培美曲塞在肿瘤患者体内的药动学  

Pharmacokinetic study of pemetrexed in cancer patients

作　　者：孙成春[1] 王宝成[1] 柳晓泉[2] 马丕林 毕经旺[1] 曹媛[2] 曹婉雯[2] 刘欣[1] 吕伟伟[1] 

机构地区：[1]济南军区总医院,山东济南250031 [2]中国药科大学药代研究中心,江苏南京210002 [3]齐鲁制药有限公司,山东济南250100

出　　处：《中国医院药学杂志》2010年第23期1975-1979,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究培美曲塞在肿瘤患者体内的药动学特征。方法:选择符合入选条件的肿瘤患者10例,单次使用培美曲塞500mg.m-2,10min内静脉输注完成。给药后0～48h采集血样及尿样,采用液相-质谱联用法测定血浆及尿液中的培美曲塞浓度。采用BAPP2.0药动学程序计算各个成分的药动学参数。结果:培美曲塞药动学参数如下:Cmax为(100.7±38.5)mg.L-1,tmax为(0.18±0.03)h,t1/2为(1.5±0.5)h,AUC0-48为(132.2±60.9)mg.L-1.h,AUC0-∞为(132.3±60.9)mg.L-1.h。48h内尿累计排泄率为69.60%。试验期间未发现严重不良事件。结论:培美曲塞在肿瘤患者体内过程符合线性药动学特征,500mg.m-2给药是安全的。OBJECTIVE To study the pharmacokinetic character of pemetrexed in cancer patients. METHODS A single dose of 500 mg·m-2 pemetrcxed was given to 10 selected cancer patients. Their plasma and urine were collected before adrnin istration and up to 48 hours after tbe administration. The concentration of pemetrexed were delermined by high performance liquid chromatography mass spectrum（HPLC MS） and its pharmacokinetic properties was calculated by BAPP 2.0. RESULTS The main pharmacokinetic parameters were as follow： C=max （ 100. 7± 38.5 ） mg·L- 1 , tmax （0. 18± 0. 03） h, t1/2 （ 1.5 ±0.5 ） h, AUQ0- 48 （ 132. 2 ± 60. 9） mg. L-1·h, AUC0-∞ （ 132. 3± 61）. 9） mg·L^-1·h, respectively. The excretory rate of pemetrexed in 48h urine was 69. 600/00. There was no finding of severe adverse event in the experimental patients. CONCLUSION Pemetrexed in cancer patients fits the linear pharmacokinetic characteristics and is safe with the dosage 500 mg,m-2. KEY WORDS： pemetrexed; pharmaeokinetic; HPLC MS

关 键 词：培美曲塞 药动学 高效液相色谱-质谱联用 

分 类 号：R969.1[医药卫生—药理学]