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五倍子在中华倒刺鲃体内的药动学研究

         

摘要

The study reports the pharmacokinetics of Galla chinensis in Spinibarbus sinensis with a single-dosing oral ad-ministration 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 perform-ance 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 ( t1/2α) was 1.054 h and the elimination half -life ( t1/2β) 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 258.047μg h/mL and 6.480 h in the renal, respectively.The results showed that G.chinensis can be absorbed preferably and rapid-ly in S.sinensis.At the same time , it can be kept in vivo for enough time to get curative effect .%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77.3967μgh/mL,402.106μgh/mL和258.048μgh/mL;平均驻留时间( MRT)分别是19.3091 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。

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