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目的建立UFLC-MS/MS法测定格拉司琼的血药浓度,研究自制盐酸格拉司琼透皮贴片和Sancuso贴片在新西兰兔体内的药动学行为。方法采用平行设计,12只新西兰兔按随机区组设计分为给药组和对照组,每组6只,分别给予自制贴片和Sancuso贴片,采用经验证的UFLC-MS/MS法测定兔血浆中格拉司琼浓度。使用DAS 2.1.1软件计算药动学参数。结果格拉司琼在1.0~500 ng/ml范围内线性关系良好,方法回收率为92.5%~101.4%,日内、日间精密度的RSD均小于5%。新西兰兔经皮给予自制贴片和Sancuso贴片的主要药动学参数AUC(0-t)为(2106±337.0)与(2402±557.7)μg/L.h、AUC(0-∞)为(2 107±336.8)与(2 404±558.7)μg/L.h、C max为(63.03±17.53)与(82.32±34.76)μg/L、T max为(3.7±2.3)与(4.8±3.2)h、T1/2为(2.4±1.5)与(3.5±2.5)h。结论本方法高效、快速、灵敏、准确、专属性强,适用于格拉司琼血药浓度的监测。本研究结果显示,格拉司琼在兔体内的吸收和消除速度快,且两种贴剂C max、AUC(0-t)和AUC(0-∞)在相同给药周期下的组间差异具有统计学意义。
Objective To establish a method for the determination of granisetron by UFLC-MS / MS and to study the pharmacokinetics of granisetron hydrochloride and Sancuso in New Zealand rabbits. Methods A parallel design was used. Twelve New Zealand rabbits were randomly divided into two groups according to a randomized block design: control group and control group. Six rabbits in each group were given self-made patches and Sancuso patches respectively. Rabbits were evaluated by UFLC-MS / MS Plasma concentrations of granisetron. Pharmacokinetic parameters were calculated using DAS 2.1.1 software. Results Granisetron had a good linearity in the range of 1.0-500 ng / ml. The method recoveries ranged from 92.5% to 101.4%. The intra-day and inter-day RSDs were less than 5%. The main pharmacokinetic parameters AUC (0-t) were (2106 ± 337.0) and (2402 ± 557.7) μg / Lh, and the AUC (0-∞) The Tmax was (3.7 ± 2.3) and (4.8 ± 3.2) h, respectively, and the T max was (333 ± 558.7) μg / L and Cmax were (63.03 ± 17.53 and 82.32 ± 34.76) μg / 2 were (2.4 ± 1.5) and (3.5 ± 2.5) h. Conclusion The method is efficient, rapid, sensitive, accurate and specific. It is suitable for the monitoring of granisetron plasma concentration. The results of this study show that granisetron is rapidly absorbed and eliminated in rabbits and that the difference between groups for Cmax, AUC (0-t) and AUC (0-∞) for the two patches at the same dosing cycle has Statistical significance.