帕利哌酮长效针剂在中国精神分裂症患者的药代动力学特征

Pharmacokinetic characteristics of paliperidone palmitate in Chinese patients with schizophrenia

目的:评估棕榈帕利哌酮酯注射液3个月(PP3M)与棕榈酸帕利哌酮注射液1个月剂型(PP1M)在中国精神分裂症患者的药代动力学特征方法:本研究为多中心随机双盲非劣效试验。观察经过PP1M开放治疗达到临床稳定再随机给予PP1M或PP3M治疗后,两组患者帕利哌酮血药浓度的变化情况,计算相关参数并进行统计学分析。结果:各组患者的帕利哌酮血药浓度曲线均密集分布于有效血药浓度区间(15~60 ng/ml),平均峰谷比均<2。对应剂量的PP1M组和PP3M组平均血药浓度无显著差异、Cmax及药物暴露水平类似。结论:PP3M与PP1M在患者体内血药浓度平稳,波动较小,均可提供稳定有效的治疗浓度,两者形成的血药浓度变化及暴露剂量相当。

Objective:To evaluate the pharmacokinetics of paliperidone palmitate 3-month(PP3M)and 1-month(PP1M)formulation in Chinese schizophrenic patients.Method:This study was a multicenter randomized double-blind noninferiority trial.Patients were given PP1M open treatment to clinical stability and then randomly given PP1M or PP3M treatment,the changes of paliperidone blood concentration in the two groups were observed,calculated and statistically analyzed.Results:The paliperidone blood concentration of patients were close to the effective plasma concentration range(15-60 ng/ml),and the mean peak-to-trough ratio was less than 2.No statistical difference was found in average blood concentration,Cmax or extent of drug exposure in corresponding doses of PP1M and PP3M.Conclusion:PP3M and PP1M could provide stable and effective therapeutic concentrations in patients with schizophrenia.The paliperidone blood concentration and drug exposure formed by the two formulation were similar.