Phosphatidylserine Sodium Salt Curcumin Stabilization

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Solution Overview

Problem

Current pharmaceutical formulations of phosphatidylserine (PS) are prone to degradation and oxidation, limiting their stability and bioavailability, especially when combined with curcumin, which has low bioavailability due to its lipophilicity, making it ineffective in treating brain aging and osteoporosis-related disorders.

Innovation Solution

A stable combination of PS sodium salt and curcumin is developed, which stabilizes PS, preventing degradation and enhancing bioavailability, allowing for the formulation of stable pharmaceutical products in various forms, including soft capsules, tablets, and solutions, thereby maintaining pharmacological properties and improving treatment efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If phosphatidylserine is formulated in conventional pharmaceutical forms, then it can be administered for cognitive disorders, but it degrades and oxidizes rapidly, forming harmful degradation products

Engineering Contradiction:
Improvestability of phosphatidylserineVSAvoiddegradation products
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Curcumin acts as an intermediary substance that protects phosphatidylserine from degradation and oxidation. The curcumin molecule interferes with the harmful chemical reactions that would otherwise degrade PS, serving as a protective mediator between PS and environmental factors causing degradation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite pharmaceutical formulation combining phosphatidylserine and curcumin in specific ratios (1:4 to 4:1 w/w). This composite material leverages the stabilizing properties of curcumin to protect the labile phosphatidylserine component, resulting in a formulation with enhanced overall stability.

Inventive Principle:
Principle #40Composite materials

2Reliability

If curcumin is used to stabilize phosphatidylserine, then degradation is prevented, but curcumin has low bioavailability due to lipophilicity

Engineering Contradiction:
Improvestability of formulationVSAvoidbioavailability of curcumin
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention optimizes the concentration parameters of both curcumin and phosphatidylserine within specific ranges (0.1-10 mg curcumin per mg PS). By adjusting these parameters, the formulation achieves a balance where curcumin provides sufficient stabilization while remaining at concentrations that improve bioavailability through synergistic absorption mechanisms.

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If phosphatidylserine is administered alone, then cognitive benefits are achieved, but the treatment is ineffective for osteoporosis and osteoarthritis

Engineering Contradiction:
Improvetherapeutic scopeVSAvoidefficacy for bone disorders
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The curcumin-phosphatidylserine formulation achieves multi-functionality, treating not only cognitive disorders but also osteoporosis and osteoarthritis. Curcumin contributes anti-inflammatory and bone-protective properties, while phosphatidylserine provides neuronal membrane stabilization, creating a universally applicable therapeutic agent for multiple age-related conditions.

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

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 PS sodium salt/curcumin combination reduces nitric oxide production, inhibits inflammatory cytokines, and promotes neuronal differentiation, demonstrating synergistic effects in treating neurodegenerative disorders and osteoporosis, with improved bioavailability and stability compared to previous formulations.

Implementation Method 1

Curcumin (diferuloylmethane; 1,7-bis[4-hydroxy-3-methoxyphenyl]-1,6-heptadiene-3,5-dione) is a liposoluble molecule... its anti-inflammatory and antioxidant power is well documented

Methodology Applied
Scientific EffectAntioxidant: Oxidation

Data Source

PatentEP2806866B1Pharmaceutical compositions containing phosphatidylserine sodium salt and curcumin
Publication Date: 2018.11.28 FIDIA FARM SPA
  • EP2806866B1 patent drawingFigure 1
  • EP2806866B1 patent drawingFigure 2
  • EP2806866B1 patent drawingFigure 3

AI summary

The present invention describes and claims stable pharmaceutical compositions and/or food supplements based on phosphatidylserine (PS) and curcumin, which are consequently devoid of degradation products, for use in the prevention and treatment of disorders associated with brain aging, and in the prevention and treatment of osteoporosis and/or osteoarthritis.