中国临床药学杂志

目的建立肿瘤患者紫杉醇给药后血浆药物浓度的测定方法,并研究患者个体内CYP3A酶活性与紫杉醇血药浓度之间的相关性。方法采用HPLC法,分别测定20例肿瘤患者血浆紫杉醇浓度及尿液CYP3A酶活性,采用两变量Bivarite法进行相关性分析。结果紫杉醇个体血药浓度范围为0.2～5.83mg·mL-1,相差近30倍;紫杉醇血药浓度与CYP3A酶活性常用对数(lgCYP3A酶活性)线性相关,r=0.9381。结论紫杉醇血药浓度个体差异大,临床有必要进行血药浓度监测;通过测定CYP3A酶活性制定紫杉醇给药方案是可行的。

AIM To establish a method for the determination of paclitaxel in tumor patient's plasma and to investigate the correlation between drug concentration and CYP3A activity.METHODS The concentration of paclitaxel in plasma and hydrocortisone,6β-hydroxycortisol in urine were determined by HPLC,respectively.The urinary ratio of 6β-hydroxycortisol/hydrocortisone had been used as a noninvasive scale for human CYP3A activity.The concentration of paclitaxel was assessed with CYP3A activity to do correlative analysis.RESULTS Concentration of paclitaxel in plasma varied from 0.2 to 5.83 mg·L-1,which showed a good correlation with lgCA,r=0.938 1.CONCLUSION It is necessary to monitor the concentration of paclitaxel in tumor patients and it is feasible to determine the paclitaxel therapeutic schedule through detection of CYP3A.