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目的 :建立Beagle犬血浆中氧化苦参碱的LC MS测定法 ,测定它的绝对生物利用度。方法 :Beagle犬 6只 ,随机分为 2组 ,采用单剂量双周期自身交叉设计 ,分别给犬单剂量静脉注射或灌胃氧化苦参碱 ,用LC MS法测定给药后的血浆中药物浓度。结果 :氧化苦参碱在 2～ 5 0 0 0 μg·L-1的范围内呈良好的线性关系 (r =0 .9990 ) ,最低检出限达0 .6 μg·L-1,日内和日间误差均小于 4 .2 % ,方法回收率大于 96 .7% ;氧化苦参碱的药 时数据符合二室模型 ,Cmax为 2 .4 2± 0 .97μg·L-1,Tmax为 1.0± 0 .3h ,T1 2 β为 5 .5 4± 1.5 8h ,AUC0→∝ 为 6 .12± 1.0 8μg·L-1·h-1,绝对生物利用度为 (19.4± 9.0 1) %。结论 :该法灵敏、简单 ,专属性强 ;氧化苦参碱在Beagle犬体内绝对生物利用度较低
Objective : To establish an LC MS method for determination of oxymatrine in Beagle dogs plasma and determine its absolute bioavailability. METHODS: Six Beagle dogs were randomly divided into 2 groups. Single-dose double-cycle self-crossover design was used. Dogs were given a single dose of intravenous or gastric oxymatrine, and plasma drug concentrations were measured by LC MS. . Results: Oxymatrine showed a good linear relationship in the range of 2–500 μg·L-1 (r=0.9990) with a detection limit of 0.6 μg·L-1. The error between days was less than 4.2%, the method recovery was greater than 96.7%; the time data of oxymatrine met the two-compartment model, Cmax was 2.42 ± 0.97μg·L-1, and Tmax was 1.0. ± 0.3h, T1 2 β was 5.54 ± 1.58h, AUC0 → ∝ was 6.12 ± 1.08μg·L-1 · h-1, and the absolute bioavailability was (19.4 ± 9.01%). Conclusion: This method is sensitive, simple, and highly specific; Oxymatrine has low absolute bioavailability in Beagle dogs.