Topical Gel Formulation with Menthol Penetration Enhancer
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Solution Overview
Problem
Current pharmaceutical formulations combining flurbiprofen and thiocolchicoside require multiple drugs for administration, leading to application difficulties and systemic side-effects, with suboptimal skin absorption rates, especially in acute situations like sports injuries, necessitating enhanced percutaneous penetration for rapid pain relief.
Innovation Solution
A topical gel formulation comprising flurbiprofen, thiocolchicoside, and menthol, with carbomer and triethanolamine as viscosity enhancers, and polysorbate and ethyl alcohol as penetration enhancers, formulated to achieve anti-inflammatory, analgesic, and myorelaxant activities, enhancing skin absorption and providing a local anesthetic effect.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If multiple separate drugs are used for administration, then comprehensive therapeutic coverage is achieved, but application difficulty increases and systemic side-effects occur
Solution Approach 1:
The patent combines flurbiprofen (anti-inflammatory and analgesic), thiocolchicoside (muscle relaxant), and menthol (local anesthetic and penetration enhancer) into a single topical gel formulation. This merging of multiple therapeutic agents into one product eliminates the need for separate administrations, reduces application complexity, and minimizes systemic side-effects while maintaining comprehensive therapeutic coverage for musculoskeletal conditions.
2Ease of operation
If standard topical formulations are used, then ease of application is maintained, but skin absorption rate remains suboptimal
Solution Approach 1:
Menthol serves as a penetration enhancer in the gel formulation, acting as an intermediary that facilitates the percutaneous absorption of flurbiprofen and thiocolchicoside. The menthol disrupts the stratum corneum lipid structure temporarily, creating pathways for enhanced drug penetration while maintaining the ease of topical application. This mediator approach achieves rapid local therapeutic effects without compromising application simplicity.
3Productivity
If penetration enhancers are added to improve absorption, then percutaneous penetration is enhanced, but formulation complexity increases
Solution Approach 1:
Menthol performs multiple functions simultaneously in the gel formulation: it acts as a local anesthetic providing immediate pain relief, serves as a penetration enhancer to facilitate drug absorption, and contributes to the cooling sensation that masks pain. This multi-functionality approach enhances percutaneous penetration without significantly increasing formulation complexity, as a single ingredient achieves multiple therapeutic and pharmacokinetic goals.
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 formulation achieves rapid absorption and localized pain relief, shortening treatment time and providing mental and psychological benefits through enhanced percutaneous penetration and anesthetic effects, suitable for conditions like osteoarthritis, muscle spasms, and sports injuries.
Implementation Method 1
The rate of percutaneous penetration of said combination is enhanced with the auxiliaries it contains
Implementation Method 2
with the menthol used in said combination stimulating the receptors by which the cold sensation is perceived
Data Source
AI summary
A topical pharmaceutical gel comprising flurbiprofen or a pharmaceutically acceptable salt of flurbiprofen, thiocolchicoside or a pharmaceutically acceptable salt of thiocolchicoside, and menthol. The present invention more particularly relates to pharmaceutical combinations of flurbiprofen, thiocolchicoside, and menthol in the form of topical gels with anti-inflammatory, analgesic, and myorelaxant activities.