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研究了青藤碱在大鼠的药动学节律。用Wistar大鼠,在自然昼夜节律条件下,自由摄食和饮水。选择卯时(早7时)和酉时(晚7时)给予相同剂量的青藤碱,在给药后不同的时间点采取血桨和脑组织,用HPLC法测定血浆和脑中的青藤碱浓度,结果表明,卯时给药,血浆中和脑中的青藤碱浓度明显高于酉时(P<0.05)。无论是卯时还是酉时给药,青藤碱血中的药时曲线均可用开放型二房室模型描述,但动力学参数存在着较大的差异,卯时给药Cmax44.5mg/L,K100.44h-1,AUC98.75mg·h/L,T1/2α0.13h,T1/2β3.99h和Vd0.45L/kg;酉时给药,Cmax16.7mg/L,K100.30h-1,AUC55.02mg·h/L,T1/2α0.24h,T1/2β3.31h和Vd1.20L/kg。本研究提示青藤碱的药代动力学受生物节律依赖性的影响。
The pharmacokinetics of sinomenine in rats was studied. Wistar rats were allowed to eat and drink freely under natural circadian rhythms. The same doses of sinomenine were given at the time of spasm (early 7:00 am) and time of spasm (early 7 o’clock). Blood oars and brain tissue were taken at different time points after administration, and plasma and brain sinomenine concentrations were determined by HPLC. The results showed that the concentration of sinomenine in plasma and brain was significantly higher than that in sputum (P<0.05). The drug-time curve in sinomenine blood can be described by the open two-compartment model, regardless of whether it is administered at the time of pupa or at the time of spasm. However, there is a big difference in kinetic parameters. At the time of administration, Cmax 44.5mg/L, K100.44h- 1, AUC98.75mg·h/L, T1/2α0.13h, T1/2β3.99h and Vd0.45L/kg; administration at time of administration, Cmax 16.7mg/L, K100.30h-1, AUC55.02mg·h/ L, T1/2 ? 0.24h, T1/2?3.31h and Vd1.20L/kg. This study suggests that the pharmacokinetics of sinomenine is influenced by biological rhythm dependence.