愈风宁心胶囊在兔体内的药动学和生物利用度研究

Pharmacokinetics and bioavailability of Yufeng Ningxin Jiaonang in rabbits

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 pharmacokinetics parameters and bioavailability of puerarin in Yufeng Ningxin Jiaoang in rabbits, and study the influence of dosage forms on the pharmacokinetics process of puerarin. METHODS: The concentration of puerarin in plasma was determined by HPLC. The 60 ml·L -1 HClO 4 was used to precipitate protein. The analytical column was Shimpack CLC ODS (5 μm,150 mm×4.6 mm ID). YWG C 18 H 37 was used as guard column. The mobile phase consisted of methol 360 ml·L -1 acetic acid water (25∶3∶72). The detecting wavelength was 247 nm. The 3P87 program was used to calculate the pharmacokinetic parameters. RESULTS : Puerarin was considered the main effective ingredient of Yufeng Ningxin Jiaonang and the target ingredient of the determination. The vivo course of puerarin in Yufeng Ningxin Jiaonang could be best described by an open two compartment model. Its main pharmacokinetics parameters were as follows: t 1/2(β) =78.03 min,Cl=10.283 L·min -1 , AUC=97.25 mg·min·L -1 , c max =0.675 mg·L -1 , t peak =44.5 min. Its bioavailability was 5.45%. CONCLUSION: The bioavailability of puerarin in Yufeng Ningxin Jiaonang was very low. This study will provide a scientific basis for the quality evaluation and dosage forms reformation of Yufeng Ningxin Jiaonang.