目的研究羟基红花黄色素A(hydroxysafflor yellow A,HYSA)在人体内的药动学特征。方法12名健康受试者随机分为低、中、高3个剂量组,每组4人,分别脉滴注给予注射用红花黄色素(以羟基红花黄色素A的含量为35,70和140 mg计算),采用高效液相色谱法测定给药后不同时间点血浆中羟基红花黄色素A的浓度并计算药动学参数。结果羟基红花黄色素A在体内过程符合二室模型。主要药动学参数如下:ρ_max分别为(2.02±0.18),(7.42±0.61),(14.48±4.71) mg·L^-1;t_1/2β分别为(3.05±0.70),(3.56±0.77),(3.35±0.91)h;AUC_0-15分别为(6.79±1.29),(26.75±5.46),(49.81±13.75)mg·h·L^-1。AUC_0-∞分别为(7.85±1.07),(28.60±5.51),(53.80±14.85)mg·h·L^-1。结论高、中、低3个单剂量组中羟基红花黄色素A在人体内的消除半衰期较快,AUC_0-15,AUC_0-∞和ρ_max均与剂量呈线性关系。

OBJECTIVE To study the pharmacokinetics of hydroxysafflor yellow A for intravenous infusion injection in Chinese healthy volunteers.METHODS 12 Healthy volunteers,randomly divided into 3 groups with 4 volunteers in each group, received HSYA at single dose of 35,70 and 140 mg,respectively.The concentrations of HSYA in human plasma at different time were analyzed by HPLC-UV method.The pharmacokinetic parameters were calculated by the software DAS 2.0.RESULTS The plasma concentration-time curves of the preparation were fitted by a two-compartment model.The main pharmacokinetic parameters were as follows:ρ_max were(2.02±0.18),(7.42±0.61),(14.48±4.71) mg·L^-1;t_l/2β were(3.05±0.70),(3.56±0.77), (3.35±0.91)h;AUC_0-15were(6.79±1.29),(26.75±5.46),(49.81±13.75)mg·h·L^-1。AUC_0-∞ were(7.85±1.07),(28.60±5.51), (53.80±14.85) mg·h·L^-1.CONCLUSION The t_1/2β was similar among three dosages and the values of AUC_0-15,AUC_0-∞,ρ_max were linear in the dose range from 35 mg to 140 mg.