HMG-CoA Inhibitor Citrulline Combination for Fat Reduction

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Solution Overview

Problem

Current treatments for overweight and obesity often result in significant muscle loss, and existing cosmetic methods fail to effectively target fat reduction without adverse health consequences, particularly in non-pathological cases of excess fat mass like cellulite.

Innovation Solution

A combination product comprising an HMG-CoA reductase inhibitor, such as atorvastatin or red yeast rice extract, and citrulline, administered without arginine, which is designed to reduce fat mass while preserving lean mass, used for both therapeutic and cosmetic purposes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Weight of moving object

If current treatments for overweight and obesity are used, then weight loss is achieved, but significant muscle loss occurs

Engineering Contradiction:
Improveweight lossVSAvoidmuscle mass
Core Design Contradiction:
Weight of moving objectVSStrength

Solution Approach 1:

The patent changes the biochemical parameters of fat metabolism by combining HMG-CoA reductase inhibition with citrulline administration. This parameter change allows selective fat reduction while preserving muscle mass, as the combination affects lipid synthesis pathways without the catabolic effects that cause muscle loss in conventional weight loss treatments.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses a composite approach by combining two substances with complementary functions: HMG-CoA reductase inhibitor (which blocks fat synthesis) and citrulline (which preserves muscle mass and improves metabolism). This composite combination achieves weight loss without muscle loss, resolving the contradiction between fat reduction and muscle preservation.

Inventive Principle:
Principle #40Composite materials

2Shape

If existing cosmetic methods are used to target fat reduction, then localized fat reduction is attempted, but adverse health consequences occur

Engineering Contradiction:
Improvefat reductionVSAvoidadverse health consequences
Core Design Contradiction:
ShapeVSObject-affected harmful factors

Solution Approach 1:

The patent introduces citrulline as an intermediary substance that modulates the effects of HMG-CoA reductase inhibition. Citrulline acts as a mediator that preserves lean mass and improves glucose tolerance, thereby reducing adverse health consequences while still achieving effective fat reduction for cosmetic purposes.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the safety parameters of fat reduction treatments by using a combination that preserves muscle mass and improves metabolic health. This parameter change allows cosmetic fat reduction without the adverse health effects associated with conventional methods, making the treatment both effective and safe.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If HMG-CoA reductase inhibitor is used alone, then fat mass reduction is achieved, but lean mass is lost

Engineering Contradiction:
Improvefat massVSAvoidlean mass
Core Design Contradiction:
Quantity of substanceVSLoss of substance

Solution Approach 1:

The patent merges HMG-CoA reductase inhibition with citrulline administration to achieve a synergistic effect. This combination allows fat mass reduction through HMG-CoA reductase inhibition while citrulline simultaneously preserves lean mass, resolving the contradiction between fat reduction and lean mass preservation.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent converts the potential harm of HMG-CoA reductase inhibition (which can cause lean mass loss) into a benefit by combining it with citrulline. Citrulline counteracts the harmful effect of lean mass loss while enhancing the beneficial fat reduction effect, turning a harmful side effect into a beneficial outcome.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The combination product demonstrates a synergistic effect on weight loss and fat reduction without muscle loss, improving glucose tolerance and effectively addressing excess fat mass in both therapeutic and cosmetic applications.

Implementation Method 1

an inhibitor of the HMG-CoA-reductase enzyme

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

citrulline or a salt thereof... citrulline being administered at a daily dose of 1 to 15 g/day

Methodology Applied
Scientific EffectMetabolic conversion:

Data Source

PatentEP2819635B1Combination product for treating excess weight and/or for improving the figure
Publication Date: 2018.07.11 INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE
  • EP2819635B1 patent drawingFigure 1~2
  • EP2819635B1 patent drawingFigure 3A~3B
  • EP2819635B1 patent drawingFigure 4A~4C

AI summary

The invention relates to a combination product including, as active substances, at least one inhibitor of the HMG-CoA reductase enzyme and citrulline or a compound that is the bioequivalent thereof, for treating excess weight or obesity and/or the accumulation of body fat. The invention also relates to a cosmetic treatment method for improving or slimming the figure and/or stimulating the loss of excess weight and/or cellulite and/or reducing the accumulation thereof, said method including administering a combination product that includes, as active substances, at least one inhibitor of the HMG-CoA reductase enzyme or a physiologically acceptable salt thereof, and citrulline or a compound that is the bioequivalent thereof, or one of the analogs thereof, and repeating said administration until the desired cosmetic effect has been achieved. Finally, the invention relates to the use of a combination product as defined above for improving or slimming the figure and/or stimulating the loss of excess weight and/or cellulite and/or reducing the accumulation thereof.