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[Binding affinity of ibuprofen in human tissues].
Arzneimittel-Forschung
|March 1, 1992
Summary
This study investigated ibuprofen binding to human tissues. Muscle tissue showed the highest ibuprofen concentration, while tendons had the lowest, explaining in vivo findings after topical application.
Area of Science:
- Pharmacology
- Tissue distribution
- Drug binding kinetics
Context:
- Understanding drug distribution is crucial for optimizing topical therapies.
- Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID).
- Local application of ibuprofen cream necessitates knowledge of its tissue penetration and retention.
Purpose:
- To investigate the in vitro binding of ibuprofen to various human tissues.
- To correlate in vitro tissue binding with observed in vivo tissue concentrations.
- To elucidate the pharmacokinetic behavior of ibuprofen in different human tissue types.
Summary:
- Radioactive ibuprofen was incubated with human skin, subcutaneous tissue, muscle, tendon, and joint capsule tissues at 37°C for 2 hours.
- Following incubation, tissues were washed, and radioactivity was quantified using a liquid scintillation counter to determine ibuprofen binding.
- Results indicated specific binding of ibuprofen across different tissues, with muscle tissues exhibiting the highest concentrations and tendons the lowest.
Impact:
- Provides a mechanistic explanation for observed in vivo differences in ibuprofen tissue concentrations after topical administration.
- Informs the development and application of localized ibuprofen therapies.
- Contributes to the understanding of NSAID pharmacokinetics in diverse human tissues.