目的 用高效液相色谱-质谱法测定健康男性受试者单次空腹口服受试及参比托拉塞米片后的血药浓度,计算受试制剂和参比制剂的药动学参数,评价两种制剂是否生物等效。方法 采取两制剂、双周期、交叉的设计试验,24例男性健康受试者单剂量口服受试制剂和参比制剂的托拉塞米片,以HPLC-MS测定血浆中的托拉塞米浓度。采用SPSS及BAPP2.2软件处理计算主要药动学参数。结果 受试制剂与参比制剂中托拉塞米的ρmax分别为(1 408.29±337.27)和(1 487.86±360.24)ng·mL-1,tmax分别为(0.90±0.42)和(1.03±0.50)h,t1/2分别为(4.43±0.57)和(4.43±0.60)h,MRT分别为(3.90±0.60)和(4.01± 0.72)h,AUC0-24 h分别为(3 886.86±865.99)和(3 906.06±761.72) ng·h·mL-1,AUC0-∞分别为(3 936.57±903.93)和(3 956.96±789.98) ng·h·mL-1。按AUC0-24 h和AUC0-∞计算,受试制剂的相对生物利用度分别为(99.8±11.7)%和(99.7±12.0)%。结论 两种制剂在健康人体内具有生物等效性。
Abstract
OBJECTIVE To evaluate the bioequivalence of tested and reference torasemide tablets in healthy male volunteers. METHODS A single oral dose of the two formulations was given to 24 healthy male volunteers according to a randomized crossover design. Plasma drug concentrations were determined by HPLC-MS. RESULTS The pharmacokinetic parameters of torasemide of the two preparations were as follows: ρmax (1 408.29±337.27) and (1 487.86±360.24) ng·mL-1, tmax (0.90±0.42) and (1.03±0.50) h, t1/2(4.43±0.57) and (4.43±0.60) h, MRT (3.90±0.60) and (4.01±0.72) h, AUC0-24 h(3 886.86±865.99) and (3 906.06±761.72) ng·h·mL-1, AUC0-∞ (3 936.57±903.93) and (3 956.96±789.98) ng·h·mL-1, respectively. The relative bioavailability of tested torasemide tablets were (99.8±11.7)% and (99.7±12.0)% when calculated by AUC0-24 h and AUC0-∞, respectively. CONCLUSION The two formulations of torasemide are bioequivalent in healthy Chinese volunteers.
关键词
托拉塞米 /
生物等效性 /
高效液相色谱-质谱
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Key words
torasemide /
bioequivalence /
HPLC-MS
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中图分类号：
R965
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参考文献
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