Fixed-Dose Analgesic Composition Synergistic Pain Relief
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Solution Overview
Problem
Current pharmaceutical compositions for pain treatment, 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 paracetamol or propacetamol, face challenges with side effects at high dosages and prolonged use, necessitating a formulation that offers rapid therapeutic effects with high tolerability and safety while reducing undesired side effects.
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 paracetamol or propacetamol, formulated to provide a synergistic therapeutic effect, allowing for lower overall doses and reduced side effects, with varying weight ratios and administration forms to optimize efficacy and compliance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high dosages of (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 paracetamol are administered to achieve rapid and strong pain relief, then therapeutic efficacy is improved, but side effects increase
Solution Approach 1:
The patent combines two different analgesic mechanisms in a single pharmaceutical composition: (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 (a selective COX-2 inhibitor) and paracetamol (a non-selective COX inhibitor with additional central analgesic effects). This combination allows for synergistic pain relief at lower individual doses, reducing side effects while maintaining or improving therapeutic efficacy.
2Duration of action of stationary object
If prolonged use of high dosages is continued to maintain pain relief, then duration of action is improved, but tolerability and safety deteriorate
Solution Approach 1:
By combining two analgesics with different mechanisms of action and metabolic profiles, the patent achieves prolonged pain relief through complementary duration of action. The COX-2 selective inhibitor provides sustained peripheral analgesia while paracetamol contributes central analgesic effects, together extending the effective duration while allowing lower individual doses that improve tolerability for prolonged use.
3Reliability
If higher dosages are administered to ensure therapeutic effectiveness, then pain relief efficacy is improved, but patient compliance deteriorates due to side effects
Solution Approach 1:
The patent formulates both analgesics in a single combined pharmaceutical composition, improving patient compliance by simplifying the dosing regimen to one tablet instead of multiple medications. The synergistic combination allows effective pain relief at lower total doses with reduced side effects, further enhancing compliance. The fixed-dose combination ensures proper dosing ratios and facilitates adherence to treatment protocols.
Data Source
AI summary
The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient 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 selected from paracetamol and propacetamol.