厄洛替尼在大鼠脑脊液和血浆中浓度与其疗效的相关性研究  

Concentration of Erlotinib in Rat Cerebrospinal Fluid and Plasma and its Correlation with Efficacy

作　　者：李晓琴[1] 王秀丽[1] 朱红革[1] 展翼翼 刘春玲[1] 

机构地区：[1]新疆医科大学附属肿瘤医院,830011

出　　处：《实用癌症杂志》2016年第3期353-355,共3页The Practical Journal of Cancer

基　　金：新疆医科大学创新基金课题(编号:XJC201282);吴阶平医学基金会临床科研专项资助基金(编号:320.6750.13136)

摘　　要：目的检测厄洛替尼在大鼠脑脊液和血浆中的浓度,并对其与NSCLC患者疗效间的相关性进行分析。方法随机选取40只健康大鼠,雌雄各半。实验前1日禁食12 h,实验当日分别按照10 mg/kg的剂量注入大鼠尾静脉。另外选取2011年1月至2014年12年收治的110例NSCLC患者作为研究对象,对其临床资料进行回顾性分析。对比大鼠1、4、12、24 h的脑脊液和血浆中厄洛替尼浓度水平,并对两者间相关性进行分析;参照评价标准将110例NSCLC患者分为CR组、PR组、SD组及PD组,对比不同组间的血浆厄洛替尼浓度,并对临床疗效与血浆厄洛替尼浓度的相关性进行分析。结果大鼠1、4、12、24 h脑脊液和血浆中的厄洛替尼浓度水平存在显著性差异,随着时间的推移,其在脑脊液和血浆中的浓度逐渐降低(P<0.05)。不同时刻的大鼠脑脊液与血浆中的厄洛替尼浓度间均呈显著正相关(P<0.05)。不同疗效患者组间血浆中厄洛替尼浓度存在显著性差异(P<0.05),组间多重比较结果显示不同组间血浆浓度由高至低依次为CR组>PR组>SD组>PD组(P<0.05)。结论厄洛替尼在大鼠脑脊液和血浆中的浓度呈显著正相关,且患者疗效与其血浆中药物浓度具有相关性,血浆浓度越高,疗效越好,故厄洛替尼在治疗非小细胞肺癌脑转移中具有重要的临床意义,可作为放疗等治疗手段的有力补充。Objective To detect the concentration of Erlotinib in rat cerebrospinal fluid and plasma and its correlation with efficacy. Methods 40 healthy rats were selected, half male and half female rats. Before testing, the rats took absolute diet for 12 h. 10 mg/kg of Erlotinib were separately injected into the tail vein of rats. The clinical data of 110 NSCLC patients were reviewed. The concentration levels of Erlotinib in cerebrospinal fluid and plasma in 1 h ,4 h, 12 and 24 h were compared and their correlations were analyzed ;according to evaluation criterion, 110 NSCLC patients were divided into CR group ,PR group, SD group and PD group. The concentration of Edotinib of the 3 groups were compared. The correlation of clinical effects with the concentration of Erlotinib in plasma was analyzed. Results The concentration levels of Erlotinib in cerebrospinal fluid and plasma in 1 h, 4 h, 12 h and 24 h were significantly different. As time passed, the concentration levels of Erlotinib in eerebrospinal fluid and plasma was gradually reduced （P 〈 0.05 ） ;at different moments, the concentration levels of Erlotinib in cerebrospinal fluid and plasma had a significant positive correlation （P 〈 0.05 ） ;the concentration levels of Erlotinib in plasma was significantly different（ P 〈 0.05 ） ; based on the muhiple comparisons, the plasma concentration was arranged from high to low ： CR group 〉 PR group 〉 SD group 〉 PD group （ P 〈 0.05 ）. Conclusion The concentration levels of Erlotinib in eerebrospinal fluid and plasma have a significant positive relationship while the clinical efficacy is correlated with the concentration of Erlotinib in plasma. The higher concentration is, the better the clinical efficacy is. Erlotinib has an important clinical significance in the treatment of NSCLC metastasis and can be supplementary to radiation treatment and others.

关 键 词：厄洛替尼 脑脊液 血浆 疗效 相关性 

分 类 号：R734.2[医药卫生—肿瘤]