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Combination medicine and its pharmaceutical composition for treating diabetes and its complications

A diabetes and drug technology, applied in drug combinations, urinary system diseases, active ingredients of heterocyclic compounds, etc., can solve the problems of effective population and long-term curative effect limitations, complications prevention and control effect differences, etc.

Active Publication Date: 2021-03-02
CHENGDU CHIPSCREEN PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are at least 8 categories of oral or injectable therapeutic drugs other than insulin according to the therapeutic mechanism, but the effective population and long-term efficacy of existing drug monotherapy have limitations
[0004] In addition, diabetic patients have a higher risk of complications such as cardiovascular and cerebrovascular, kidney and liver compared with other populations, and the existing therapeutic drugs have different effects on the prevention and control of these complications in addition to controlling blood sugar

Method used

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  • Combination medicine and its pharmaceutical composition for treating diabetes and its complications
  • Combination medicine and its pharmaceutical composition for treating diabetes and its complications
  • Combination medicine and its pharmaceutical composition for treating diabetes and its complications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Comparing the effect of siglitastat sodium combined with empagliflozin on body weight and blood sugar compared with single treatment

[0061] Experimental design: In diabetic mice, siglitastat sodium, empagliflozin or the combination of the two were orally administered, and the effects of single drug and drug combination on the body weight and blood sugar of the mice were investigated.

[0062] Test process: 6-week-old db / db male mice were orally administered 100 microliters of vehicle (0.1% sodium carboxymethylcellulose), 10 mg / kg siglitastat sodium, 3 mg / kg Engel Liejing or the same dose of siglitastat sodium and empaglitazine orally at the same time. Wild-type C57BLKS / Jnju mice were used as normal control mice (administered with vehicle). The dosing cycle was 14 days, and the animals were dissected on the 15th day. From the beginning of drug administration, mice were weighed every 3 days and fasting blood glucose was measured (fasting for 4-6 hours). Tes...

Embodiment 2

[0064] Example 2 Comparing the effect of siglitastat sodium combined with dapagliflozin on body weight and blood sugar compared with single treatment

[0065] Experimental design: In diabetic mice, siglitastat sodium, dapagliflozin or the combination of the two were orally administered, and the effects of the single drug and drug combination on the body weight and blood sugar of the mice were investigated.

[0066] Test process: 6-week-old db / db male mice were orally administered 100 microliters of vehicle (0.1% sodium carboxymethylcellulose), 10 mg / kg siglitastat sodium, 1.5 mg / kg Dagretal once a day according to their body weight Liejing or siglitastat sodium and dapaglitazine at the same dose orally at the same time. Wild-type C57BLKS / Jnju mice were used as normal control mice (administered with vehicle). The dosing cycle was 14 days, and the animals were dissected on the 15th day. From the beginning of drug administration, mice were weighed every 3 days and fasting blood...

Embodiment 3

[0068] Example 3 Effect of siglitastat sodium combined with empagliflozin on blood lipids

[0069] Experimental design: In diabetic mice, siglitastat sodium, empagliflozin or the combination of the two were administered orally, and the effects of single drug and drug combination on total cholesterol (TC) and triglyceride (TG) in serum of mice were investigated.

[0070] Test process: 6-week-old db / db male mice were orally administered 100 microliters of vehicle (0.1% sodium carboxymethylcellulose), 10 mg / kg siglitastat sodium, 3 mg / kg Engel Liejing or the same dose of siglitastat sodium and empaglitazine orally at the same time. Wild-type C57BLKS / Jnju mice were used as normal control mice (administered with vehicle). The dosing cycle was 14 days, and the animals were dissected on the 15th day. Whole blood was collected, the serum was collected by centrifugation, and the TC and TG of the serum were measured by a biochemical analyzer. Test results such as image 3 shown.

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Abstract

The invention belongs to the field of biotechnology, and in particular relates to combined medicine and its pharmaceutical composition for treating diabetes and its complications. The invention discloses the combination of component (i): compound represented by general formula (I) and its pharmaceutically acceptable salts, and their isomers, and component (ii): SGLT2 inhibitor for the preparation of And / or use in medicine for treating diabetes and / or diabetic complications, and a pharmaceutical composition containing component (i) and component (ii). The present invention can synergistically reduce the blood sugar of db / db diabetic mice, produce an unexpected synergistic effect, and also bring about the improvement of blood lipid indexes, especially improve the content of triglyceride in serum, and can also control body weight, Blood lipids, blood pressure, liver and kidney protection and other aspects have a comprehensive effect, thus bringing more benefits to the prevention and / or treatment of diabetes and its complications, including cardiovascular and cerebrovascular diseases, kidney diseases and liver diseases.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to combined medicine and its pharmaceutical composition for the treatment of diabetes and its complications. Background technique [0002] Diabetes is a disease caused by a variety of genetic disorders, and it currently plagues a considerable part of the world's population. It is mainly divided into two types: (1) type 1 diabetes or insulin-dependent diabetes mellitus (IDDM), in which patients secrete little or no insulin; (2) type 2 diabetes or non-insulin-dependent diabetes mellitus (NIDDM). The core problem of patients with type 2 diabetes is insulin resistance, that is, peripheral tissues such as muscle, liver and adipose tissue have obstacles to the absorption and metabolism of blood sugar stimulated by insulin, which in turn increases the burden of insulin secretion by the islets, and eventually leads to the progressive decline or even loss of islet function. . 90% of diabetic p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/403A61K31/381A61K31/7048A61K31/382A61K31/35A61K31/401A61P3/10A61P9/00A61P13/12A61P1/16
CPCA61K45/06A61K31/403A61K31/381A61K31/7048A61K31/382A61K31/35A61K31/401A61P3/10A61P9/00A61P13/12A61P1/16A61K2300/00A61K31/7042A61K31/70A61P3/06A61K31/7034A61K31/404
Inventor 黄圣健鲁先平潘德思廖国强赵一如
Owner CHENGDU CHIPSCREEN PHARM LTD
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