摘要
目的建立测定人血浆中雷替曲塞浓度的高效液相色谱(HPLC)法,研究国产注射用雷替曲塞在中国晚期实体瘤患者体内的药动学特征。方法采用固相萃取法提取血浆样品中的雷替曲塞,进行HPLC分析。6名中国晚期实体瘤患者使用雷替曲塞单药3 mg.m-2静脉滴注,采用HPLC法测定血浆中雷替曲塞浓度的变化,采用DAS 2.0软件计算药动学参数。结果雷替曲塞在2.5～2 000μg.L-1浓度范围时线性关系良好,回归方程为Y=284.79 X+853.64,r=0.996(n=3)。雷替曲塞浓度为5、100和1 000μg.L-1的提取回收率分别为(102.7±2.6)%、(89.7±4.6)%和(99.1±7.5)%,RSD分别为1.72%、3.75%和5.28%。雷替曲塞给药剂量3 mg.m-2时,ρmax为(839.4±246.2)μg.L-1,AUC0-t为(719.8±146.7)μg.L-1.h。结论本方法操作简便、结果准确可靠、灵敏度高,重复性好,适合药动学研究。
AIM To establish a HPLC to study the pharmacokinetics of raltitrexed for method for the determination of rahitrexed in human plasma and injection in patients with advanced solid tumor. METHODS The raltitrexed in plasma were extracted by solid phase microextraction （SPME）, and then analyzed by HPLC. Six Chinese patients with advanced solid tumor received intravenously raltitrexed 3mg·m-2. The plasma concentration of rahitrexed was determined by HPLC, and the pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS The calibration curve was linear in the range of 2.5 - 2 000 μg·L-1, and the linear equation was Y = 284.79 X＋ 853.64, r = 0.996 （n = 3）. The extraction recovery of rahitrexed at the concentration of 5, 100 and 1 000 μg·L-1 were （102.7 ± 2.6） %, （89.7 ± 4.6） % and （99.1 ± 7.5） %, and the RSD were 1.72%, 3.75% and 5.28% respectively. The pharmacokinetic parameters of rahitrexed 3 mg·m-2 were as follows： pmax was （839.4 ± 246.2） μg·L-1 and AUC0-t was （719.8 ± 146.7） μg·L-1·h. CONCLUSION This HPLC method is simple, accurate, sensitive and reproducible, and suitable for the study of pharmacokinetics of rahitrexed in human plasma.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2011年第9期709-712,共4页
Chinese Journal of New Drugs and Clinical Remedies
关键词
雷替曲塞
色谱法
高压液相
药动学
rahitrexed
chromatography, high pressure liquid
pharmacokinetics
作者简介
李如标（1968-），男，江苏连云港人，副主任药师，学士，主要从事医院药学工作，Phn：86—518—8279—6735，E—mail：Lirb8@qq．com
