伏立康唑磺丁基醚-β-环糊精包合物体内药动学的对比研究

Comparison of pharmacokinetics of voriconazole sulfobutyl ether-β-cyclodextrin inclusion complex

目的:自制伏立康唑磺丁基醚-β-环糊精包合物与注射用伏立康唑(VFEND~)大鼠体内药动学对比研究。方法:以VFEND~为对照,Wistar大鼠为受试动物,采用超高效液相-飞行时间质谱(U-HPLC/Q-TOF-MS)监测伏立康唑的血药浓度,计算药动学参数,对自制药与对照药的各药动参数进行独立样本双侧t检验。结果:自制药和对照药大鼠体内伏立康唑的消除半衰期(t1/2)分别为(2.099±0.202)h和(2.142±0.163)h,药物浓度-时间曲线下面积(AUC0-12)分别为(23.247±1.264)μg·h·mL^(-1)和(22.748±1.568)μg·h·mL^(-1)。结论:自制药与对照药的大鼠体内药动学行为相似,各药动学参数相近。

OBJECrIVE To study the pharmacokinetics of voriconazole sulfobutyl ether-β-cyclodextrin inclusion complex, self-developed and VFEND in rats. 1VIETHODS Using VFEND as control group, Wistar rats as animal subjects, concentra- tion of voriconazole was detected by U-HPLC/Q-TOF-MS. The pharmacokinetic parameters were calculated and conducted through independent sample t test. RESULTS Elimination half-life and area under the drug concentration-time curves of vori- conazole sulfobutyl ether-β-cyclodextrin inclusion complex self developed and in market were （2. 099 ± 0. 202） and （2. 142±0. 163） h, （23. 247 ± 1. 264） and （22. 748 ± 1. 568） μg.h.mL-1. CONCLUSION Pharmacokinetics and parameters of voricon- azole sulfobutvl ether-β-cyclodextrin inclusion complex in market and self developed are similar in vivo.