Characterization of Transdermal Pharmacokinetics of Ketoprofen in Sinclair and Gottingen Minipigs

Authors

Stricker-Krongrad, A., Zhong, M., Leigh, H., Liu, Y., Fu, Y.A., Liu, J., Bouchard, G.F.

Abstract

Purpose: To characterize transdermal pharmacokinetics of a ketoprofen cream formulation in the Sinclair and
Gӧttingen strains of minipigs.

Methods: Sinclair and Gӧttingen minipigs (3 per gender of each strain) were used in this study. Four mL of 2.5%
ketoprofen cream were topically applied on the back of each minipig in an area equivalent to ~3% of the total
body surface area (BSA). Blood samples were collected predose and at multiple time points postdose. Plasma
samples were analyzed with LC/MS/MS system. The linear range of quantitation for ketoprofen was 50 to 25600
ng/mL. Individual animal data were analyzed with the non-compartmental analysis. Area under the plasma
concentration versus time curve (AUC) was calculated with the liner trapezoidal method.

Results: Although ketoprofen was shown to be absorbed better in Gӧttingen than in Sinclair minipigs in the
average plasma concentration time curves (Figure 1), no statistically significant difference was observed between
the PK parameters of the two strains (Table 2). These data suggested that ketoprofen had a similar ADME process
in both minipigs, which was supported by the fact that ketoprofen had a similar terminal half-life, time to the
maximum plasma concentration, and mean residence time in both strains of minipigs.

Conclusion: Ketoprofen displays a similar ADME profile in both Sinclair and Gӧttingen minipigs, which fits a one
compartment model.

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