Synergistic Pharmaceutical Composition for Pain Management

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Solution Overview

Problem

Current pharmaceutical compositions for pain management, particularly those containing (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and propionic acid derivatives, face challenges with side effects at high doses or prolonged use, and there is a need for compositions that offer rapid therapeutic effects with high tolerability and safety.

Innovation Solution

A pharmaceutical composition combining (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine with a propionic acid derivative, such as ibuprofen, in a synergistic ratio to reduce overall dose and minimize side effects, formulated into a single dosage form like a tablet for enhanced patient compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of analgesic compounds are administered to achieve rapid therapeutic effects, then pain relief efficacy is improved, but side effects increase

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

Solution Approach 1:

The patent combines two different analgesic compounds with distinct mechanisms of action into a single pharmaceutical composition. The first compound (1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine acts as an analgesic, while the second compound (a propionic acid derivative) provides anti-inflammatory effects. This combination allows for synergistic pain relief at lower individual doses, thereby reducing side effects while maintaining therapeutic efficacy.

Inventive Principle:
Principle #5Merging (Combining)

2Object-affected harmful factors

If multiple pharmacologically active compounds are combined in one dosage form to reduce overall dose, then side effects are reduced, but device complexity increases

Engineering Contradiction:
Improveside effectsVSAvoidcomposition complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent integrates two pharmacologically active compounds into a single pharmaceutical composition with a defined synergistic ratio. This merging approach reduces the need for multiple separate medications, simplifying the treatment regimen while maintaining the benefits of combined therapy with reduced side effects.

Inventive Principle:
Principle #5Merging (Combining)

3Duration of action of stationary object

If prolonged use of analgesic compounds is necessary for chronic pain management, then therapeutic effect is maintained, but accumulation of side effects occurs

Engineering Contradiction:
Improveduration of therapyVSAvoidaccumulated side effects
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent employs a combination of two analgesic compounds with different mechanisms of action, where the first compound provides analgesic effects and the second compound (propionic acid derivative) provides anti-inflammatory effects. This dual-mechanism approach allows for effective chronic pain management with reduced dosage of each individual compound, thereby minimizing the accumulation of side effects during prolonged therapy.

Inventive Principle:
Principle #5Merging (Combining)

4Adaptability or versatility

If separate dosage forms are used for different analgesic compounds to maintain flexibility, then adaptability is improved, but ease of operation decreases

Engineering Contradiction:
Improvedosage flexibilityVSAvoidpatient compliance
Core Design Contradiction:
Adaptability or versatilityVSEase of operation

Solution Approach 1:

The patent combines two analgesic compounds into a single pharmaceutical composition, eliminating the need for patients to take multiple separate medications. This unified dosage form significantly improves patient compliance and ease of operation while maintaining the therapeutic benefits of combined therapy. The composition can be administered in various routes (oral, parenteral, topical) providing adequate dosage flexibility.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS10076510B2Pharmaceutical composition comprising (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano-[3,4,b]indol]-4-amine and a propionic acid derivative
Publication Date: 2018.09.18 ADNEURIS THERAPEUTICS INC
  • US10076510B2 patent drawing
  • US10076510B2 patent drawing
  • US10076510B2 patent drawing

AI summary

The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient, which is selected from (1r,4r)-6′-fluoro-N,N-dimethyl-4-phenyl-4′,9′-dihydro-3′H-spiro[cyclohexane-1,1′-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient, which is a propionic acid derivative selected from the group consisting of ibuprofen, naproxen, ketoprofen, flurbiprofen, fenoprofen, fenbufen, suprofen, pirprofen, indoprofen, tiaprofenic acid, oxaprozin, ibuproxam, flunoxaprofen, alminoprofen, naproxcinod, and the physiologically acceptable salts thereof.