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目的:观察非典型抗精神病药物利培酮及9-羟基利培酮在人体内的药物动力学特点,为临床合理用药提供一定的依据。方法:选取2016年1~2016年6月在我院住院的精神分裂症患者30人,给予利培酮进行治疗,分别于给药后不同时间段内抽取患者静脉血,采用高效液相色谱法测定患者血浆中不同时段的血药浓度,计算其药物动力学指标。结果:利培酮达到最大血药浓度的平均时间tmax=1.6±0.7h,半衰期t1/2=3.2±1.2h,平均稳态浓度ρ=31.1±25.8μg/L,表观清除率CL/F=8.3±5.8L/h。9-羟利培酮的达到最大血药浓度的平均时间tmax=2.5±0.9h,半衰期t1/2=5.2±1.7h,平均稳态浓度ρ=135.6±38.2μg/L。结论:利培酮进入人体后吸收迅速,短时间内即可达到稳药浓度,但半衰期和表观清除率存在较大的个体差异,需引起临床重视。
Objective: To observe the pharmacokinetic characteristics of atypical antipsychotic risperidone and 9-hydroxy risperidone in human and to provide some evidences for clinical rational use of drugs. Methods: 30 schizophrenic patients hospitalized in our hospital from January 2016 to June 2016 were selected and treated with risperidone. Venous blood samples were taken from patients at different time points after administration. The patients were divided into two groups: high-performance liquid chromatography Determination of plasma concentrations in patients with plasma at different times, calculate its pharmacokinetic parameters. Results: The mean time to maximum plasma concentration of risperidone was 1.6 ± 0.7h, the half-life was t1 / 2 = 3.2 ± 1.2h, the average steady-state concentration was ρ = 31.1 ± 25.8μg / L and the apparent clearance rate was CL / F = 8.3 ± 5.8 L / h. The mean time to maximum plasma concentration of 9-hydroxy-risperidone was 2.5 ± 0.9 h, half-life t1 / 2 = 5.2 ± 1.7 h, and mean steady-state concentration ρ = 135.6 ± 38.2 μg / L. CONCLUSION: Risperidone can be rapidly absorbed into human body and reach stable drug concentration within a short period of time. However, there is a large individual difference in half-life and apparent clearance, which needs clinical attention.