【摘要】 目的比较重酒石酸长春瑞滨注射用乳剂与市售注射液在肿瘤患者的药动学。方法在符合入选标准的肿瘤患者中,采用随机平行对照单次给药的方法进行药动学试验,给药剂量30 mg·m-2,采用LC-MS/MS法测定血浆样品中长春瑞滨的浓度,计算主要药动学参数并进行统计分析。结果重酒石酸长春瑞滨注射用乳剂和市售注射液在肿瘤患者中的主要药动学参数分别为:t1/2(16.78±5.24)和(20.03±24.72)h,CL(22.75±5.81)和(17.71±2.88)L·h-1·m-2,Vc(541.04±223.36)和(486.03±567.17)L·m-2,AUC0-t(1 297.09±308.73)和(1 629.31±309.41)μg·L-1·h,AUC0-∞(1 388.37±318.54)和(1 736.23±299.83)μg·L-1·h,ρmax(1 426.25±397.56)和(2 187.50±828.04)μg·L-1,tmax(0.22±0.04)和(0.29±0.18)h,MRT0-t(6.95±1.08)和(4.94±1.31)h;两制剂AUC0-t、t1/2、tmax、ρmax和Vc均无显著差异(P>0.05)。结论重酒石酸长春瑞滨注射用乳剂和市售注射液相比,在肿瘤患者中具有相似的药动学特征。更多还原

【Abstract】 AIM To study the pharmacokinetics of vinorelbine bitartrate injectable emulsion comparing with the commercial vinorelbine injectable solution in tumor patients. METHODS A single dose randomized parallel pharmacokinetic study was carried out in selected tumor patients, and the dose was 30 mg·m-2 for each patient. The plasma concentration of vinorelbine was determined by LC- MS/MS method. Main pharmacokinetic parameters were calculated and statistically analysed. RESULTS The main pharmacokinetic parameters of vinorelbine bitartrate injectable emulsion and the commercial vinorelbine injectable solution in tumor patients were as follows: t1/2(16.78 ± 5.24) and(20.03 ± 24.72) h, CL(22.75 ± 5.81) and (17.71 ± 2.88) L·h-1·m-2,Vc( 541.04 ± 223.36) and ( 486.03 ± 567.17) L·m-2; AUC0-t( 1 297.09 ± 308.73) and ( 1 629.31 ±309.41) μg·L-1·h; AUC0-∞(1 388.37 ± 318.54) and (1 736.23 ± 299.83) μg·L-1·h; ρmax(1 426.25 ±397.56) and (2 187.50 ± 828.04) μg·L-1; tmax(0.22 ± 0.04) and (0.29 ± 0.18) h; MRT0-t(6.95 ± 1.08) and (4.94 ± 1.31) h. AUC0-t, t1/2, tmax, ρmaxand Vcshown no significant difference between the two preparations.CONCLUSION The vinorelbine bitartrate injectable emulsion has a similar pharmacokinetic profile to the commercial vinorelbine injectable solution in tumor patients.更多还原