95-99), completed the animal hypoglycemic efficacy evaluation experiment (this model can simulate type I and type II diabetes islet β cell damage state). For limonoid compounds, choose Yichang Hesin, Yichang Genxin, and Yichang Hesin Glycoside, and set up a separate acarbose administration group, Yichang Hesin administration group, Yichang Genxin administration group, and Yichang Hesin Vegetarian glycoside administration group and combined administration group compounded with acarbose.

[0062] Experimental feeding conditions: ICR mice (20±2g), 6 weeks old, were purchased from Zhejiang Academy of Medic...

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Abstract

The invention relates to a combination product containing limonoid (and a derivative, ester, a stereoisomer, salt or prodrug acceptable in pharmacy of the limonoid) and an alpha-glucosidase inhibitor(such as acarbose, acarbose derivative, voglibose, miglitol and the like). The invention further relates to application of the combination product containing the limonoid and the alpha-glucosidase inhibitor in treating and / or preventing diabetes-related diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a limonoid compound (and pharmaceutically acceptable derivatives, esters, stereoisomers, salts or prodrugs thereof) and an alpha-glucosidase inhibitor (or its Combination products of pharmaceutically acceptable derivatives). The present invention also relates to the use of the combined product in treating and / or preventing diabetes and diseases related to metabolic syndrome. Background technique [0002] According to IDF statistics, there were about 425 million people with diabetes worldwide in 2017, and 1 in every 11 people has diabetes. The number of diabetic patients in China is about 110 million, ranking first in the world. It is predicted that by 2040, there will be 642 million people with diabetes worldwide, and 151 million people with diabetes in China. Diabetes requires lifelong monitoring and treatment. If it is not well controlled, it will lead to secondary cardiova...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61K31/7036A61P3/10A61P3/00
CPCA61K31/585A61K31/7036A61P3/10A61P3/00A61K2300/00A61K31/702A61K31/366A61K31/7048A61K45/06A61K9/2054A61K9/2095A61K31/133A61K31/445
Inventor 李栋吴妍胡柳薛莲
Owner NATURAL MEDICINE INST OF ZHEJIANG YANGSHENGTANG
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