Ferulic acid Jiangtang compound salt as well as preparation method and application thereof

A technology for lowering blood sugar of ferulic acid and biguanides, which is applied in the field of medicine, can solve problems such as no reports of double salts of ferulic acid-biguanides hypoglycemic compounds, and achieve the goal of preventing and treating diabetic complications and inhibiting further damage Effect

Active Publication Date: 2011-08-24
CHENGDU ZIHAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no report on the double salt of ferulic acid-biguanide hypoglycemic compound

Method used

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  • Ferulic acid Jiangtang compound salt as well as preparation method and application thereof
  • Ferulic acid Jiangtang compound salt as well as preparation method and application thereof
  • Ferulic acid Jiangtang compound salt as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Preparation of metformin ferulic acid double salt

[0027] Dissolve 4.1 g of ferulic acid and 2.6 g of metformin in acetone respectively, mix and stir until a large amount of precipitates are precipitated, let stand until no precipitates are formed, filter, collect the precipitates, and recrystallize with water to obtain 4.9 g of white short needle-like crystals. 1HNMR (D20, 400MHz): δppm 7.26 (1H, d, J = 15.9Hz), 7.17 (1H, s), 7.05 (1H, m), 6.78 (1H, m), 6.28 (1H, dd, J = 15.7 , 4.26Hz), 3.82 (3H, s), 2.97 (6H, s). m.p.114-116℃, molecular formula: C 10 h 10 o 4 ·C 4 h 11 N 3 .

Embodiment 2

[0028] Example 2 Preparation of phenformin ferulic acid double salt

[0029] Dissolve 4.1 g of ferulic acid and 4.3 g of phenformin in acetone respectively, mix and stir until a large amount of precipitates are precipitated, leave to stand until no precipitates are produced, filter, take the precipitates, and obtain milky white crystals by recrystallization. m.p.124-126℃, molecular formula: C 10 h 10 o 4 ·C 10 h 15 N 5 .

[0030] The beneficial effects of the present invention will be described below through experimental examples.

experiment example 1

[0031] Experimental Example 1 Effects of Compounds of the Present Invention on Blood Glucose and Renal Function in Alloxan-Induced Diabetic Mice

[0032] Take Kunming mice weighing 22-26 grams, inject 200 mg / kg alloxan intraperitoneally, measure blood sugar 72 hours later, select mice with blood sugar levels above 14.5 mmol / L, and divide 10 mice into each group, half male and female Be 7 groups, i.e. diabetes model group (give equal volume physiological sodium chloride solution), metformin group (150mg / kg), ferulic acid group, embodiment 1,2 gained compound group, intragastric administration (every 10g body weight gives 0.2m1), for 4 consecutive weeks. After 2 weeks of administration, the tail was cut to collect blood, and blood glucose was measured with a rapid blood glucose meter (Johnson & Johnson, USA). After another 2 weeks of administration, the eyeball was removed 3 hours after the last administration to take blood, the blood sample was centrifuged for 10 minutes (2000...

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Abstract

The invention relates to a ferulic acid biguanide compound salt as shown in a formula I. In the formula I, R is a biguanide Jiangtang compound. The invention also provides a preparation method, application and the like of the compound salt. The ferulic acid biguanide compound salt has the functions of reducing side effect and taking a synergistic effect, can be used for preventing and treating dabetes mellitus and has the functions of preventing and treating Diabetic complication-diabetic nephropathies.

Description

technical field [0001] The invention relates to a double salt formed of ferulic acid and a biguanide hypoglycemic compound, a preparation method and application thereof, and belongs to the field of medicines. technical background [0002] According to WHO data, the worldwide incidence of diabetes is 3% to 5%, and the total number is about 170 to 200 million. It is estimated that it will reach about 350 million in 2030, and about 50% of the patients have not been diagnosed and treated. China is one of the countries with the fastest growing number of diabetes patients, and the age of onset is getting younger. 80% of the patients have not been diagnosed and treated. Diabetes is associated with multiple devastating complications: microvascular complications (diabetic retinopathy, nephropathy, and neuropathy); macrovascular complications (atherosclerosis, coronary heart disease, stroke, and peripheral vascular disease). Studies have found that although lowering blood sugar alone...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C59/64C07C51/41C07C279/26C07C277/08A61K31/192A61K31/155A61P3/10A61P13/12
Inventor 李玲吴四灵刘小军
Owner CHENGDU ZIHAO PHARMA
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