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Obeticholic acid and metformin composition and application thereof

A technology of metformin hydrochloride and obeticholic acid, applied in the field of medicine, can solve problems such as side effects of high and low density lipoprotein cholesterol

Inactive Publication Date: 2017-07-25
CHENGDU BESTCHIRALBIO LIMITED LIABILITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The recently published literature (Lancet.2015Mar 14; 385(9972):956-965) pointed out that in the clinical study of obeticholic acid treatment of non-alcoholic fatty liver disease, high low-density lipoprotein cholesterol (LDL cholesterol) was observed in the test samples. -C) side effects, which is a huge challenge for obeticholic acid to be marketed as a potential non-alcoholic fatty liver disease

Method used

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  • Obeticholic acid and metformin composition and application thereof
  • Obeticholic acid and metformin composition and application thereof
  • Obeticholic acid and metformin composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Therapeutic research experiment of abnormal blood index in golden hamster induced by high-fat diet

[0046] Model establishment: Golden hamsters were fed with custom-made high-fat diets, and normal rats were fed with normal rat growth feeds. Animal serum was collected after 4 weeks to detect changes in indicators. Compared with the golden hamsters in the normal group, the levels of LDL-C and TC in the serum of the golden hamsters induced by high-fat diet were significantly increased with statistical differences, which proved that the hyperlipidemia model was successfully established.

[0047] Test groups and dose design: normal control group, high-fat model control group, simvastatin group (8mg / kg), metformin (MET) group (100mg / kg), obeticholic acid (OCA) group (10mg / kg ), metformin+obeticholic acid (MET+OCA) low-dose group ((50mg+5mg) / kg), metformin+obeticholic acid (MET+OCA) high-dose group ((100mg+10mg) / kg). Number of animals: 10 per group. Administration...

Embodiment 2

[0057] Example 2 Study on Drug Curative Effect of Fatty Liver in Golden Hamsters Induced by High Fat Diet

[0058] Description of research animals: The research animals used in this experiment are the animals used in the above-mentioned "in vivo lipid-lowering experiment of the golden hamster model". Parts were frozen at -80°C, fixed for more than 48 hours, and examined for pathological section staining (H&E staining, Oil Red-O staining). Focus on the structural integrity of the liver, inflammatory cell infiltration, and the severity of fatty liver, and score them (grading criteria: grade 0: normal; grade 1: 80%). The results are shown in the table below.

[0059]

[0060] The results showed that in the high-fat model group, compared with the normal group, the volume of adipocytes in the liver increased significantly, and bullous steatosis appeared. A large number of inflammatory cells were infiltrated, and the above phenomena indicated that the modeling of non-alcoholic ...

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Abstract

The present invention provides a pharmaceutical composition comprising obeticholic acid or a pharmaceutically acceptable salt thereof and metformin or a pharmaceutically acceptable salt thereof. In addition, the present invention also provides applications related to the pharmaceutical composition and the like. The compound combination can effectively eliminate the side effect of increasing LDL-C caused by obeticholic acid, significantly improve the blood biochemical indexes of high-fat and high-sugar animals, significantly improve fatty liver symptoms, and cure non-alcoholic fatty liver disease.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, the invention relates to a compound composition, a preparation, a preparation method and an application etc. comprising obeticholic acid and metformin. Background technique [0002] Obeticholic acid (OCA for short, such as structural formula I), also known as 6-ethylchenodeoxycholic acid (6-ECDCA), is a natural ligand of the farnesoid derivative X receptor (FXR). Obeticholic acid is a farnesoid X receptor agonist, which indirectly inhibits the gene expression of cytochrome 7A1 (CYP7A1) by activating farnesoid X receptor. Obeticholic acid was successfully developed by Intercept Pharmaceutical Company of the United States. It is the first drug developed for the treatment of cholestatic liver disease in two decades. The study was performed in patients who did not respond adequately to or could not tolerate the older standard of care, ursodeoxycholic acid. Obeticholic acid (OCA) in...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61K31/155A61P3/10A61P3/06A61P1/16A61P3/04
CPCA61K31/575A61K31/155
Inventor 李德群
Owner CHENGDU BESTCHIRALBIO LIMITED LIABILITY
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