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Medicine capable of promoting secretion of glp-1 and restraining secretion of gip

A technology of inhibitors and medicaments, used in endocrine system diseases, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problems of needing a doctor, unable to completely inhibit secretion, etc., to promote secretion, and achieve excellent human safety. Effect

Inactive Publication Date: 2013-03-13
SANWA CORNSTARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although conventional α-GI agents can suppress GIP secretion to some extent, they cannot completely suppress secretion (acarbose: Non-Patent Document 3, voglibose: Non-Patent Document 4, Miglitol : Non-Patent Document 5)
In addition, although conventional α-GI agents can be taken orally with daily meals, a doctor's prescription is still required

Method used

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  • Medicine capable of promoting secretion of glp-1 and restraining secretion of gip
  • Medicine capable of promoting secretion of glp-1 and restraining secretion of gip
  • Medicine capable of promoting secretion of glp-1 and restraining secretion of gip

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0039] The agent of the present invention is among antagonistic inhibitors and non-antagonistic inhibitors of sucrose decomposing enzymes, and by using the non-antagonistic inhibitor, it stimulates only L cells in the lower intestinal tract without stimulating K cells in the upper intestinal tract. Stimulates and promotes the secretion of desired GLP-1 and inhibits the secretion of undesired GIP, thus being an extremely useful substance for the treatment of abnormal glucose tolerance or the prevention of diabetes.

[0040] As the non-antagonist inhibitor of the active ingredient of the medicament of the present invention, any conventionally known substance can be used, but from the viewpoint of safety, it is preferably present in nature, and from the viewpoint of food experience, generally Preference is given to plant origin for food use. In addition, when using substances that hardly exist in nature, it is preferable to use those that can be added to foods approved by public ...

Embodiment 1

[0050] [Example 1: Validation test of the effect of using L-arabinose as a non-antagonist inhibitor]

[0051] 【experiment method】

[0052] For the case where sucrose and L-arabinose were administered to rats, the case where sucrose alone (control) was administered to rats, and the case where L-arabinose alone (control) was administered to rats, GLP-1 And the secretion of GIP, check the inhibitory effect of blood sugar and insulin.

[0053] First, 12 SD male rats (4-week-old) acclimated to normal food for 1 week were used, and these were divided into 3 groups of 4 each, and 2.5 g of sucrose / body weight kg+L-arabinose was orally administered to each group. 125 mg / kg body weight (5% relative to sucrose), 2.5 g / kg body weight sucrose, or 125 mg / kg body weight L-arabinose.

[0054] Portal blood and venous blood were collected from each rat before administration, 30 minutes after administration, and 60 minutes after administration. Prepare a blood collection tube filled with DPP-...

Embodiment 2

[0058] [Example 2: Test to check the effect of varying the amount of L-arabinose used]

[0059] 【experiment method】

[0060] The amount of L-arabinose administered to the rats in Example 1 was varied, and changes in the secretion amounts of GLP-1 and GIP were investigated.

[0061] First, using 24 male SD rats (4 weeks old) acclimated to normal food for 1 week, these were divided into 6 groups of 4 each, and 2.5 g of sucrose / body weight kg+L-arabinose was orally administered to each group. 25mg / body weight kg (relative to sucrose 1%), sucrose 2.5g / body weight kg+L-arabinose 62.5mg / body weight kg (relative to sucrose 2.5%), sucrose 2.5g / body weight kg+L-arabinose 100mg / body weight kg ( Relative to sucrose 4%), sucrose 2.5g / body weight kg+L-arabinose 250mg / body weight kg (relative to sucrose 10%), sucrose 2.5g / body weight kg+L-arabinose 500mg / body weight kg (relative to sucrose 20%), Or 2.5g of sucrose / kg of body weight. The post-administration treatment was performed as in E...

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Abstract

The invention provides an incretin-associated medicine capable of restraining secretion of GIP completely and promoting secretion of GLP-1 and highly safe. The medicine capable of promoting the secretion of GLP-1 (glucagon-like peptide-1) and restraining the secretion of the GIP (glucose-dependent insulinotropic peptide) comprises non-antagonistic inhibitor of clastic enzyme of cane sugar, such as L-gum sugar, D-wood sugar and D-tagatose, as an active ingredient.

Description

【Technical field】 [0001] The present invention relates to an incretin-related drug useful for the treatment of abnormal glucose tolerance or the prevention of diabetes. 【Background technique】 [0002] The number of diabetic patients in Japan is about 7.4 million according to the national statistics (2004), including about 16.2 million people with high risk (Ministry of Health, Labor and Welfare's 2002 Diabetes Survey). Compared with the previous survey ( 1997) increased by about 20%. As a cause of death, it ranks 10th among men and 9th among women (overview of vital statistics of the Ministry of Health, Labor and Welfare in 2005). Even more amazing. [0003] Impaired glucose tolerance is attracting attention as an initial symptom in persons at high risk of diabetes. Impaired glucose tolerance is a symptom in which the blood sugar level after a meal is difficult to drop, and is usually judged by a 75g glucose load test (75gOGTT). [0004] In recent years, incretin (glucos...

Claims

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Application Information

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IPC IPC(8): A61K31/7004A61P5/50A61P3/10
CPCA23L2/52A23L29/30A61K31/7004A61K31/7016A23V2200/328A61K2300/00
Inventor 森俊雄出川洋子柴沼清
Owner SANWA CORNSTARCH
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