梓醇冻干粉针在大鼠体内的药动学研究  

Pharmacokinetics of lyophilized catalpol powder in rats

作　　者：何瑶[1] 薛强[2] 陈红[3] 徐晓玉[4] HE Yao XUE Qiang CHEN Hong XU Xiao-yu(Department of Pharmacy, Chongqing Emergency Medical Center, Chongqing 400014, China College of Pharmacy ＆ College of Tranditional Chinese Medicine, Chongqing Medical and Pharmaceutical College, Chongqing 401331, China Department of Pharmacy, Southwest Hospital, Chongqing 400038, China College of Pharmaceutical Sciences ＆ College of Chinese Medicine, Southwest University, Chongqing 400716, China)

机构地区：[1]重庆市急救医疗中心药剂科,重庆400014 [2]重庆医药高等专科学校药学院&中药学院,重庆401331 [3]第三军医大学附属西南医院药剂科,重庆400038 [4]西南大学药学院,重庆400716

出　　处：《中国新药杂志》2017年第15期1773-1777,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项资助项目(2014ZX09304-306-04);国家自然科学基金资助项目(81473549);重庆医药高等专科学校人才引进科研启动项目(2016304)

摘　　要：目的:建立大鼠血浆中梓醇的含量测定方法,研究梓醇冻干粉针在大鼠体内的药动学。方法:按5.0 mg·kg^(-1)给大鼠尾静脉注射1.0 mg·m L-1梓醇冻干粉针生理盐水和梓醇生理盐水,定时取血,测定血浆中的梓醇含量,DAS 2.1药动学软件计算药动学参数。结果:静脉注射梓醇冻干粉针后,药动学符合二室模型,分布半衰期(t1/2α)为(30.52±5.81)min、消除半衰期(t1/2β)为(182.25±36.32)min、中央室表观分布容积(Vc)为(0.191 9±0.016 2)L·kg^(-1)、清除率(CL)为(0.001 5±0.000 1)kg·L·min-1、药时曲线下面积(AUC)为(3 451.66±210.41)mg·min·m L-1;其药动学参数与梓醇生理盐水组相比无统计学差异。结论:静脉注射梓醇冻干粉针在大鼠体内的吸收和消除呈一级动力学特征,且冻干粉针剂制剂并未改变梓醇在大鼠体内的药动学行为。Objective： To develop an HPLC method for the determination of catalpol in rat plasma,and determine the pharmacokinetics of lyophilized catalpol powder. Methods： Catalpol and its lyophilized powder（ 5. 0mg·kg^（-1）） were injected through tail vein. The content of catalpol in plasma was measured by HPLC at 1,5,15,30,45,90,120,240,420,and 600 min after administration,respectively. Then,the pharmacokinetic parameters of catalpol were calculated by DAS 2. 1 pharmacokinetic software. Results： After administration with lyophilized catalpol powder,the pharmacokinetics of catalpol was in accordance with two compartment model. The main pharmacokinetic parameters of lyophilized powder of catalpol are as follows： the t1/2α was（ 30. 52 ± 5. 81） min,t1/2β was（ 182. 25 ± 36. 32） min,Vcwas（ 0. 191 9 ± 0. 016 2） L·kg^（-1）,CL was（ 0. 001 5 ± 0. 000 1） kg·L·min-1,and AUC was（ 3 451. 66 ± 210. 41） mg·min·m L-1,respectively. There were no significant differences between the parameters of the two preparations. Conclusion： After intravenous injection,the absorption and elimination of catalpol were in accordance with the feature of first order kinetics process. In addition,the pharmacokinetic featureof catalpol does not change in lyophilized catalpol powder.

关 键 词：梓醇冻干粉针 药动学 大鼠 

分 类 号：R932[医药卫生—生药学] R965[医药卫生—药学]