复方去甲斑蝥素胃内滞留漂浮型缓释片在犬体内的药动学研究

目的:研究复方去甲斑蝥素(NECT)胃内滞留漂浮型缓释片在犬体内的药动学过程。方法:采用高效液相色谱法,测定Beagle犬血浆药物浓度。双周期交叉实验设计,8只健康Beagle犬分别服用漂浮型缓释片或普通片,检查药动学参数。结果:复方NECT胃内漂浮型缓释片与NECT普通片在犬体内的药动学规律均符合二室模型,tmax分别为(3.01±0.02)、(2.02±0.03)h,Cmax分别为(58.3±4.4)、(56.6±3.90)μg.mL-1,AUC0~24分别为(536.4±33.8)、(232.50±10.63)μg.h.L-1,MRT分别为(8.3±0.4)、(3.3±0.05)h,复方NECT胃内漂浮型缓释片的相对生物利用度为230.71%。结论:复方NECT胃内漂浮型缓释片可以提高NECT的生物利用度。

Pharmacokinetics of Compound Norcantharidin Sustained Release Tablets Remaining- floating in Stomach in Dogs

OBJECTIVE： To study the pharmacokinetic process of Compound norcantharidin sustained release tablets remaining floating in stomach in dogs. METHODS： Plasma drug concentration was determined by HPLC. By twoperiod crossover experiment design, 8 healthy beagle dogs were assigned to receive Compound norcantharidin sustained release tablets remaining- floating in stomach or common norcantharidin tablets, with pharmacokinetic parameters determined. RESULTS： The pharmacokinetics of both Compound norcantharidin remaining- floating sustained release tablets and common norcantharidin tablets fitted two- compartment model, their pharmacokinetic parameters were stated as follows： tmax： （3.01 ± 0.02） h vs.（2.02±0.03） h; Cmax： （58.3±4.4） μg·mL^-1 vs.（56.6±3.90） μg·mL^- 1 AUC0-24： （536.4±33.8） μg· h· L^-1 vs. （232.50 ± 10.63） μg · h · L^- 1; MRT ： （8.3 ± 0.4） h vs. （3.3 ± 0.05） h. The relative bioavailability of Compound norcantharidin remaining- floating sustained release tablets was 230.71%. CONCLUSION： The Remaining- floating （in stomach） property of Compound norcantharidin sustained release tablets contributed to higher bioavailability as compared with the common tablets of norcantharidin.