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目的研究左舒必利注射液在中国健康受试者单次及多次给药的药代动力学。方法用开放、随机、平行的试验设计。30名受试者,男女各半,分为3个剂量组,分别接受单次及多次肌内注射不同剂量左舒必利,采集不同时间的血样,用高效液相色谱-串联质谱法(HPLC/MS/MS)测定血浆中左舒必利的浓度。用DAS 3.0软件计算药代动力学参数。结果单次肌内注射25,50,75 mg左舒必利的主要药代动力学参数:cmax分别为(724.70±248.91),(949.60±234.80),(1619.00±366.80)μg·L-1;t1/2分别为(7.65±1.32),(7.58±0.89),(8.01±0.88)h,AUC0-t分别为(2874.17±1093.71),(4481.75±913.09),(7559.33±1428.87)μg·L-1·h。连续给药组t1/2为(7.41±0.79)h;AUC0-t为(4658.33±909.51)μg·L-1·h。结论中国健康受试者单次肌内注射给药左舒必利在25~75 mg内呈线性药代动力学特征,多次给药没有蓄积倾向,男、女间比较,差异无统计学意义。
Objective To study pharmacokinetics of single and multiple doses of Zusanlipping in Chinese healthy subjects. Methods Using an open, randomized, parallel trial design. 30 subjects, half male and half female, divided into 3 dose groups, receiving single and multiple intramuscular injections of different doses of left supremab, blood samples were collected at different times, using high performance liquid chromatography - tandem mass spectrometry (HPLC / MS / MS) was used to determine the plasma concentration of Zuvalipide. Pharmacokinetic parameters were calculated using DAS 3.0 software. Results The main pharmacokinetic parameters of 25, 50 and 75 mg of Zuvalipide were: cmax (724.70 ± 248.91), (949.60 ± 234.80) and (1619.00 ± 366.80) μg · L-1, respectively; 2 were (7.65 ± 1.32), (7.58 ± 0.89) and (8.01 ± 0.88) h respectively, and the AUC0-t were 2874.17 ± 1093.71, 4481.75 ± 913.09 and 7559.33 ± 1428.87 μg · L-1 · h T1 / 2 in continuous administration group was (7.41 ± 0.79) h; AUC0-t was (4658.33 ± 909.51) μg · L-1 · h. Conclusions The single pharmacokinetics of levosulfapy in Chinese healthy volunteers was linear pharmacokinetic within 25-75 mg. There was no tendency of accumulation in multiple administrations. There was no significant difference between male and female patients.