Topical Psoriasis Composition Combining Antimitotic and Anti-inflammatory Agents

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Solution Overview

Problem

Current treatments for psoriasis often have low efficacy and significant side effects, with existing medications failing to provide an optimal solution for managing the condition effectively without adverse reactions.

Innovation Solution

A topical pharmaceutical composition combining 4,6-dimethyl-N-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine and 2,4-O-(2-furanylmethylene)-1,3,5,6-tetra-O-methyl-D-glucitol, formulated with suitable excipients, which enhances therapeutic efficacy and reduces relapse periods without side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments (corticosteroids, tar, photochemotherapy) are used, then some therapeutic effect is achieved, but significant side effects occur

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

Solution Approach 1:

The patent combines two distinct compounds with different mechanisms of action: 4,6-dimethyl-N-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine (antimitotic agent) and 2,4-O-(2-furanylmethylene)-1,3,5,6-tetra-O-methyl-D-glucitol (anti-inflammatory agent). This combination creates a synergistic effect that enhances therapeutic efficacy while reducing the need for high doses of individual agents, thereby minimizing side effects.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite pharmaceutical formulation containing both compounds in specific proportions (0.1-10% w/w of compound I and 0.1-10% w/w of compound II). This composite approach allows the formulation to leverage the benefits of both agents simultaneously, achieving reliable therapeutic results without the severe side effects associated with conventional monotherapies.

Inventive Principle:
Principle #40Composite materials

2Reliability

If chemotherapeutic agents (cyclosporine A, methotrexate, retinoids) are used, then severe psoriasis is treated, but high liver toxicity occurs

Engineering Contradiction:
Improveeffectiveness in severe psoriasisVSAvoidliver toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines an antimitotic compound with moderate cytostatic action and a low-toxicity compound with anti-inflammatory properties. This combination provides effective treatment for severe psoriasis through synergistic action on different pathological pathways, while avoiding the high liver toxicity associated with conventional chemotherapeutic agents like cyclosporine A and methotrexate.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If biopharmaceuticals (monoclonal antibodies) are used, then good activity with low organ toxicity is achieved, but they are ineffective in obese individuals and inadvisable for patients with tumour history

Engineering Contradiction:
Improveactivity with low organ toxicityVSAvoidsuitability for all patient populations
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent creates a topical formulation with dual mechanisms of action that can be universally applied across different patient populations. The combination of antimitotic and anti-inflammatory compounds addresses multiple aspects of psoriasis pathology, making the treatment effective and safe for obese individuals and patients with tumour history, whereas biopharmaceuticals have specific contraindications for these groups.

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

4Reliability

If single compound treatments are used, then treatment is simple, but efficacy is insufficient for optimal psoriasis management

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges two compounds with complementary mechanisms of action into a single topical formulation, achieving synergistic therapeutic effects that are superior to either compound alone. The formulation maintains relative simplicity by combining agents that work through different pathways, addressing both cell proliferation and inflammation, thereby optimizing efficacy without excessive complexity.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP3164110B1Pharmaceutical compositions for the treatment of psoriasis
Publication Date: 2019.10.02 SPECIAL PRODS LINE
  • EP3164110B1 patent drawing
  • EP3164110B1 patent drawing

AI summary

Pharmaceutical compositions for topical administration for the treatment of psoriasis are described, containing as active ingredient therapeutically effective quantities of 4,6-dimethyl-N-(3,4,5-trimethoxyphenyl)pyrimidin-2-amine (I) and 2,4-O-(2-furanylmethylene)-1,3,5,6-tetra-O-methyl-D-glucitol combined with suitable excipients and/or diluents.