Delay of metabolism rate of ciclosporin by simvastatin in 7 Chinese healthy men.

AIM: To study the effects of simvastatin (Sim) on pharmacokinetics of ciclosporin (Cic). METHODS: Seven healthy young volunteers took Cic 100 mg alone or in combination with Sim 10 mg in a randomized crossover study. The Cic concentrations in blood were determined by specific fluorescence polarization immunoassay. Data were analyzed with 3P87 program. RESULTS: The blood concentration-time curve was fitted to open 2-compartment model, and the pharmacokinetic parameters of Cic alone and Cic + Sim were: Cmax (646 +/- 94) and (698 +/- 340) micrograms.L-1; Tmax (1.12 +/- 0.13) and (1.13 +/- 0.21) h; AUC (2.3 +/- 0.4) and (2.6 +/- 1.2) mg.h.L-1; T1/2 beta (12 +/- 6) and (23 +/- 8) h (P < 0.05). CONCLUSION: Sim delays the metabolism rate of Cic when they are given simutaneously.