CAJ | 학술논문

目的：建立大鼠血浆中阿苯达唑及其代谢物高效液相色谱（ HPLC ）测定方法并测定阿苯达唑脂质体冻干粉相对生物利用度。方法大鼠单剂量灌胃给予阿苯达唑片和脂质体冻干粉后，用HPLC法测定各时间点的血药浓度，并用3 P97软件拟合药代动力学参数。结果2种制剂的主要药代动力学参数如下：Cmax分别为（4．32±0．70），（5．27±0．60）μg? mL－1，Tmax分别为（4．71±1．17），（5．39±0．94）h，AUC分别为（63．93±13．08），（84．56±14．97）μg? h? mL－1，以片剂为参比制剂，脂质体冻干粉相对生物利用度为154．17％。结论2种制剂在大鼠体内药代动力学符合二室模型，冻干粉能显著提高药物的生物利用度。
목적：건립대서혈장중아분체서급기대사물고효액상색보（ HPLC ）측정방법병측정아분체서지질체동간분상대생물이용도。방법대서단제량관위급여아분체서편화지질체동간분후，용HPLC법측정각시간점적혈약농도，병용3 P97연건의합약대동역학삼수。결과2충제제적주요약대동역학삼수여하：Cmax분별위（4．32±0．70），（5．27±0．60）μg? mL－1，Tmax분별위（4．71±1．17），（5．39±0．94）h，AUC분별위（63．93±13．08），（84．56±14．97）μg? h? mL－1，이편제위삼비제제，지질체동간분상대생물이용도위154．17％。결론2충제제재대서체내약대동역학부합이실모형，동간분능현저제고약물적생물이용도。
Objective To establish a HPLC method for the determina-tion of albendazole and its metabolites in rat plasma, and then calculate the relative bioavailability of freeze -dried albendazole liposomes ( L -ABZ).Methods A single oral dose of freeze-dried L-ABZ and al-bendazole tablets( T-ABZ) were given in rats, plasma concentrations at each time point were assayed by HPLC method.The pharmacokinetic pa-rameters were calculated with 3P97 program.Results The pharmacoki-netic parameters of two formulations were as follows: Cmax were(4.32 ± 0.70),(5.27 ±0.60)μg? mL-1; Tmax were (4.71 ±1.17),(5.39 ± 0.94)h;AUC were(63.93 ±13.08),(84.56 ±14.97) μg? h? mL-1, respectively.Compared with the T-ABZ, the relative bioavailability of freeze-dried L-ABZ was 154.17%.Conclusion The pharmacokinet-ics of two formulations accord with the two compartment models and the freeze-dried can improve bioavailability significantly.