摘要
目的2-[5,6-双(4-甲氧基苯基)吡嗪-2-氧基]-2-甲基丙酸(简称BMPA-01)是新型吡嗪类血小板聚集抑制剂。制备BMPA-01混悬剂、BMPA-01钠盐及其混悬剂,并对它们进行大鼠体内药动学和大鼠口服生物利用度研究。方法通过大鼠灌胃给药比较BMPA-01与其钠盐、BMPA-01与其混悬剂、BMPA-01钠盐与其混悬剂的药动学和口服生物利用度。结果大鼠体内药动学数据显示,BMPA-01钠盐AUC0-t(129086.38 ng·min/mL)比BMPA-01(73944.58 ng·min/mL)有所提高,BMPA-01混悬剂和BMPA-01钠盐混悬剂可显著提高药物的达峰浓度,增加药物口服生物利用度,其中BMPA-01钠盐混悬剂提高更为明显。结论钠盐混悬剂具有良好的生物利用度,该结果为BMPA-01后续的药剂配方选择提供了重要的数据支撑。
Objective 2-[5,6-bis(4-methoxyphenyl)pyrazine-2-yloxy]-2-methylpropionic acid(BMPA-01)is a novel pyrazine based platelet aggregation inhibitor.Prepare BMPA-01 suspension,BMPA-01 sodium salt and their suspension,and conduct pharmacokinetic and oral bioavailability studies on them in rats.Methods The pharmacokinetics and oral bioavailability of BMPA-01 and its sodium salt,BMPA-01 and its suspension,and BMPA-01 sodium salt and its suspension were compared by gavage administration in rats.Results The pharmacokinetic data in rats showed that the AUC 0-t of BMPA-01 sodium salt(129086.38 ng·min/mL)was higher than that of BMPA-01(73944.58 ng·min/mL).Both BMPA-01 suspension and BMPA-01 sodium salt suspension significantly increased the peak drug concentration and oral bioavailability,with the latter showing more pronounced improvement.Conclusion The sodium salt suspension demonstrated favorable bioavailability,providing crucial data support for the subsequent formulation selection of BMPA-01.
作者
袁琳
朱峰
于雅鑫
孙振国
楚庆如
李凤新
刘景昌
YUAN Lin;ZHU Feng;YU Yaxin(Jilin Provincial Institute of Pharmaceutical Research,Changchun,Jilin 130061,China)
出处
《中国处方药》
2026年第1期38-40,共3页
Journal of China Prescription Drug
