Sceletium Extract PDE4 Inhibitor with Activity Enhancer

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Solution Overview

Problem

Current PDE4 inhibiting compounds have narrow therapeutic windows and often cause undesirable side effects such as nausea, diarrhea, and headaches, while there is a demand for naturally derived PDE4 inhibitors that can achieve effective PDE4 inhibition with minimal adverse effects.

Innovation Solution

A formulation comprising a Sceletium extract combined with an activity enhancer, which enhances PDE4 inhibitory activity beyond the levels achieved by either component alone, offering a synergistic effect that is more effective than additive, thereby potentially reducing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If PDE4 inhibiting compounds are administered at therapeutically effective doses, then PDE4 inhibition is achieved, but undesirable side effects such as nausea, diarrhea, and headaches occur

Engineering Contradiction:
ImprovePDE4 inhibition efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters of PDE4 inhibitors by deriving them from natural sources (plants, fungi, bacteria) rather than synthetic compounds. This parameter change in the source and chemical structure allows achieving PDE4 inhibition while reducing the narrow therapeutic window and associated side effects of conventional synthetic PDE4 inhibitors

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite natural-derived compounds and their combinations as PDE4 inhibitors. By using composite materials from natural sources rather than single synthetic compounds, the invention achieves therapeutic effects with improved safety profiles and reduced adverse side effects

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If naturally derived PDE4 inhibitors are developed, then consumer demand for natural ingredients is met, but achieving effective PDE4 inhibition with minimal side effects remains challenging

Engineering Contradiction:
Improvenatural ingredient demandVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent identifies multiple natural sources (plants, fungi, bacteria) that produce PDE4 inhibiting compounds. This universality across different natural sources provides a versatile platform to meet consumer demand for natural ingredients while maintaining therapeutic effectiveness through diverse biochemical pathways

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

Data Source

PatentUS10179155B2Phosphodiesterase-4 inhibiting phytochemical compositions
Publication Date: 2019.01.15 NATURES SUNSHINE PRODUCTS INC
  • US10179155B2 patent drawing

AI summary

Phosphodiesterase-4 (PDE4) inhibiting compositions comprising a Sceletium and an activity enhancer are disclosed and described. Methods and systems for inhibiting PDE4, as well as, dosage forms comprising a Sceletium extract and an activity enhancer are also disclosed. Additionally disclosed are methods for enhancing the potency or PDE4 inhibitory activity of a Sceletium extract by addition of an activity enhancer.