Percutaneous Penetration Kinetics of Lidocaine and Prilocaine in Two Local Anesthetic Formulations Assessed by in Vivo Microdialysis in Pigs(Biopharmacy)

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The aim of this study was to characterize and compare the percutaneous penetration kinetics of lidocaine (L) and prilocaine (P) in two local anesthetic formulations by in vivo microdialysis coupled with HPLC. The microdialysis system for studying lidocaine and prilocaine was calibrated by a no-net-flux method in vitro and retrodialysis method in vivo, respectively. A dosage of 0.2 g/cm^2 of an in-house P-L formulation (2.5% lidocaine and 2.5% prilocaine, methylcellulose-based) and commercially available Eutectic Mixture of Local Anesthesia (EMLA, 2.5% lidocaine and 2.5% prilocaine, carbopol-based) was separately but symmetrically applied in the dorsal region of pigs. Saline (0.9%, w/v) was perfused into the linear microdialysis probe at a flow rate of 1.5μl/min. Dialysate was collected upon topical application up to 6 h at 20-min intervals and assessed by HPLC. The results demonstrated the area under the concentration-time curve (AUC_<0-6h>) of lidocaine and prilocaine in EMLA was 71.95±23.36μgh/ml and 38.01±14.8μh/ml, respectively, in comparison to 167.11±56.12μgh/ml and 87.02±30.38μgh/ml in the P-L formulation. The maximal concentrations (C_<max>) of lidocaine and prilocaine in the dermis were 29.2±9.08μg/ml and 16.54±5.31μg/ml in EMLA and 80.93±17.98μg/ml and 43.69±12.87μg/ml in the P-L formulation, respectively. This study indicates a well-calibrated microdialysis system can provide vital real-time information on percutaneous drug delivery and specifically a methylcellulose-based P-L formulation can increase percutaneous absorption of both lidocaine and prilocaine in pigs compared to carbopolbased EMLA.
2007-04-01

Percutaneous Penetration Kinetics of Lidocaine and Prilocaine in Two Local Anesthetic Formulations Assessed by in Vivo Microdialysis in Pigs(Biopharmacy)

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