论文部分内容阅读
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。
Objective To establish a high performance liquid chromatography (HPLC) method for the determination of raltitrexed in human plasma and study the pharmacokinetics of domestic raltitrexed in patients with advanced solid tumors in China. Methods Raltitrexed in plasma samples were extracted by solid-phase extraction and analyzed by HPLC. Six Chinese patients with advanced solid tumors were treated with 3 mg.m-2 of raltitrex alone, and the plasma concentration of raltitrexed was determined by HPLC. The pharmacokinetic parameters were calculated by DAS 2.0 software. Results The calibration curve of raltitrexed was linear in the range of 2.5-2 000 μg.L-1. The regression equation was Y = 284.79 X + 853.64, r = 0.996 (n = 3). The recoveries were (102.7 ± 2.6)%, (89.7 ± 4.6)% and (99.1 ± 7.5)% for Raltitrexed at concentrations of 5,100 and 1 000 μg, respectively, with RSDs of 1.72% and 3.75, respectively % And 5.28%. The ρmax was (839.4 ± 246.2) μg.L-1 and the AUC0-t was (719.8 ± 146.7) μg.L-1.h with raltitrexed at a dose of 3 mg.m-2 Conclusion The method is simple, accurate, reliable, sensitive and reproducible. It is suitable for pharmacokinetic studies.