Pharmacokinetic study of bifonazole in human / 中国药学杂志

ABSTRACT

OBJECTIVE　To study the pharmacokinetics of bifonazole in healthy human,in order to evaluate the safety of bifonazole.METHODS　8 healthy volunteers were given single dose of 300 mg bifonazole solution and cream preparation respectively in a cross-over design.Blood samples were collected at the designed time,and the concentrations of bifonazole in plasma were determined by means of GC-MS(SIM) quantitative method.The pharmacokinetic parameters were calculated with the 3P87 software.RESULTS　The plasma concentration-time curves of the two preparations were fitted to two-compartment open model.The tmax of the solution and cream preparations were 2.91 h and 5.62 h,cmax 713.46 ng.mL-1 and 410.70 ng*mL-1,respectively.The cream preparations absorption,distribution and clearance was a little slower than that of the solution preparation.However,no significant difference in their AUC.CONCLUSION　Bifonazole is a safe drug,and clinical use of the solution and cream preparation in turn is suggested to improve its therapeutic efficacy.