摘要
以五倍子的有效成分没食子酸为目标药物,采用高效液相色谱法检测药物浓度,用房室模型和非房室模型法同时分析药动学数据,获得25.0℃水温条件下20 mg/kg单剂量口灌五倍子(Galla chinensis)后中华倒刺鲃(Spinibarbus sinensis)体内的药物代谢情况。结果表明:血液中的药动学数据可以用一级吸收二室开放模型描述,一些血液的药动参数和肝脏、肾脏的数据用非房室模型分析,药物在中华倒刺鲃体内的吸收、分布和消除半衰期分别是:0.523 h,1.054 h和10.501 h。在血液、肝脏和肾脏均在1 h时达到最大药物峰,Cmax值分别是9.166μg/mL,76.214μg/mL和85.860μg/mL;药时曲线下面积(AUC)分别是77.396 7μgh/mL,402.106μgh/mL和258.048μgh/mL;平均驻留时间(MRT)分别是19.309 1 h,25.935 h和6.480 h。五倍子在中华倒刺鲃体内有较快和较好的吸收,同时在体内能保持较高浓度足够时间以达到治疗效果。
The study reports the pharmacokinetics of Galla chinensis in Spinibarbus sinensis with a single- dosing oral administration of 20 mg drug per kilogram weight at the water temperature 25. 0 ℃. The designed experiment took the active ingredient gallic acid( GA) as the object drug,and the drug concentration in the tissues was determined by high performance liquid chromatography( HPLC) method. Both compartment and non- compartment model analysis were used to obtain the pharmacokinetic parameters. The serum concentration- time data were fitted to a two- compartment open model with 1st order absorption. Some of the serum parameters,as well as the liver and renal concentration- time data were calculated with non- compartment model analysis. The absorption half- life( t1 /2 Kα) was 0. 523 h and the distribution half- life( t1 /2 α) was 1. 054 h and the elimination half- life( t1 /2 β) was 10. 501 h in the serum. And the studied tissues of serum, liver and renal all reached the maximum concentration( Cmax) at the time point of 1 h and the values were 9. 166,76. 214 and 85. 860 μg / mL,respectively. The area under the concentration- time curve( AUC) and mean residence times( MRT) were 77. 397 μg h/mL and 19. 309 h in the serum,402. 106 μg h/mL and 25. 935 h in the liver,and 258. 047 μg h/mL and 6. 480 h in the renal,respectively. The results showed that G. chinensis can be absorbed preferably and rapidly in S. sinensis. At the same time,it can be kept in vivo for enough time to get curative effect.
出处
《淡水渔业》
CSCD
北大核心
2014年第3期68-74,共7页
Freshwater Fisheries
基金
Agriculture Special Research Project of Non-profit Undertakings of China(ASRPNUC,200903048-08)