Study on the Multi-Component Skin Pharmacokinetics of Crossbow Microemulsion after Transdermal Administration Based on Microdialysis Combined with UPLC

  OBJECTIVE  To investigate the pharmacokinetic characteristics of crossbow microemulsion in rabbit skin.

  METHODS  The concentrations of chlorogenic acid, benzoyl new aconitine, periplocin and new aconitine were determined by UPLC. The effects of temperature, perfusion speed and mass concentration on the recovery rate of the probe were investigated by incremental and decrement methods, the changes of multi-component content in the dialysate at different time points after transdermal administration of crossbow microemulsion were determined by UPLC, and DAS 2.0 software was used to process the data.

  RESULTS  The recovery rate of the probe increased with increasing temperature, and the higher the flow rate, the lower the recovery rate. The pharmacokinetic parameters of chlorogenic acid, benzoyl new aconitine, periplocin and new aconitine in microemulsion C_max were (3.24±0.39) (1.04±0.29) (4.78 ± 2.15) (2.86 ± 0.55) μg·mL^-1, respectively, and in AUC_0-∞ were (52.42 ± 30.84) (7.70 ± 3.73) (42.23 ± 13.93) (22.68 ± 12.51) h·mg·mL^-1, respectively.

  CONCLUSION  A real-time in vivo microdialysis sampling technique was first used and a UPLC detection technique was established to study the skin pharmacokinetics of multi-components of crossbow microemulsion after transdermal administration, which provides a reference for the follow-up investigation and application of crossbow microemulsion.