帕利哌酮缓释片治疗精神分裂症患者有效血药浓度的研究

Effective blood drug level of paliperidone extended release tablets for treating patients with schizophrenia

目的：探究帕利哌酮缓释片治疗精神分裂症的有效血药浓度,并观察其临床疗效和不良反应。方法：采用单臂、开放、前瞻性研究。共纳入32例精神分裂症患者,单用帕利哌酮缓释片治疗,观察期8周,完成30例。通过PANSS量表评价疗效;安全性评估包括体格检查、实验室检查指标、心电图及不良反应记录表。采用HPLC-MS方法测定治疗1周末、2周末、4周末及8周末帕利哌酮的血药浓度。结果：治疗有效率达76.67%（23/30）。治疗有效患者的帕利哌酮治疗剂量为（9.52±2.15）mg·d-1,平均有效血药浓度为（49.14±26.38）ng·m L-1,有效血药浓度范围为13.5-93.7 ng·m L-1,治疗剂量与有效血药浓度存在正相关（r=0.396,P〈0.05）。主要不良反应为锥体外系反应和高催乳素血症。结论：帕利哌酮缓释片治疗精神分裂症疗效好,安全性高,有效血药浓度范围为13.5-93.7 ng·m L-1。

Objective： To explore the effective blood drug level of paliperidone extended release tablets for treating patients with schizophrenia,and observe its clinical effectiveness and side effects. Methods： This was a one-arm,open and prospective study. Totally 32 schizophrenic patients were enrolled in the study and treated with paliperidone. Of them 30 completed the whole 8-week observation period. The PANSS was used to evaluate effectiveness. The results of a physical examination,lab tests,electrocardiogram and adverse events scale were used to evaluate safety. The blood drug level of paliperidone extended release tablets was detected by HPLC at the weekends of 1,2,4,8 weeks after the treatment. Results： The effective rate of paliperidone extended release tablets was 76. 67%（ 23 /30）. The dosage of paliperidone extended release tablets was（ 9. 52 ± 2. 15） mg·d- 1in those effective patients. The mean effective blood drug level was（ 49. 14 ± 26. 38） ng·m L- 1. The range of its effective blood drug level was（ 13. 5 - 93. 7） ng·m L- 1. There was a positive correlation between its dose and effective blood level（ r = 0. 396,P〈 0. 05）. The main side effects were extrapyramidal syndrome and higher serum prolactin.Conclusion： Paliperidone extended release tablets are an effective and high safety antipsychotic for schizophrenic patients,and the range of its effective blood drug level is（ 13. 5 - 93. 7） ng·m L- 1.