【摘要】 目的:研究2种注射用亚叶酸盐的生物等效性。方法:采用随机交叉试验设计,血样采用三氯乙酸沉淀蛋白,直接经反相高效液相色谱法测定血浆中亚叶酸的浓度。计算注射用亚叶酸钠(受试制剂)与注射用亚叶酸钙(参比制剂)的主要药动学参数和相对生物利用度,并进行统计学分析。结果:单剂量注射受试制剂与参比制剂后,tmax分别为(0.292±0.096)、(0.25±0)h,Cmax分别为(31.973±4.337)、(33.332±3.312)μg.mL-1,AUC0～24分别为(139.670±13.859)、(144.401±13.574)μg.h.mL-1,AUC0～∞分别为(154.246±16.481)、(161.306±17.871)μg.h.mL-1,MRT0～24分别为(6.795±0.730)、(6.963±0.713)h,t1/2分别为(7.183±1.469)、(7.316±2.045)h。受试制剂平均相对生物利用度为(98.2±3.7)%。结论:2种制剂在健康人体内生物等效。更多还原

【Abstract】 OBJECTIVE:To study the bioequiavailability of sodium/calcium folinate for injections in healthy volunteers.METHODS:By a randomized crossover design,trichloracetic acid was used to precipitate the protein in serum sample.Serum concentration of folinate was determined by RP-HPLC.The pharmacokinetic parameters and relative bioavailability of sodium folinate for injection vs.calcium folinate for injection were computed and analyzed statistically.RESULTS:The pharmacokinetic parameters of single dose of sodium folinate for injection(trial formulation)vs.calcium folinate for injection(reference formulation)were as follows:tmax(0.292±0.096)h vs.(0.25±0)h;Cmax(31.973±4.337)μg·mL-1 vs.(33.332±3.312)μg·mL-1;AUC0～24(139.670±13.859)μg·h·mL-1 vs.(144.401±13.574)μg·h·mL-1;AUC0～∞(154.246±16.481)μg·h·mL-1 vs.(161.306±17.871)μg·h·mL-1;MRT0～24(6.795±0.73)h vs.(6.963±0.713)h;t1/2(7.183±1.469)vs.(7.316±2.045).The mean relative bioavailability of the sodium folinate for injection was(98.2±37.1)%.CONCLUSION:The two formulations are proved to be bioequivalent.更多还原