硝苯地平缓释微丸家犬体内药动学和生物利用度
硝苯地平缓释微丸,,硝苯地平;海藻酸钠;缓释微丸;控释片;药动学;生物利用度,1实验材料,2实验方法,3结果,4讨论
摘 要 目的:研究硝苯地平缓释微丸在家犬体内的药动学及生物利用度。方法:家犬自身交叉对照分别口服单剂量硝苯地平缓释微丸(A)和进口硝苯地平控释片(B)各30 mg, 采用反相高效液相色谱法测定血药浓度,应用3P87药动学程序对血药浓度数据进行拟合。结果:硝苯地平缓释微丸和进口硝苯地平控释片的药动学参数:Tmax分别为3.47和5.41 h;Cmax分别为25.7和20.2 ng·mL-1;AUC0~∞分别为216和168 mg·h·mL-1。以B为参比制剂,单剂量给药时A的相对生物利用度为129%。结论:两种制剂单剂量给药30 mg为生物不等效。关键词 硝苯地平;海藻酸钠;缓释微丸;控释片;药动学;生物利用度
Pharmacokinetics and relative bioavailability of nifedipine
sustained release pellets
MA Ping, ZHU Li, SUN Shuying, XIN Yanru, YANG Jingyan, GAO WenJing
(1.General Hospital of Rocket Forces, Beijing 100088;2.Shengyang University of Pharmaceutical Sciences, Shengyang110015)
Abstract Objective:To study the pharmacokinetics and relative bioavailability of nifedipine sustained release pellets. Methods: The plasma concentration of nifedipine was determined by HPLC. The data was processed with the software 3P87. Results: The parameters of the two formulations for nifedipine: Tmax of the pellets and tablets were 3.47 and 5.41 h;Cmax were 25.7 and 20.2 ng/mL;and AUC0~∞were 216 and 168 mg·h·mL-1 respectively. The bioavailability of nifidipine sustained pellets with reference to nifedipine controlled-release tablets is 129%. Conclusions: The results of single oral administration 30 mg nifidipine demonstrated that two formulations were not bioequivalent. ......
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