甲磺酸加替沙星与加替沙星的药物代谢动力学比较

目的甲磺酸加替沙星(GATM)和加替沙星(GAT)是喹诺酮类抗感染药物的新型制剂,对改变酸根的甲磺酸加替沙星在大鼠体内的药物代谢动力学规律和特点进行了考察并和加替沙星进行比较。方法以SD大鼠为研究对象,单剂量口服等克分子剂量(0.0497 mmol.kg-1)GATM和GAT后,采用高效液相色谱法(HPLC)检测血清中GAT的含量,采用3p97程序软件计算二者在大鼠体内的药代动力学参数。结果大鼠单次口服GATM(23.43 mg.kg-1)和GAT(20 mg.kg-1)后,二者的血药浓度经时变化符合一级消除动力学特征,药时曲线拟合为二房室模型,其中GATM的药代动力学参数为:血浆消除半衰期(T12β)9.13 h,药时曲线下面积(AUC)15.05 mg.L-1.h,血药峰浓度(Cm ax)4.41mg.L-1,达峰时间(Tm ax)0.5 h;而GAT的药代参数分别为:T12β10.70 h,AUC 13.84 mg.L-1.h,Cm ax4.25 mg.L-1,Tm ax0.5 h。结论在上述剂量条件下GATM与GAT的吸收(Tm ax、Cm ax、AUC)、分布(V/F)和消除(T12β、CL)参数差异未见显著性,二者的血药浓度经时变化相似,药代动力学规律基本一致。

Pharmacokinetics of gatifloxacin mesylate and gatifloxacin in rats in vivo

Aim To investigate the difference in pharmacokinetics between gatifloxacin mesylate(GATM) and gatifloxacin(GAT) in SD rats in vivo.Method The plasma concentration-time courses of GAT in rats were measured by HPLC method after a single oral dose of GATM and GAT,and the pharmacokinetic parameters were estimated by program 3p97 software.Results The results shown that both of GATM and GAT plasma concentration-time courses were best fitted to two-compartment models after a single oral dose(GATM 23.43 mg·kg~(-1)and GAT 20 mg·kg~(-1),respectively).The major average pharmacokinetic parameters of GATM were as follwing: T_(2)β: 9.13 h,AUC: 15.05 mg·L~(-1)·h,C_(max): 4.41 mg·L~(-1),and T_(max): 0.5 h,respectively.On the other hand,the pharmacokinetic parameters of GAT were as follwing: T_(2)β:10.70 h,AUC:13.84 mg·L~(-1)·h,C_(max):4.25 mg·L~(-1),T_(max):0.5 h,respectively.Conclusion Under the equi-mole dose condition treated as above,both of pharmacokinetic characters between GATM and GAT were not significantly differences in rats