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目的研究帕利哌酮棕榈酸盐在精神分裂症患者中多次给药的血浆药物浓度水平及其与治疗安全性的关系。方法 18名符合DSM-IV精神分裂症诊断患者经过第1,8,38 d的固定剂量注射后,每30 d进行一次剂量可变的药物注射,按照最后3针实际给予的药物剂量分组。于试验第8,11,14,17,21,28,38,68,98,128,158,188 d采血,高效液相色谱法测定血浆中帕利哌酮浓度,临床症状在试验第1 d和188 d用PANSS评分,安全性则通过不良事件监测、生命体征监测、实验室检查以及锥体外系反应量表评估,用SPSS软件分析数据。结果17名最终完成试验的患者分为75 mg eq.(n=5)、100 mg eq.(n=9)、150 mgeq.(n=3)3组,各组的稳态血药浓度为(23.42±11.95),(24.52±12.44),(16.92±6.53)ng.mL-1,注射后的峰浓度出现在第11～18 d,平均为17 d。11例患者共出现17例次不良事件,程度均为轻中度。结论给药后,帕利哌酮棕榈酸盐各剂量组间稳态浓度无差异,但个体差异明显。药物剂量与不良反应间未见关联。
Objective To investigate the plasma drug concentration levels of paliperidone palmitate administered multiple times in schizophrenia patients and its relationship with the safety of treatment. Methods A total of 18 DSM-IV patients diagnosed with schizophrenia were given a fixed dose injection every 1, 8, and 38 days after the first dose. The patients were divided into three groups according to the dose of the last 3 doses. Blood samples were collected on the 8th, 11th, 14th, 17th, 21st, 28th, 38th, 68th, 98th, 128th, 158th and 188th days respectively. The plasma concentrations of paliperidone were determined by HPLC. , And safety was assessed by SPSS software using adverse event monitoring, vital sign monitoring, laboratory tests and extrapyramidal response scales. Results Seventeen patients who completed the final test were divided into three groups: 75 mg eq. (N = 5), 100 mg eq. (N = 9), 150 mgeq. (N = 3) (23.42 ± 11.95), (24.52 ± 12.44) and (16.92 ± 6.53) ng.mL-1, respectively. The peak concentrations after injection ranged from 11 to 18 days with an average of 17 days. Eleven patients had a total of 17 adverse events, the degree of mild to moderate. Conclusion After administration, the steady-state concentrations of paliperidone palmitate in each dose group were not different, but the individual differences were obvious. There was no correlation between dose and side effects.