Tocopherol Ester Nasal Composition for Allergic Rhinitis

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Solution Overview

Problem

Current treatments for allergic rhinitis often have side effects and poor patient compliance, leading to risks of disease diffusion to other allergens and allergic asthma.

Innovation Solution

A topical composition containing an ester of alpha-tocopherol, such as alpha-tocopheryl acetate or alpha-tocopheryl linoleate, combined with an oily vehicle like hydrogenated polydecene, for direct application to the nasal mucosa, which forms a protective film or chemically neutralizes allergens, reducing symptoms without systemic side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If antihistamines and corticosteroids are used for treatment of allergic rhinitis, then symptom relief is achieved, but side effects occur and patient compliance decreases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and eliminates the harmful side effects associated with conventional antihistamines and corticosteroids by using a purely natural composition of tocopherol esters and plant oils, which provides effective symptom relief without the adverse reactions that limit patient compliance

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention uses a composite formulation combining multiple tocopherol esters (alpha-tocopheryl acetate, gamma-tocopheryl acetate) with plant-derived oils (olive oil, sunflower oil, hemp seed oil) to create a synergistic composition that maintains treatment effectiveness while avoiding the side effects of synthetic pharmaceuticals

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional medications are used for allergic rhinitis, then some symptom relief is provided, but patient compliance remains inadequate leading to disease diffusion

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent employs a simple, natural composition that can be easily applied topically to the nasal mucosa, replacing complex pharmaceutical regimens with a user-friendly formulation that patients are more willing to use consistently, thereby preventing disease diffusion through improved compliance

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Object-generated harmful factors

If tocopherol and vitamin E are used alone, then antioxidant effects are provided, but insufficient therapeutic effect is achieved for allergic rhinitis

Engineering Contradiction:
Improveoxidative stress reductionVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent merges tocopherol esters with plant-derived oils containing complementary active substances (flavonoids, phenolic compounds, essential oils) to create a synergistic composition where the combined therapeutic effect exceeds the sum of individual components, achieving effective treatment of allergic rhinitis

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite material combining tocopherol esters with plant oils rich in bioactive compounds, where the interaction between different substances produces enhanced anti-inflammatory, antiallergic, and protective effects that neither component achieves alone

Inventive Principle:
Principle #40Composite materials

4Stability of the object's composition

If topical compositions contain emulsifiers and carriers, then stability is improved, but the composition becomes more complex and less natural

Engineering Contradiction:
Improveformulation stabilityVSAvoidcomposition complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent uses plant-derived oils that naturally serve as both carriers and stabilizing agents for the tocopherol esters, eliminating the need for additional emulsifiers and synthetic carriers. The plant oils' natural properties provide sufficient stability while maintaining a simple, natural formulation

Inventive Principle:
Principle #25Self-service

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 reduces nasal obstruction, secretion, and improves sleep and quality of life, allowing patients to reduce or discontinue antihistamines and corticosteroids, with high patient adherence and willingness to continue treatment.

Implementation Method 1

a compound that inhibits reactive oxygen species... tocopherol

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Implementation Method 2

for topical application... direct application to the nasal mucosa, which forms a protective film

Methodology Applied
Scientific EffectFilm formation: Coatings

Data Source

PatentEP3171873B1Composition comprising an ester of alpha-tocopherol for prevention and treatment of allergic rhinitis
Publication Date: 2019.12.25 BIO LO GA SRL

AI summary

Composition for topical application, for use in the prevention and treatment of allergic rhinitis, consisting ofan ester of alpha-tocopherol selected from the group consisting of tocopheryl acetate, n-propionate and linoleate, and an oily vehicle selected from the group consisting of hydrogenated polyisobutene, hydrogenated polydecene and mixtures of hydrogenated polyisobutene and/or hydrogenated polydecene with hydrogenated polyolefins, in particular hydrogenated C6-C14 hydrogenated polyolefins, Caprylic/Capric Triglyceride, Olus Oil, Adansonia Digitata Oil, Adansonia Digitata Seed Oil, Coco-Caprylate/Caprate, Olive Squalane, Olive Squalene, Sunflower (Heliantus Annus) Seed Oil, Coco-Caprylate, Isononyl Isononanoate, Cyclopentasiloxane, and mixtures thereof.