Pharmaceutical compositions of berberine with epa and dha, and methods thereof

Abstract

The invention provides various novel compositions of berberine in combination with pharmacologically active EPA and DHA, and related methods of their use in treating various diseases or disorders. The pharmaceutical compositions of the invention are useful in treating and / or preventing various diseases or disorders, including metabolic diseases or disorders such as dyslipidemia, hyperglycemia, hypertriglyceridemia, hyperlipidemia, diabetic dyslipidemia, diabetic hyperlipidemia, dyslipidemia in statin-intolerance patients, diabetes, diabetic complications, hypercholesterolemia, or obesity. Additionally, the pharmaceutical compositions of the invention are useful in treating and / or preventing atherosclerosis, heart diseases, neurodegenerative diseases, inflammation, cancers, as well as various liver diseases or disorders, such as fatty liver, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, cholestatic liver diseases or graft-versus-host disease of the liver. Furthermore, the pharmaceutical compositions of the invention are useful in improving liver functions in chronic viral associated liver diseases and alcohol-related liver diseases.

Description

PRIORITY CLAIMS AND RELATED PATENT APPLICATIONS[0001]This application claims the benefit of priority, under 35 U.S.C. §120, from the U.S. designation of International Application No. PCT / CN2016 / 105294, filed on Nov. 10, 2016, which claims benefit of priority from U.S. Provisional Application Ser. No. 62 / 254,739, filed on Nov. 13, 2015, the entire content of each of PCT / CN2016 / 105294 and Ser. No. 62 / 254,739 is incorporated herein by reference in its entirety for all purposes.TECHNICAL FIELD OF THE INVENTION[0002]The invention generally relates to novel compositions and methods of preparation and therapeutic use thereof. In particular, the invention relates to novel pharmaceutical compositions of berberine in combination with omega-3 fatty acids, e.g., eicosapentaenoic acid (EPA) and / or docosahexaenoic acid (DHA), or esters thereof, and methods of their use. The pharmaceutical compositions of the invention are useful in treating and / or preventing various diseases or disorders, includi...

AI Technical Summary

Benefits of technology

The invention is about a new pharmaceutical composition that combines berberine with omega-3 fatty acids, such as EPA and DHA, to treat various diseases and disorders. The composition can be used to treat metabolic diseases, heart diseases, neurodegenerative diseases, inflammation, cancers, and liver diseases. The composition can be in the form of a pill or liquid form and can be used in combination with other medications. The technical effect of this invention is to provide a new and effective treatment for various diseases and disorders by combining berberine with omega-3 fatty acids.

Problems solved by technology

Hyperglycemia is a potentially serious condition if not treated in time since ketoacidosis, a life-threatening condition, could occur and needs immediate treatment.

Chronic hyperglycemia causes injuries to the heart and is strongly associated with heart attacks and death in subjects with no coronary heart disease or history of heart failure.

Many therapeutic treatments are available for the management of type 2 diabetes, but they are often accompanied by various side effects.

Despite persistent efforts and meaningful progress over the past decades in the understanding and management of diabetes, people with diabetes continue to have an increased risk of, and many do suffer from, a number of serious complications inflicting the heart and blood vessels, eyes, kidneys, and nerves due to high blood glucose, high cholesterol, and high blood pressure.

Diabetic nephropathy caused by damages to small blood vessels in the kidney leads to decreased kidney function or kidney failure altogether.

Despite the development of a number of anti-diabetic agents, there are significant unmet needs for therapeutics that can be used effectively for the treatment and management of diabetic complications.

Metabolic syndrome has been demonstrated to increase the risk of developing cardiovascular diseases, particularly heart failure, and diabetes.

Although statins are generally well tolerated, statin intolerance occurs in some patients and requires careful consideration.

In addition, patients are sometimes concerned about the potential risk of statins causing diabetes mellitus, cancer, and memory loss and often question whether they should continue with their medication.

For statin-intolerant patients, non-statin LDL-C-lowering drugs can be used; however, till the PCSK9 inhibitors are approved, none of the approved drugs has been nearly as effective as statins.

Neurons normally don't reproduce or replace themselves when they become damaged or die.

Neurodegenerative diseases are incurable and debilitating conditions that result in progressive degeneration and / or death of nerve cells.

While many treatment options for cancer exist, including surgery, chemotherapy, radiation therapy, hormonal therapy, targeted therapy and palliative care, cancer remains a top health threat and is responsible for about 15% of all human deaths.

Nevertheless, NASH can be severe and can lead to cirrhosis, when the liver is permanently damaged and scarred and no longer work properly.

Currently, there are no drugs approved for the treatment of NASH, which occurs in about a quarter of patients with NAFLD.

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