Influence of probenecid on pharmacokinetics of cefaclor / 中国临床药理学与治疗学

ABSTRACT

AIM: To observe the effects of proben-ecid of different doses on pharmacokinetics of cefaclor and to provide the basis of their co-adiministration. METHODS: 30 rabbits were randomly divided into 5 groups: Cef 50 mg?kg -1, Cef 50 mg?kg -1+Pro 50 mg?kg -1,Cef 50 mg?kg -1+Pro 100 mg?kg -1,Cef 50 mg?kg -1+Pro 200 mg?kg -1,Cef 25 mg?kg -1+Pro 100 mg?kg -1. The blood samples were drawn from thigh vein after IG and the concentrations of cefaclor were determined by HPLC. Pharmacokinetics parameters were calculated by NDST procedure. RESULTS: In groups with Cef 50 mg?kg -1, C max and AUC of cefaclor increased, and Vd/F and Cl/F decreased progressively with the adding probenecid. There was no significant difference between Cef 25 mg+Pro 100 mg and Cef 50 mg?kg -1 in each parameter except Cl/F. CONCLUSION: Probenecid can remarkably alter the pharmacokinetics of cefaclor and the magnitude of the effects of probenecid is dependent on its dose in this trial. Cef 25 mg?kg -1 with Pro 100 mg?kg -1 can reach the same blood concentration as Cef 50 mg?kg -1 alone.