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[The percutaneous absorption of diclofenac]
Arzneimittel-Forschung
|July 1, 1986
Summary
Diclofenac absorption via topical formulations like Voltaren Emulgel and Voltaren cream was studied in animals and humans. Both formulations demonstrated effective percutaneous absorption and localized drug delivery for potential pain relief.
Area of Science:
- Pharmacology
- Dermatology
- Drug Delivery
Context:
- Topical non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for pain management.
- Understanding the percutaneous absorption and tissue distribution of topical diclofenac is crucial for optimizing therapeutic efficacy and minimizing systemic exposure.
Purpose:
- To investigate and compare the percutaneous absorption of diclofenac diethylammonium in an emulsion cream/gel (Voltaren Emulgel) versus diclofenac sodium in a cream formulation (Voltaren cream).
- To evaluate the transdermal delivery, tissue penetration, and plasma concentration profiles of diclofenac in preclinical models (guinea-pig, rabbit) and humans.
Summary:
- Percutaneous absorption of diclofenac sodium cream in guinea-pigs was 3-6% under occlusion.
- Topical diclofenac penetrated rabbit knee joint tissues, including synovial fluid.
- In humans, Voltaren Emulgel showed 6% absorption on non-occluded skin over 12 hours, with similar metabolite patterns to oral administration.
Impact:
- Provides insights into the comparative absorption and distribution of different topical diclofenac formulations.
- Supports the use of topical diclofenac for localized pain relief with predictable systemic levels.
- Informs formulation development and clinical application of topical NSAIDs for musculoskeletal conditions.