联苯苄唑的正常人体药物动力学研究

 目的研究联苯苄唑的正常人体药物动力学，以对联苯苄唑的安全性作一评价。方法采用GC-MS单离子检测的方法测定联苯苄唑溶液剂和霜剂在8名正常人体的血药浓度，并用3P87软件估算了药物动力学参数。结果溶液剂和霜剂的体内过程均符合二室开放模型，t^max分别为2.91和5.61h，C^max分别为713.46和410.70ng·mL-1。霜剂吸收、分布和清除较溶液剂慢，但曲线峰下面积没有显著性差别。结论联苯苄唑是一个较安全的外用药物，建议临床上交替使用，以提高疗效。

Pharmacokinetic study ofbifonazole in human

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.