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目的研究利培酮(risperdal)及其活性代谢产物9-羟基利培酮(9-OH-risperdal)在中国女性精神分裂症患者的临床药动学。方法单周期实验,20例女性患者经过17d的利培酮治疗,收集系列标本,高效液相色谱-质谱联用(HPLC-MS)测定血浆中的药物浓度。结果利培酮吸收迅速,其tmax和t1/2分别为1.6和3.3h。9-羟利培酮的tmax和t1/2分别为2.6和25.1h。利培酮和9-羟基利培酮的ρassv分别为30.5和136.8μg.L-1,AUC0ss-12分别为482.4和1744.3μg.h.L-1。利培酮的CL/F和V/F分别为8.4L.h-1和33.2L。结论利培酮和9-羟基利培酮的血药浓度,尤其是利培酮,存在着巨大的个体差异。结果表明,治疗药物浓度监测对维思通的合理用药有重要意义。
Objective To study the clinical pharmacokinetics of risperdal and its active metabolite 9-OH-risperdal in Chinese women with schizophrenia. Methods In a single-cycle experiment, 20 female patients were treated with risperidone for 17 days. Serial samples were collected and their plasma concentrations were determined by high performance liquid chromatography-mass spectrometry (HPLC-MS). The results of risperidone absorption rapidly, the tmax and t1 / 2 were 1.6 and 3.3h. The tmax and t1 / 2 for 9-hydroxy-risperidone were 2.6 and 25.1 h, respectively. The ρassv of risperidone and 9-hydroxyrisperidone were 30.5 and 136.8 μg.L-1, respectively, and AUC0ss-12 was 482.4 and 1744.3 μg.h.L-1, respectively. Risperidone had CL / F and V / F of 8.4 L · h -1 and 33.2 L, respectively. Conclusions There is a huge individual difference in the plasma concentrations of risperidone and 9-hydroxyrisperidone, especially risperidone. The results show that the therapeutic drug concentration monitoring VST on the rational use of drugs is important.