Abstract: AIM: To study the pharmacokinetics of cyclosporin A (CsA) with or without combination of berberine chloride (Ber) in healthy volunteers. METHODS: After taking CsA of a single dosage of 6 mg·kg ^-1, 6 healthy male volunteers were administrated with Ber at 300 mg twice daily for 13 days and on day 15 took CsA of a single dosage at 6 mg·kg ^-1 again.The blood concentrations of CsA before and after coadministration with Ber were determined by fluorescence polarization immunoassay (FPIA) and the pharmacokinetic parameters were calculated by 3p87 program. RESULTS: The main pharmacokinetic parameters of CsA before and after coadministration of Ber were as follow:K a were 0.913 ±0.30 h ^-1 and 1.092 ±0.348 h ^-1;T1 2β were 6.18 ±0.94 h and 6.86 ±1.27 h;AUC_{0 -24} were 11.0 ±1.6mg·h·L ^-1 and 10.6 ±1.6 mg·h ^-1 ·L ^-1;CL(s) were 34.3 ±6.7 L· h ^-1 and 36.6 ±9.3 L·h ^-1;C_max were 1.8 ±0.4 mg· L ^-1 and 1.9 ±0.4 mg·L ^-1, respectively.Both values of T_peak were 1.5 ±0.55 h; CONCLUSION: The pharmacokinetic parameters of CsA before and after coadministration with Ber have no significant differences in healthy volunteers.Therefore, the action site of Ber influencing CsA is supposed to lie in intestines.

Key words: pharmacology, cyclosporin A, berberine chloride, pharmacokinetics, healthy volunteers