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目的研究健康受试者单剂量静脉注射两种地塞米松棕榈酸酯的药代动力学。方法用开放、双周期随机交叉给药方案,10名健康受试者单剂量静脉注射两种地塞米松棕榈酸酯1 m L,用LC-MS/MS法测定血浆中地塞米松棕榈酸酯、地塞米松和尿样中的地塞米松,计算其主要药代动力学参数。结果 9名受试者完成全部试验。单剂量静脉注射地塞米松棕榈酸酯受试制剂和参比制剂后,地塞米松棕榈酸酯的主要药代动力学参数:AUC0-tn分别为(951.57±341.39),(955.03±434.42)ng·m L-1·h;AUC0-∞分别为(954.83±341.82),(957.85±433.95)ng·m L-1·h;cmax分别为(681.33±307.91),(622.00±205.71)ng·m L-1;t1/2分别为(0.73±0.05),(0.76±0.18)h。单剂量静脉注射地塞米松棕榈酸酯受试制剂和参比制剂后,地塞米松的主要药代动力学参数:AUC0-tn分别为(179.11±27.99),(199.18±26.90)ng·m L-1·h;AUC0-∞分别为(208.35±37.54),(237.45±45.52)ng·m L-1·h;cmax分别为(26.17±3.19),(32.44±2.74)ng·m L-1;tmax分别为(2.00±1.09),(1.56±0.64)h,t1/2分别为(3.74±1.02),(4.30±1.46)h。48 h地塞米松的尿中累积排泄率分别为(3.58±1.07)%和(3.93±1.23)%。结论两种制剂的主要药代动力学参数无显著性差异。
Objective To study the pharmacokinetics of two single dexamethasone palmitate in healthy subjects. Methods Two open-cycle and double-period randomized crossover dosing regimens were used. Ten healthy volunteers received a single intravenous injection of two dexamethasone palmitate (1 m L), and plasma concentrations of dexamethasone palmitate , Dexamethasone, and dexamethasone in urine samples to calculate their major pharmacokinetic parameters. Nine subjects completed all the trials. The main pharmacokinetic parameters of dexamethasone palmitate after single-dose intravenous dexamethasone palmitate test and reference formulation were AUC0-tn (951.57 ± 341.39), (955.03 ± 434.42) ng (954.83 ± 341.82) and (957.85 ± 433.95) ng · m L-1 · h, respectively, and the values of cmax were (681.33 ± 307.91) and (622.00 ± 205.71) ng · m L-1; t1 / 2 were (0.73 ± 0.05) and (0.76 ± 0.18) h, respectively. The main pharmacokinetic parameters of dexamethasone: AUC0-tn were (179.11 ± 27.99), (199.18 ± 26.90) ng · m L after single-dose intravenous dexamethasone palmitate test and reference formulation -1 · h; AUC0-∞ were (208.35 ± 37.54) and (237.45 ± 45.52) ng · m L-1 · h, respectively; cmax were (26.17 ± 3.19) and (32.44 ± 2.74) ng · m L -1 ; tmax were (2.00 ± 1.09), (1.56 ± 0.64) h, t1 / 2 were (3.74 ± 1.02) and (4.30 ± 1.46) h, respectively. Urine cumulative excretion rates at 48 h dexamethasone were (3.58 ± 1.07)% and (3.93 ± 1.23)%, respectively. Conclusion There was no significant difference in the main pharmacokinetic parameters between the two preparations.