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目的:研究高剂量表阿霉素在肿瘤化疗患者体内的药物动力学过程,并初步探讨药效学特点。方法:11例肿瘤患者接受了包含 100mg·m~(-2)高剂量表阿霉素的联合化疗, HPLC法测定血药浓度; PCNONLIN程序进行药物动力学房室模型数据拟合和参数计算;血液学毒性指标作为药效学参数,进行药物动力学和药效学相关性及剂量调整因素的研究。结果:高剂量表阿霉素的消除具有典型的三室特征,患者对表阿霉素的代谢存在较大的个体差异;药效学和药物动力学参数之间未见到明显相关性,年龄与血浆清除率之间呈负相关。结论:与低剂量表阿霉素比较,未发现药物动力学参数的差异;年龄是影响清除率的一个重要因素,对高龄患者应适当减少药物剂量;应用100mg·m~(-2)表阿霉素患者的耐受性良好。
OBJECTIVE: To study the pharmacokinetics of high-dose epirubicin in patients with tumor chemotherapy and to investigate its pharmacodynamic characteristics. Methods: Eleven patients with cancer were treated with high dose epirubicin (100 mg · m -2) combined with chemotherapy. The plasma concentration was determined by HPLC. PCNONLIN program was used to conduct pharmacokinetic model fitting and parameter calculation. Hematological toxicological parameters as pharmacodynamic parameters, pharmacokinetics and pharmacodynamics related and dose adjustment factors. Results: The elimination of high-dose epirubicin had typical three-compartment characteristics. There was a large individual difference in the metabolism of epirubicin. There was no significant correlation between pharmacodynamics and pharmacokinetic parameters, Plasma clearance was negatively correlated. CONCLUSIONS: Compared with low dose epirubicin, no difference in pharmacokinetic parameters was found. Age was an important factor affecting clearance rate, and drug dose should be appropriately reduced in elderly patients. The application of 100 mg · m -2 Tolerance of patients with good toxin.