利培酮与9-羟利培酮对精神分裂症患者血药浓度与剂量的关系

The relationship between dose of risperidone and the steady plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients

目的:探讨口服利培酮的精神分裂症患者利培酮、9羟利培酮血药浓度、利培酮与9羟利培酮血药浓度之和及比值与剂量的关系。方法:采用液质联用法测定利培酮和9羟利培酮血药浓度;计算利培酮、9羟利培酮血药浓度及两者之和与剂量的相关系数。结果:利培酮、9羟利培酮及两者之和与剂量相关系数分别0.7668,0.9800和0.9798。36.6%患者9羟利培酮血药浓度高于利培酮。结论:9羟利培酮血药浓度及两者之和比利培酮血药浓度与剂量有更好相关性,9羟利培酮在精神分裂症治疗中有重要作用。

To evaluate the relationship between dose of risperidone and the steady plasma concentration of risperidone and 9-hydroxyrisperidone in schizophrenic patients. METHODS The steady plasma concentrations of risperidone and 9-hydroxyrisperidone were determined by HPLC-MS method and the relationship between total plasma concentration of risperidone and 9-hydroxyrisperidone and doses are evaluated.RESULTS The steady plasma concentration of RSP had a relationship sith administered daily oral dose, r = 0. 766 8. A much better relationship existed between dialy dose of risperidone and the steady plasma concentration 9-hydroxyrisperidone （r =0. 9800）or the total active moiety, risperidone plus 9-hydroxyrisperidone concentrations （r =0. 979 8）. CONCLUSION The steady plasma concentrations of 9-hydroxyrisperidone or risperidone plus 9-hydroxyrisperidone were more related to the dialy dose of risperidone than that of risperidone.9-hydroxyrisperidone has an important role in risperidone clinical application.