Simmondsin Enteric Formulation for Targeted Release

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Solution Overview

Problem

Current pharmaceutical compositions for treating degenerative diseases like cancer and arthritis often require high doses and result in significant side effects due to uncontrolled release of active agents in the stomach, leading to inefficient treatment and adverse reactions.

Innovation Solution

An oral enteric formulation comprising jojoba components and enzymes that release the active agents specifically in the small intestine, modulating Fibroblast Growth Factor and angiogenesis, while controlling intestinal microflora, to achieve targeted and reduced dosing with fewer side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of simmondsin are administered to treat degenerative diseases, then therapeutic effect is improved, but side effects increase

Engineering Contradiction:
Improvetherapeutic effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by pre-incubating simmondsin with beta-glucosidase before administration to patients. This enzymatic pre-treatment converts simmondsin into its active form (simmondsin aglycon) in advance, ensuring that the therapeutic agent is already activated and ready to exert its anti-angiogenic effect at lower doses, thereby improving therapeutic efficacy while reducing side effects associated with high dose administration.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses beta-glucosidase as an intermediary substance to facilitate the conversion of simmondsin into its active form. This enzyme acts as a mediator that enables the therapeutic transformation of the compound, allowing controlled activation and reducing the need for high doses of the original simmondsin compound, thus improving the therapeutic index.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If simmondsin is released in the stomach, then absorption is achieved, but uncontrolled release causes side effects

Engineering Contradiction:
Improveabsorption efficiencyVSAvoiduncontrolled release side effects
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent applies the taking out principle by removing simmondsin from its glucoside form through enzymatic hydrolysis using beta-glucosidase. This extraction of the glucose moiety yields the active simmondsin aglycon, which can be selectively released and absorbed in the gastrointestinal tract without the unwanted side effects associated with releasing the intact glucoside form in the stomach.

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If jojoba components are used to treat cancer and arthritis, then disease treatment is improved, but dosage control becomes difficult

Engineering Contradiction:
Improvedisease treatment efficacyVSAvoiddosage control
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent applies parameter changes by transforming simmondsin from its glucoside form to its aglycon form through enzymatic hydrolysis. This chemical transformation changes the pharmacokinetic parameters of the compound, resulting in improved bioavailability, enhanced therapeutic efficacy at lower doses, and better dosage control for treating diseases such as cancer and arthritis.

Inventive Principle:
Principle #35Parameter changes

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 formulation effectively treats or relieves degenerative diseases with lower doses, reducing side effects and improving treatment efficiency by targeted release and modulation of key biological pathways, maintaining a balance in angiogenesis and Fibroblast Growth Factor activity.

Implementation Method 1

at least one enzyme suitable to splice off the glucose moiety of one or more Jojoba components

Methodology Applied
Scientific EffectEnzyme: Enzyme

Implementation Method 2

submitting jojoba oil to a heat treatment at a temperature of 150 to 350° C. in presence of an acidic bentonite clay

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS11406678B2Simmondsin formulation
Publication Date: 2022.08.09 RAES STEFAAN
  • US11406678B2 patent drawing
  • US11406678B2 patent drawing
  • US11406678B2 patent drawing

AI summary

A human oral at least partly enteric formulation comprising one or more jojoba components, for controlling, stimulating or modulating functions for patients suffering from a degenerative disease, or for patients at risk from suffering from a degenerative disease, or for patients under therapeutic treatment of a degenerative disease.