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目的建立大鼠全血中靛玉红含量测定方法及大鼠体内靛玉红的药动学行为研究。方法采用超声、碱化及液-液萃取等方法处理全血样品;色谱条件:GL ODS C18(4.6×250mm,5μm)色谱柱,流动相为甲醇-5%甲酸(68∶32,v/v),流速:1mL.min-1,检测波长289nm为检测条件;以5.6mg.kg-1的剂量大鼠尾静脉i.v.和200mg.kg-1的剂量大鼠i.g.给药,采用非那雄胺为内标物,测定给药后全血中靛玉红的含量并用DAS 2.1.1软件计算药动学参数。结果靛玉红在5.55~1110ng.mL-1的浓度范围线性关系良好,最低定量限为5.55ng.mL-1,提取回收率71.8±6.4%~80.7±6.5%;大鼠灌胃和静脉注射给药后其体内药动学过程分属二室模型和三室模型,绝对生物利用度10.19%。结论实验表明本法操作简单,灵敏度高,重现性良好,结果准确可靠,可以用于大鼠体内靛玉红的药动学行为研究。
Objective To establish a method for the determination of indirubin in rat whole blood and the pharmacokinetics of indirubin in rat. Methods The whole blood samples were processed by sonication, alkalization and liquid-liquid extraction. The chromatographic conditions were as follows: GL ODS C18 (4.6 × 250 mm, 5 μm) column with methanol-5% formic acid (68:32, v / v ), Flow rate: 1mL.min-1, the detection wavelength of 289nm for the detection conditions; a dose of 5.6mg.kg-1 rat tail vein iv and 200mg.kg-1 dose ig administration, finasteride As an internal standard, the content of indirubin in the whole blood after the administration was measured and the pharmacokinetic parameters were calculated using the DAS 2.1.1 software. Results The results showed that the linear range of indirubin was 5.55-1110ng.mL-1, the lowest limit of quantification was 5.55ng.mL-1 and the recovery was 71.8 ± 6.4% -80.7 ± 6.5%. The rats were intragastrically and intravenously Pharmacokinetics in vivo after administration belong to two-compartment model and three-compartment model, the absolute bioavailability of 10.19%. Conclusion The experiments show that this method is simple, sensitive, reproducible and accurate. It can be used to study the pharmacokinetics of indirubin in rats.