MTX药代动力学以及组织与全血浓度相关性研究

目的 研究MTX药代动力学以及组织与全血药物浓度相关性。方法 用30mg/m²MTX的给药剂量,在肿瘤病人体内研究其药代动力学过程,并对肿瘤局部血及外周血中的药物浓度进行了相关性比较,同时对该剂量下的药品不良反应作了观察。结果 用同 30mg/m²剂量MTX静脉滴注后,肿瘤病人体内药代动力学为一级动力学三房室模型。肿瘤局部与外周血药浓度有显著相关性。应用本剂量药品不良反应发生率较低。结论 治疗药物浓度监测可为临床治疗捉供客观有效的数据,有指导意义,使用30 mg/m²剂量为一安全有效的治疗剂量。

Study of MTX pharmacokinetics and relationship between local and systemic drug concentration in patients

Aim Pharmcokinetic action of MTX and the relationship of drug concentration in cancers with that in the systemic blood were studied. Methods MTX in a dose of 30 mg/m² was given to 31 cancer patients. Samples of systemic blood were taken at 1h, 3h, 6h, 12h, 24h, 30h, and 48h after drug administration. The same dosage of MTX was given to 30 patients with mammary cancer 3 hours before operation and blood samples from the organ where the cancer was located and from peripheral veins were taken during operation. The drug concentration in each kind of samples was detected and analysed. Results The plasma concentration vs time date were better described by an open three compartment model. In patients with 30 mg/m²,local and systemic drug concentrations were in high relationship, and adverse drug reactions were smaller than that of other dose. Conclusion The 30mg/m2 dose of MTX was a safe therapeutic dose.