奥丹西酮在原发性肝癌患者的药物动力学

目的 观察奥丹西酮在原发性肝癌患者体内的药物动力学特性。方法 8 名接受顺铂+5-氟尿嘧啶化疗的原发性肝癌患者单次和多次口服16mg 奥丹西酮后, 应用反相高效液相色谱法测定血浆药物浓度, 并用PKBP-N₁程序在计算机上拟合。结果 奥丹西酮表现为二房室模型, 其单剂量和多剂量口服主要药动学参数分别为:T_1/2β为4.3±0.5h 和5.7±0.7h (P<0.01), C_max 为42.6±3.8μg/L 和49.2±2.3μg/L(P<0.05), T_max为1.8±0.2h 和1.8±0.1h, AUC_0~∞为643.2±84.7μg/h·L 和833.4±96.7μg/L·h (P<0.01)。结论 原发性肝癌患者多次口服奥丹西酮后与单次口服相比, 体内有蓄积现象, 消除能力下降, 生物利用度升高。

Pharmacokinetics of ondansetron in primary carcinoma of the liver

Aim To study the pharmacokingtics character of ondansetron in patients with primary carcinoma of liver.Methods Ondansetron was given po both in a single dose of 16 mg and in multiple doses of 16mg each and its concent ration in plasma was determined by reve rsed-phase high performance liquid chromatography.The concent ration data were fitted with a PKBP-N₁ program on computer.Results The concent ration-time curve was described by a two-compartment open model with T_1/2ka=0.8±0.1h and 0.7±0.1h, T_1/2α=1.9±0.4h and 1.8±0.3h, T_1/2β=4.3±0.5h and 5.7±0.7h, C_max=42.6±3.8μg/L and 49.2±2.3 μg/L, T_max = 1.8±0.2h and 1.8±0.1h, AUC_0~∞=643±85 μg/h·L and 833±97 μg/h·L, respectively.Conclusion Ondansetron was absorbed repidly, and also eliminated at a fairly rapid rate.It could be stored up in the patients contrating primary carcinoma of liver when ondansetron is admani steaed in multiple doses.