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目的:测定愈风宁心胶囊中主要有效成分葛根素在家兔体内的药时曲线,据此测算其体内代谢动力学参数。并与葛根素注射剂比较,研究了愈风宁心胶囊的绝对生物利用度。方法:用高效液相色谱法测定兔血浆中的葛根素,以体积分数为6%的高氯酸沉淀血浆蛋白质,用3P87程序计算药动学参数和生物利用度。结果:愈风宁心胶囊在兔体内的过程为二室开放模型,主要动力学参数是t1/2(β)=78.03min,Cl=10.283L·min-1,AUC=97.25mg·min·L-1,cmax=0.675mg·L-1,达峰时间为44.5min。绝对生物利用度为5.45%。结论:该研究可为愈风宁心胶囊内在质量评价和剂型改革提供一定科学依据。
Objective: To determine the drug-time curve of puerarin, the main active ingredient in Yufeng Ningxin Capsule, in rabbits, and to measure its in vivo metabolic parameters. In comparison with puerarin injection, the absolute bioavailability of Yufengningxin capsule was studied. METHODS: Puerarin in rabbit plasma was determined by high performance liquid chromatography. Plasma protein was precipitated by perchloric acid with a volume fraction of 6%. Pharmacokinetic parameters and bioavailability were calculated using the 3P87 program. Results: The process of Yufengningxin Capsule in rabbits was a two-compartment open model. The main kinetic parameters were t1/2(β)=78.03min, Cl=10.283L·min-1, and AUC=97.25mg. Min·L-1, cmax=0.675 mg·L-1, and the peak time was 44.5 min. The absolute bioavailability is 5.45%. Conclusion: This study can provide scientific basis for the intrinsic quality assessment and dosage form reform of Yufeng Ningxin Capsule.