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目的建立测定人血浆中托烷司琼浓度的LC/MS/MS法,并用该法研究托烷司琼在健康人体内的药动学特征及其相对生物等效性。方法采用LC/MS/MS法,测定20名健康男性受试者口服含盐酸托烷司琼10 mg的受试制剂和参比制剂后,不同时刻血浆中托烷司琼的浓度,绘制药动学曲线并计算主要药动学参数。结果受试制剂和参比制剂中托烷司琼的主要药动学参数如下:tmax分别为(2.1±0.8)和(2.1±0.8)h;ρmax分别为(15.7±6.2)和(16.1±6.2)μg.L-1,t1/2分别为(9.9±5.0)和(9.4±5.0)h;用梯形法计算,AUC0-t分别为(213.2±162.7)和(210.1±159.2)μg.h.L-1,AUC0-∞分别为(231.0±190.4)和(231.2±190.9)μg.h.L-1。以AUC0-t计算,盐酸托烷司琼口腔崩解片中托烷司琼的相对生物利用度为(102.2±25.7)%。结论盐酸托烷司琼的两种制剂生物等效。
Objective To establish a LC / MS / MS method for the determination of tropisetron in human plasma and to study the pharmacokinetics and the relative bioequivalence of tropisetron in healthy volunteers. Methods The plasma concentrations of tropisetron at different time points after oral administration of 10 mg of tropisetron hydrochloride and reference preparations in 20 healthy male subjects were determined by LC / MS / MS. Learn the curve and calculate the main pharmacokinetic parameters. Results The major pharmacokinetic parameters of tropisetron in the test and reference preparations were as follows: tmax = (2.1 ± 0.8) and (2.1 ± 0.8) h; ρmax = (15.7 ± 6.2) and (16.1 ± 6.2 ) (μg · L -1) and t1 / 2 (9.9 ± 5.0) and (9.4 ± 5.0) h, respectively. The AUC0-t was (213.2 ± 162.7) and (210.1 ± 159.2) 1, AUC0-∞ were (231.0 ± 190.4) and (231.2 ± 190.9) μg.hL-1, respectively. The relative bioavailability of tropisetron in tropisetron hydrochloride orally disintegrating tablets was (102.2 ± 25.7)% based on AUC0-t. Conclusions Both formulations of tropisetron hydrochloride are bioequivalent.