Compounded Topical Cream Using DMSO Penetration Enhancer
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Solution Overview
Problem
Current compounded topical compositions for pain and inflammation often require high concentrations of active ingredients, which can pose safety risks, especially for patients with gastric issues or on blood thinners, and may not provide effective penetration into the skin.
Innovation Solution
A method of compounding a topical cream by combining lidocaine and prilocaine with diclofenac sodium, using commercially available medicated solutions and powders, to create a stable formulation with lower concentrations of active ingredients, enhancing safety and penetration through the inclusion of DMSO in the diclofenac sodium solution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high concentrations of active ingredients are used in topical compositions, then pain relief and inflammation management effectiveness is improved, but safety risks increase for patients with gastric issues or on blood thinners
Solution Approach 1:
The patent changes the concentration parameters of active ingredients from high to low levels, while compensating for reduced potency through enhanced delivery mechanisms. Specifically, the formulation uses lower concentrations of lidocaine, prilocaine, and diclofenac sodium, but achieves comparable or superior therapeutic effects through improved skin penetration and sustained release properties.
Solution Approach 2:
The patent creates a composite topical formulation combining multiple active ingredients (lidocaine, prilocaine, diclofenac sodium) with specific excipients and delivery systems. This composite approach allows synergistic effects where the combination of substances at lower concentrations achieves better therapeutic outcomes than individual high-concentration formulations, while reducing adverse effects.
2Reliability
If high concentrations of active ingredients are used, then therapeutic effectiveness is improved, but skin penetration capability deteriorates due to formulation stability issues
Solution Approach 1:
The patent optimizes formulation parameters including pH, ionic strength, and surfactant concentrations to enhance skin penetration of active ingredients. The formulation uses specific pH adjustments and surfactant systems that improve transdermal delivery while maintaining physical and chemical stability of the composition over time.
Solution Approach 2:
The patent introduces intermediary substances such as surfactants and penetration enhancers that facilitate the delivery of active ingredients through the skin barrier. These intermediaries improve bioavailability and penetration depth without requiring high concentrations of the active pharmaceutical ingredients, thereby maintaining formulation stability.
3Object-affected harmful factors
If lower concentrations of active ingredients are used, then safety profile is improved, but penetration depth into skin deteriorates
Solution Approach 1:
The patent employs penetration enhancers and surfactants as intermediary substances that facilitate deep skin penetration of low-concentration active ingredients. These intermediaries temporarily modify the skin barrier properties or form delivery vehicles that transport the pharmaceuticals deeper into the skin layers, achieving therapeutic effects at safer lower concentrations.
Solution Approach 2:
The patent utilizes porous carriers or micellar systems that can encapsulate active ingredients and deliver them deep into the skin. These porous structures provide sustained release and enhanced penetration while maintaining low bulk concentrations of the active ingredients in the formulation.
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 compounded topical solution provides effective pain relief and inflammation management with a reduced safety risk profile, allowing for deeper skin penetration and maintaining stability over time without separation or degradation.
Implementation Method 1
enhancing safety and penetration through the inclusion of DMSO in the diclofenac sodium solution
Implementation Method 2
Lidocaine and prilocaine cream, 2.5%/2.5% is a eutectic mixture of lidocaine 2.5% and prilocaine 2.5% formulated as an oil in water emulsion and is indicated for use on normal intact skin for local analgesia
Implementation Method 3
Diclofenac sodium topical solution is a non-steroidal anti-inflammatory drug (NSAID) indicated for the treatment of signs and symptoms of osteoarthritis of the knee
Data Source
AI summary
A method of compounding a topical cream includes combining ingredients including lidocaine and prilocaine, 2.5%/2.5%, cream, lidocaine hydrochloride, 4%, topical solution; and mixing the ingredients to generate a cream.