穿心莲超微粉2种成分在鸡体内的药动学研究

Study on Pharmacokinetics of Two Effective Components from Andrographis Paniculata Ultra-fine Powder in Chickens

作者研究了穿心莲超微粉中穿心莲内酯、脱水穿心莲内酯2种有效成分在鸡体内的药物代谢动力学特征。根据体质量以5 g.kg-1单剂量给鸡灌服给药,然后采用HPLC法同时测定其体内药物浓度,用3P97药动学程序分析其药动学特征。结果表明穿心莲内酯、脱水穿心莲内酯在鸡的血浆浓度-时间数据符合一级吸收二室模型,主要的药动学参数分别如下:t1/2α(47.4±3.5)和(41.9±3.9)min,t1/2β(104.8±12.8)和(143.0±12.8)min,t1/2Ka(23.2±2.6)和(9.77±1.22)min,AUC(329.3±28.8)和(329.1±25.5)(μg.mL-1).min,tmax(51.5±3.5)和(37.2±2.8)min,Cmax(1.60±0.32)和(1.44±0.09)μg.mL-1,MRT(175.2±15.9)和(219±18)min。这2种有效成分的体内过程表征了该超微粉在鸡体内的药动学规律,且吸收和消除差异有显著或极显著的差异;本研究为穿心莲粉体制剂的临床应用和中药多成分药动学研究提供参考。

The pharmacokinetic features of andrographolide and dehydroandrographolide, two ef- fective components of Andrographis paniculata, were investigated in chickens administrated with ultra-fine powder of A. paniculata in the paper. The two compounds in chicken plasma were determined simultaneously by HPLC method following oral administration of Andrographis paniculata ultra-fine powder at a single dose of 5 g ·kg^-1 B. W. , the pharmacokinetic process were evaluated by Pharmacokinetics Program 3P97. The results showed that the plasma concentration-time data of andrographolide and dehydroandrographolide in chicken plasma could be described by two compartment model with first-order absorption, with t1/2α of （47.4 ± 3. 5 ）and （41.9±3.9） min,t1/2β of （104.8±12.8） and （143.0±12.8） min,t1/2Ka of （23.2±2.6）and （9.77 ±1.22） min,AUC of （329.3±28.8） and （329.1±25.5） （μg · mL^-1） · min,tmax of （51.5±3.5） and （37.2±2.8） min,Cmax of （1.60±0.32）and （1.44±0.09）μg · mL^-1 ,MRT of （175.2±15.9） and （219 ± 18 ）min for them respectively. The pharmacokinetic rule of the ultra-fine powder could be reflected by kinetic process of the two constituents in chickens, between which significant or extremely significant difference exited in absorbtion and elimination stage, and the study could provide references for the clinical application of the powder preparation of Andrographis paniculata, also do for the pharmacokinetic study on multi-constituents from Chinese traditional medicine.