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目的对两种上市的咪唑斯汀缓释制剂进行人体药动学的研究,以评价两厂家生产的咪唑斯汀缓释片是否具有生物等效性。方法采用随机交叉试验设计,10名男性健康受试者单剂量口服咪唑斯汀缓释片(皿治林和尼乐)10mg后于规定时间点取血,用高效液相法测定血药浓度,计算两种缓释制剂的主要药动学参数,进行人体生物利用度的比较。结果10名男性健康受试者单剂量口服咪唑斯汀缓释片皿治林后的药动学参数分别为tmax为(1.70±0.59)h,cmax为(276.99±67.58)ng/mL,t1/2为(12.68±1.97)h,MRT为(15.29±2.67)h,AUC0→t为(2555.89±777.52)ng/mL·h,AUC0→∞为(2724.07±852.60)ng/mL·h;单剂量口服参比制剂尼乐后的药动学参数分别为tmax为(1.95±0.64)h,cmax为(344.56±93.96)ng/mL,t1/2为(12.42±1.89)h,MRT为(13.49±1.60)h,AUC0→t为(2532.28±776.06)ng/mL·h,AUC0→∞为(2659.16±818.06)ng/mL·h。统计结果表明药动学参数t1/2、MRT、tmax、AUC0→T、AUC0→∞受试制剂皿治林与参比制剂尼乐相比没有显著性差异,cmax具有显著性差异,与参比制剂cmax相比有所降低。AUC0→t、AUC0→∞、cmax、t1/2和MRT生物等效,tmax生物不等效。受试制剂的相对生物利用度平均为(101.26±9.82)%(n=10,以AUC0→t计算)和(102.52±8.61)%(n=10,以AUC0→∞计算);药动学参数cmax的比值为(82.17±15.32)%。结论受试制剂皿治林与参比制剂尼乐二者生物等效,但皿治林制剂咪唑斯汀峰浓度略低,达峰时间tmax略短。
OBJECTIVE To study the pharmacokinetics of two mizolastine sustained-release preparations marketed to evaluate the bioequivalence of mizolastine sustained release tablets produced by the two manufacturers. Methods A randomized crossover trial was designed. Ten healthy male volunteers were given a single dose of 10 mg mizolam sustained-release tablets (Panzhi Lin and Niile) and then blood was taken at the prescribed time points. Plasma concentrations were determined by HPLC. The main pharmacokinetic parameters of two kinds of sustained-release preparations were calculated to compare the bioavailability of human body. Results The pharmacokinetic parameters of mizolastine in a single dose of mizolastopril were respectively (1.70 ± 0.59) h, (276.99 ± 67.58) ng / mL and t1 / 2 was (12.68 ± 1.97) h, MRT was (15.29 ± 2.67) h, AUC0 → t was (2555.89 ± 777.52) ng / mL · h and AUC0 → ∞ was (2724.07 ± 852.60) ng / The pharmacokinetic parameters of oral reference formulation nile after tmax were (1.95 ± 0.64) h, cmax was (344.56 ± 93.96) ng / mL, t1 / 2 was (12.42 ± 1.89) h and MRT was (13.49 ± 1.60) h, AUC0 → t was (2532.28 ± 776.06) ng / mL · h and AUC0 → ∞ was (2659.16 ± 818.06) ng / mL · h. The statistical results showed that there was no significant difference in the pharmacokinetic parameters t1 / 2, MRT, tmax, AUC0 → T, AUC0 → ∞ between the experimental formulation and the reference formulation Neil, cmax had significant difference, Formulation cmax decreased compared to. AUC0 → t, AUC0 → ∞, cmax, t1 / 2 and MRT bioequivalence, tmax bioequivalence. The relative bioavailability of the tested formulations averaged (101.26 ± 9.82)% (n = 10 calculated as AUC0 → t) and (102.52 ± 8.61)% (n = 10 calculated as AUC0 → ∞); pharmacokinetic parameters The ratio of cmax was (82.17 ± 15.32)%. Conclusions The experimental formulation of Panzhi Lin and reference formulation Neilex are bioequivalent, but the concentration of mizolastine in Panzhi Lin formulation is slightly lower, and the peak time tmax is slightly shorter.