Synergistic Berberine and Ku Ding Cha Extract for Cardiovascular Health

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Solution Overview

Problem

Current treatments for cardiovascular disease, particularly those involving statins, have limitations such as contraindications in patients with hepatic issues, potential adverse effects, and the need for high doses of berberine, which can be toxic, highlighting the need for alternative cholesterol-lowering agents that are safer and more effective.

Innovation Solution

A synergistic combination of huanglian and Ku Ding Cha extracts, which include berberine and other active compounds like ursolic acid, betulin, and chlorogenic acid, work together to lower apolipoprotein-B secretion, offering a safer and more effective cholesterol-lowering mechanism than either component alone.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of berberine are used to achieve cholesterol-lowering effects, then the therapeutic efficacy is improved, but the toxicity and adverse effects increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines berberine with Ku Ding Cha extract to create a synergistic formulation. This merging allows the use of lower doses of berberine while achieving the same or better therapeutic effect, thereby reducing toxicity. The combination produces a greater than additive effect in lowering cholesterol and apo-B secretion.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite pharmaceutical formulation consisting of multiple active components (berberine and Ku Ding Cha extract). This composite approach leverages the complementary mechanisms of action between the components to enhance efficacy while reducing the dosage and associated toxicity of individual ingredients, particularly berberine.

Inventive Principle:
Principle #40Composite materials

2Reliability

If statins are used to lower cholesterol levels, then the lipid-lowering effect is improved, but the risk of adverse effects on liver, muscle, and kidney increases

Engineering Contradiction:
Improvelipid-lowering effectVSAvoidadverse effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent positions the herbal combination as an alternative to statins, using natural, readily available plant-based compounds. The formulation uses traditional medicinal plants with established safety profiles, replacing synthetic drugs that carry risks of hepatotoxicity, myopathy, and nephrotoxicity.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The Ku Ding Cha extract acts as an intermediary that enhances the cholesterol-lowering effect of berberine through multiple mechanisms including ACAT inhibition and apolipoprotein secretion reduction. This intermediary component allows for reduced berberine dosing while maintaining or improving therapeutic efficacy, thereby reducing adverse effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If berberine is used at toxic doses, then the cholesterol-lowering effect is maximized, but the safety and tolerability deteriorate

Engineering Contradiction:
Improvecholesterol-lowering effectVSAvoidsafety
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent merges berberine with Ku Ding Cha extract in a synergistic formulation that produces enhanced cholesterol-lowering effects at lower doses. This combination allows the system to achieve maximum productivity (cholesterol reduction) without reaching toxic thresholds, as the two components work together to amplify the therapeutic effect.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention changes the dosing parameters by using a combination formulation that requires lower berberine doses compared to monotherapy. This parameter change in dosage regimens, enabled by the synergistic interaction with Ku Ding Cha components, maintains therapeutic efficacy while improving safety and tolerability.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS8642094B2Synergistic pharmaceutical composition, method of making same and use of same
Publication Date: 2014.02.04 BAUSCH LOMB CORP
  • US8642094B2 patent drawing
  • US8642094B2 patent drawing
  • US8642094B2 patent drawing

AI summary

A medicinal combination of herbs, herbal extracts, and their chemical constituents that is synergistically effective for promoting human and veterinary health. The combination is a blood lipid level lowering synergistic composition comprising Ku ding cha, berberine or a berberine-containing plant extract, and other optional active ingredients. Methods of extraction and combination in synergistic amounts are also disclosed. The compositions according to the present invention may be used to treat or reduce the chance of contracting or the progression of a number of diseases or conditions in a subject, particularly cardiovascular diseases.