左舒必利注射液在中国健康受试者的药代动力学

发布时间：2018-10-23 19:55

【摘要】：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。
[Abstract]:Objective to study the pharmacokinetics of left sulpiride injection in Chinese healthy volunteers. Methods A total of 30 subjects, half male and half male, were divided into three dose groups, and received intramuscular injection of different doses of levosulpiride at a single and multiple doses, and blood samples were collected at different times. The concentration of levosulpiride in plasma was determined by high performance liquid chromatography-tandem mass spectrometry (HPLC/MS/MS). The pharmacokinetic parameters were calculated by DAS 3.0 software. Results the main pharmacokinetic parameters of single intramuscular injection of left sulpiride at 75 mg were (724.70 卤248.91), () 949.60 卤234.80), (1619.00 卤366.80) 渭 g / L -1 / 2, respectively (7.65 卤1.32), (7.58 卤0.89), (8.01 卤0.88) h AUC0-t were (2874.17 卤1093.71), (4481.75 卤913.09), (7559.33 卤1428.87) 渭 g hL-1 respectively. T 1 / 2 was (7.41 卤0.79) h ~ (-1) AUC _ (0-t) and (4658.33 卤909.51) 渭 g 路L ~ (-1) h in continuous administration group. Conclusion the pharmacokinetic characteristics of single intramuscular injection of levosulpiride in Chinese healthy volunteers were linear within 2575 mg, and there was no accumulation tendency in multiple doses. There was no significant difference between male and female.
【作者单位】：华中科技大学同济医学院附属协和医院临床药理研究室;
【分类号】：R969.1

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