甲磺酸桂哌齐特注射液在健康志愿者中的药动学研究  

Pharmacokinetics of cinepazide mesylate injection in healthy volunteers

作　　者：罗芳梅[1] 何周康[1] 王婷[1] 王方杰[1] 田娟[2] 丁劲松[2] 

机构地区：[1]湖南省儿童医院药学部,长沙410007 [2]中南大学湘雅药学院,长沙410013

出　　处：《中南药学》2017年第2期178-182,共5页Central South Pharmacy

摘　　要：目的研究甲磺酸桂哌齐特注射液在健康志愿者中单次给药的药动学特征。方法 12名健康志愿者分别静脉滴注甲磺酸桂哌齐特62.5、125、250和375 mg,血浆及尿液中桂哌齐特浓度以新建立的HPLC-UV法测定。结果 62.5、125、250和375 mg剂量组的主要药动学参数分别为:Cmax(1.148±0.149)、(2.614±0.410)、(5.625±0.940)、(8.887±1.197)μg·m L^(-1);AUC0~14(3.625±0.549)、(8.553±1.733)、(19.849±3.346)、(33.925±5.377)μg·h·m L^(-1);t1/2Z(2.49±1.14)、(2.39±0.41)、(2.43±0.51)、(2.22±0.27)h;24 h内桂哌齐特尿累积排泄率分别为(54.15±4.24)%、(56.09±5.90)%、(55.32±5.02)%和(56.15±5.32)%。结论甲磺酸桂哌齐特在62.5~375 mg内单次给药符合线性动力学过程,24 h内约有55%以原型经肾脏排除。Objective To determine the pharmacokinetic characteristics of cinepazide mesylate injection in healthy volunteers. Methods Twelve healthy volunteers were intravenous drip of cinepazide mesylate at 62.5, 125,250 and 375 mg. Cinepazide in the blood and urine samples was determined by HPLC-UV. Results At 62.5, 125, 250 and 375 mg, the main pharmacokinetic parameters of cinepazide were as follows： C was （1.148±0.149）, （2.614±0.410）, （5.625±0.940）, and （8.887±1.197） μg·mL^ -1; AUCo ,4was （3.625±0.549）, （8.553±1.733）, （19.849±3.346）, and （33.925±5.377） μg · h · mL ^-1; tlmzwas （2.49± 1.14）, （2.39±0.41）, （2.43 ±0.51）, and （2.22± 0.27） h. The cumulation excretory rate of cinepazide in the urine at 24 h was （54.15± 4.24）%, （56.09± 5.90）%, （55.32 ±5.02）%, and （56.15 ± 5.32）%. Conclution At the single dose range 62.5 -- 375 mg, the process of cinepazide conforms with the linear pharmacokinetic characteristics. The cumu- lative excretion rate of cinepazide in 24 h is about 55%.

关 键 词：甲磺酸桂哌齐特 药动学 HPLC-UV 

分 类 号：R96[医药卫生—药理学]