L-Arginine and L-Citrulline Composition for Sexual Function

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Solution Overview

Problem

Current compositions for treating sexual dysfunctions and improving sexual function often require daily dosing, can cause side effects, and are not effective for healthy individuals seeking to enhance their sexual experiences on demand, particularly for females.

Innovation Solution

A composition comprising specific ratios of L-arginine and L-citrulline, along with proanthocyanidins, administered as a unit dosage prior to sexual activity, providing a synergistic effect that enhances sexual function and experience without the need for continuous dosing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current compositions for treating sexual dysfunctions are used, then sexual function is improved, but daily dosing is required and side effects occur

Engineering Contradiction:
Improvesexual function improvementVSAvoiddosing frequency
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The composition is designed to be taken in advance (prior to sexual activity) rather than requiring continuous daily dosing. This preliminary action allows the active ingredients (L-arginine and L-citrulline) to be absorbed and converted to nitric oxide at the appropriate time, achieving the therapeutic effect when needed without requiring ongoing daily administration.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If current compositions for treating sexual dysfunctions are used, then sexual function is improved, but side effects occur

Engineering Contradiction:
Improvesexual function improvementVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention changes the dosage parameters by providing specific ranges of L-arginine (4-20g) and L-citrulline (1-5g) that achieve therapeutic effects while minimizing side effects. This optimized parameter combination allows for effective sexual function improvement with a favorable safety profile, avoiding the side effects associated with other treatments.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If current compositions are used, then treatment effectiveness is achieved, but they are not effective for healthy individuals seeking enhancement

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidapplicability to healthy individuals
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The composition has dual functionality: it effectively treats sexual dysfunctions in individuals who need treatment, while also providing sexual enhancement for healthy individuals. The same active ingredients (L-arginine and L-citrulline) at the specified dosages achieve both therapeutic and enhancement effects, making the composition universally applicable across different user groups without requiring separate formulations.

Inventive Principle:
Principle #6Universality (Multi-functionality)

4Reliability

If L-arginine is administered to increase nitric oxide production, then blood flow to sexual organs is improved, but presystemic metabolism reduces effectiveness

Engineering Contradiction:
Improvenitric oxide productionVSAvoidbioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention combines both L-arginine and L-citrulline in a specific ratio (4:1 to 20:1 by weight). L-citrulline is converted to L-arginine in the kidneys, providing an additional source of the substrate for nitric oxide synthesis. This combination compensates for the presystemic metabolism of L-arginine by providing both direct L-arginine and a precursor (L-citrulline) that can be converted to L-arginine systemically, thereby improving overall bioavailability and nitric oxide production.

Inventive Principle:
Principle #5Merging (Combining)

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 composition effectively improves sexual arousal, emotional satisfaction, and orgasmic function in both males and females, offering a safe and effective way to enhance sexual experiences without daily dosing, with significant improvements in sexual function scores and minimal adverse effects.

Implementation Method 1

Nitric oxide (NO) is biosynthesized endogenously from L-Arginine, oxygen and NADPH by various nitric oxide synthase (NOS) enzymes. The NOS enzymes convert L-Arginine into L-Citrulline and NO using O2 as terminal oxidant.

Methodology Applied
Scientific EffectNitric oxide synthesis: Enzyme

Implementation Method 2

Nitric oxide functions by binding to the heme moiety of cytosolic guanylate cyclase, activating guanylate cyclase and increasing intracellular levels of cyclic guanosine monophosphate (cGMP).

Methodology Applied
Scientific EffectNitric oxide binding to guanylate cyclase: Chemical Bonding

Implementation Method 3

cGMP in turn relaxes vascular smooth muscle in blood vessels, which leads to vasodilation and increased blood flow both necessary to maintain erectile function.

Methodology Applied
Scientific EffectVasodilation:

Data Source

PatentUS11571405B2Compositions for improving sexual function
Publication Date: 2023.02.07 INXO IVS

AI summary

Compositions comprising L-arginine and L-citrulline in specific ratios are provided. Use of such compositions for improving sexual function in a healthy human subject are also provided.