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目的建立快速、灵敏的HPLC法测定大鼠血浆中水合橙皮内酯(Meranzin hydrate)的血药浓度,并比较灌胃枳壳与水合橙皮内酯单体后大鼠体内水合橙皮内酯的药动学行为。方法色谱条件:色谱柱为Dikma Diamonsil C18柱(250 mm×4.6 mm,5μm),保护柱为Dikma guard柱(8 mm×4 mm,5μm),流动相为乙腈-水(体积比78∶22),流速为1 ml/min,柱温为25℃。用此HPLC法测定枳壳与水合橙皮内酯单体在大鼠体内的血药浓度,估算二者的药代动力学参数。结果线性范围12.5~1000 ng/ml(r=0.9997),最低检测浓度10 ng/ml,回收率分别为90.53%~93.45%,日内和日间精密度RSD均小于10%。与枳壳大鼠灌胃相比,灌胃水合橙皮内酯单体后的药动学参数Tmax和t1/2的值显著变小(P<0.01),而Cmax和AUC0-24则显著增大(P<0.01)。结论该方法可用于水合橙皮内酯的药动学研究。同时与灌胃枳壳相比,给予水合橙皮内酯单体的消除半衰期长,达峰时间长,消除速率慢,生物利用度更高。
OBJECTIVE To establish a rapid and sensitive HPLC method for the determination of plasma concentrations of hydranolactone in rat plasma and to compare the effects of hydromagnesium chloride lactone Pharmacokinetic behavior. Methods Chromatographic conditions were as follows: Dikma Diamonsil C18 column (250 mm × 4.6 mm, 5 μm), Dikma guard column (8 mm × 4 mm, 5 μm) as guard column and acetonitrile- water (78:22) , Flow rate 1 ml / min, column temperature 25 ℃. The HPLC method was used to determine the plasma concentration of Fructus Aurantii and hydrated orange lactone in rats, and the pharmacokinetic parameters of the two compounds were estimated. Results The linear range was 12.5-1000 ng / ml (r = 0.9997). The lowest detection concentration was 10 ng / ml. The recoveries were 90.53% ~ 93.45%. The RSDs of intra- and inter-day precision were less than 10%. Compared with the gavage of Fructus Aurantii, the pharmacokinetic parameters Tmax and t1 / 2 were significantly decreased (P <0.01), but Cmax and AUC0-24 were significantly increased Large (P <0.01). Conclusion This method can be used to study the pharmacokinetics of hydrated orange lactone. At the same time compared with perfusion Fructus Aurantii, the hydration of orange lactone monomer elimination of long half-life, a long time to peak, the elimination rate is slow, higher bioavailability.