Budesonide and Luminol Synergistic Combination for COPD

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Solution Overview

Problem

Long-term administration of budesonide, a commonly used glucocorticoid, is associated with several serious side effects, and there is a medical need to reduce the dosage while maintaining its therapeutic effectiveness and minimizing adverse effects.

Innovation Solution

The combination of budesonide with 5-amino-2,3-dihydro-1,4-phthalazinedione or its sodium salt, which acts synergistically to enhance the anti-inflammatory effects of budesonide, allowing for a reduction in budesonide dosage without compromising its efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If budesonide is administered long-term, then therapeutic effectiveness is maintained, but serious side effects occur

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

Solution Approach 1:

The patent combines budesonide with 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) to create a synergistic pharmaceutical combination. This merging of two substances allows the therapeutic effectiveness to be maintained while reducing the dosage of budesonide, thereby minimizing its harmful side effects. The combination exhibits supraadditive effects, where the combined action is greater than the sum of individual effects.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent changes the dosing parameter by reducing the amount of budesonide administered when used in combination with luminol. This parameter change is enabled by the synergistic interaction between the two drugs, which allows achieving the same therapeutic effect at lower budesonide doses, thus reducing harmful effects while maintaining reliability.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If budesonide dosage is reduced, then side effects are minimized, but therapeutic effectiveness may be compromised

Engineering Contradiction:
Improveside effectsVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

Luminol acts as an intermediary substance that enhances the anti-inflammatory effects of budesonide. When administered together, luminol mediates the therapeutic action, allowing reduced budesonide dosing while maintaining effectiveness. The synergistic interaction ensures that the combined preparation achieves the desired therapeutic outcome at lower individual drug doses.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite pharmaceutical preparation combining budesonide and luminol. This composite material exhibits synergistic properties where the combination produces greater anti-inflammatory effect than either drug alone, enabling dose reduction of budesonide while preserving therapeutic effectiveness and reducing side effects.

Inventive Principle:
Principle #40Composite materials

3Reliability

If higher doses of budesonide are used, then therapeutic effectiveness is achieved, but adverse drug reactions increase

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidadverse drug reactions
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent merges budesonide with luminol to create a synergistic combination that achieves therapeutic effectiveness at lower budesonide doses. This combining approach reduces the overall drug load and minimizes adverse reactions while maintaining the desired anti-inflammatory effect through the synergistic interaction between the two agents.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent changes the dosing parameter by using lower budesonide doses in the context of luminol combination therapy. This parameter change is supported by the synergistic mechanism, which ensures that therapeutic effectiveness is maintained even at reduced doses, thereby decreasing the frequency and severity of adverse drug reactions.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20250064800A1Combination of budesonide and 5-amino-2,3-dihydro-1,4-phthalazinedione
Publication Date: 2025.02.27 METRIOPHARM AG
  • US20250064800A1 patent drawing
  • US20250064800A1 patent drawing
  • US20250064800A1 patent drawing

AI summary

The present invention relates to a combination of budesonide and 5-amino-2,3-dihydro-1,4-phthalazinedione or one of its pharmaceutically acceptable salts. This pharmaceutical combination shall be used in the treatment of chronic inflammatory diseases, especially COPD, asthma, Crohn's disease, colitis ulcerosa and autoimmune hepatitis. The invention relates in particular to the use of 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt in this combination. Pharmaceutical compositions, advantageous formulation techniques and a method of treatment are disclosed.