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目的研究布南色林及其代谢产物在中国健康受试者多剂量药动学特征。方法 20名健康受试者随机分成两组(4 mg bid组和8 mg qd组),分别连续7 d口服布南色林,采集第5、6、7日早晨服药前和第7日服药后60 h内血样;采用HPLC-MS/MS测定血浆中布南色林及其主要代谢产物N-去乙基布南色林的浓度,并采用DAS程序对试验数据进行处理,计算药动学参数。结果4 mg组布南色林及其代谢物的药动学参数ρav分别为(327.75±83.83)和(200.38±67.75)ng·L-1,t max分别为(1.48±0.69)和(4.15±2.16)h,t1/2分别为(12.98±3.35)和(18.68±4.90)h,AUC SS分别为(3 933.00±1 005.96)和(2 404.56±813.03)ng·h·L-1,AUC0-∞分别为(8 160.18±2 173.64)和(7 730.84±1 732.06)ng·h·L-1,8 mg组布南色林及其代谢物的药动学参数分别为(289.84±140.54)和(209.72±70.81)ng·L-1,t max分别为(1.63±0.87)和(3.80±1.03)h,t1/2分别为(15.90±5.12)和(19.70±5.90)h,AUC SS分别为(6 956.05±3 372.90)和(5 033.31±1 699.39)ng·h·L-1,AUC0-∞分别为(9 660.33±3 594.69)和(9 377.57±2 686.91)ng·h·L-1。结论布南色林药动学参数个体差异较大,需要进行治疗药物监测。
Objective To study the multi-dose pharmacokinetics of buanzanlin and its metabolites in Chinese healthy subjects. Methods Twenty healthy subjects were randomly divided into two groups (4 mg bid group and 8 mg qd group). Bupanserin was administered orally for 7 consecutive days. Pre-dose and post-dose were taken on the 7th, The blood samples were collected within 60 h. The concentrations of buananserin and its major metabolite N-desmethylbutyrin in plasma were determined by HPLC-MS / MS. The experimental data were processed by DAS program to calculate the pharmacokinetic parameters . Results The pharmacokinetic parameters ρav of buananserin and its metabolites in 4 mg group were (327.75 ± 83.83) and (200.38 ± 67.75) ng · L-1, respectively. The t max were (1.48 ± 0.69) and (4.15 ± 2.16) h and t1 / 2 were (12.98 ± 3.35) and (18.68 ± 4.90) h respectively, AUC SS were (3 933.00 ± 1 005.96) and (2 404.56 ± 813.03) ng · h · L -1, (8 160.18 ± 2 173.64) and (7 730.84 ± 1732.06) ng · h · L-1, 8 mg, respectively. The pharmacokinetic parameters of Buansenserin and its metabolites were (289.84 ± 140.54) and (209.72 ± 70.81) ng · L-1, t max were (1.63 ± 0.87) and (3.80 ± 1.03) h, t1 / 2 were (15.90 ± 5.12) and (6 956.05 ± 3 372.90) and (5 033.31 ± 1699.39) ng · h · L-1, respectively, and the AUC0-∞ were (9 660.33 ± 3 594.69) and (9 377.57 ± 2 686.91) ng · h · L -1 . Conclusion The parameters of BuanSanLin pharmacokinetic parameters vary greatly, which need to be monitored by therapeutic drugs.