肿瘤患者静脉滴入卡铂的药代动力学研究

Clinical pharmacokinetic studies of intravenous drip carboplatin in patients with cancer

目的:研究国产卡铂(CBP)的临床药代动力学。方法:20例肿瘤患者静脉滴入CBP400mg,用反相高效液相色谱法测定血清CBP浓度;按WHO的标准作疗效评定。结果:用药结束时平均血药浓度(Co)为(54.79±11.81)mg/L,消除半衰期(T1/2β)为(143.12±49.41)min。有8例部分缓解(PR),12例稳定(NC)或进展(PD)。有效组(PR)和无效组(NC+PD)的Co分别为(61.03±9.28)和(52.14±12.77)mg/L,T1/2β分别为(191.27±26.92)和(119.00±35.31)min,差异有统计学意义,P<0.01。在2～10h内,有效组血清CBP浓度高于无效组,差异有统计学意义,P<0.05。结论:肿瘤患者静脉滴入CBP的血药浓度存在明显个体差异,疗效与血药浓度和消除快慢有关。

OBJECTIVE： To study the clinical pharmacokinetics of carboplatin. METHODS： Twenty patients with cancer were treated with carboplatin 400 mg in 10% glucose injection 250 mL intravenous drip for 60 minutes. Serum levels of carboplatin were determined by reversed-phase HPLC. The data were evaluated according to criteria made by WHO. RESULTS： The average serum levels of carboplatin （Co） was （54.79 ±11.81） mg/L at the end of intravenous drip. The half-live （T1/28） of carboplatin was （ 143. 12 ± 49.41 ） minutes. Eight cases （40%） were partially remitted, another 12 cases （60%） were no changes （NC） or progress of disease （PD）. The average of Co were （61.03±9.28） and （52. 14±12.77） mg/L, T1/28（191.27±26. 92） and （119.00±35.31） minutes （P〈0.01） in the effective and ineffective groups. After intravenous drip, the serum levels of carboplatin in the effective group were higher than the ineffective one from 2 to 10 hours, P〈0.05. CONCLUSIONS： The individual variation of serum levels of carboplatin is shown significantly in patients with cancer after intravenous drip. The therapeutic effect of carboplatin is related with its serum levels and parameters of elimination.