Corticosteroid and Kinin B2 Receptor Antagonist Compositions

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Solution Overview

Problem

Current treatments for osteoarthritis primarily focus on symptom relief and do not halt the progression of the disease, with long-term use of pain medications like NSAIDs and corticosteroids leading to adverse effects, and there is a need for more effective anti-inflammatory and analgesic solutions with reduced side effects.

Innovation Solution

Combining a corticosteroid with a kinin B2 receptor antagonist in pharmaceutical compositions to achieve additive and synergistic anti-inflammatory and analgesic effects, allowing for lower corticosteroid doses and longer-lasting therapeutic outcomes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If NSAIDs and corticosteroids are used for pain relief in osteoarthritis, then pain reduction is achieved, but adverse effects increase (gastrointestinal ulcers, platelet aggregation)

Engineering Contradiction:
ImprovepainVSAvoidadverse effects
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent combines a kinin B2 receptor antagonist with a corticosteroid in a single pharmaceutical composition. This combination allows the kinin antagonist to provide analgesic effects while the corticosteroid provides anti-inflammatory effects, achieving pain relief with reduced gastrointestinal and platelet-related adverse effects compared to NSAID monotherapy.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent modifies the therapeutic approach by changing the receptor target parameter from traditional NSAID COX-1/COX-2 inhibition to kinin B2 receptor antagonism. This parameter change enables pain relief through a different mechanism that avoids the harmful gastrointestinal and platelet effects associated with NSAIDs.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If conventional treatments are used to reduce pain symptoms, then quality of life improves, but disease progression continues

Engineering Contradiction:
Improvepain symptomsVSAvoiddisease progression
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent extracts and targets the specific pathophysiological mechanism of kinin B2 receptor activation in osteoarthritis. By selectively blocking this receptor pathway, the treatment addresses the underlying inflammatory process that drives disease progression, rather than merely masking symptoms.

Inventive Principle:
Principle #2Taking out (Extraction)

3Reliability

If higher doses of corticosteroids are administered, then anti-inflammatory effect increases, but side effects increase

Engineering Contradiction:
Improveanti-inflammatory effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent merges a kinin B2 receptor antagonist with a corticosteroid to achieve synergistic anti-inflammatory effects. The kinin antagonist enhances the anti-inflammatory activity of the corticosteroid, allowing effective treatment at lower corticosteroid doses that minimize side effects while maintaining therapeutic efficacy.

Inventive Principle:
Principle #5Merging (Combining)

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 combination of corticosteroids and kinin B2 receptor antagonists provides a complete anti-inflammatory effect, significantly reduces pain, and can be administered at lower doses, offering a more effective treatment for osteoarthritis and other inflammatory disorders with minimal side effects.

Implementation Method 1

a kinin B2 receptor antagonist... Bradykinin, through stimulation of the B2 receptor, is one of the most important mediators of inflammation and pain

Methodology Applied
Scientific EffectReceptor antagonism:

Implementation Method 2

Their anti-inflammatory and antiallergic action is mainly produced by inducing synthesis of the enzyme lipocortin, which inhibits phospholipase A2

Methodology Applied
Scientific EffectPhospholipase A2 inhibition:

Implementation Method 3

Combining a corticosteroid with a kinin B2 receptor antagonist in pharmaceutical compositions to achieve additive and synergistic anti-inflammatory and analgesic effects

Methodology Applied
Scientific EffectSynergistic interaction:

Data Source

PatentEP2303268B1Pharmaceutical compositions based on kinin b2 receptor antagonists and corticosteroids, and their use
Publication Date: 2012.06.20 IST LUSO FARMACO D ITALA SRL
  • EP2303268B1 patent drawing
  • EP2303268B1 patent drawing
  • EP2303268B1 patent drawing

AI summary

Disclosed are pharmaceutical compositions containing, as active ingredients, a mixture of a corticosteroid and a kinin B2 receptor antagonist. Said compositions have proved particularly effective, especially in the treatment of inflammatory disorders such as asthma, ophthalmic or dermatological disorders and, above all, as regards the joints, arthritis.