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本文建立了用反相高效液相色谱法分离并测定家兔、大鼠、狗血浆中天麻素(甙)及其代谢产物对羟基苯甲醇(甙元)。本方法简便、迅速、灵敏,且精密度高。三种动物 iv 天麻素后的药一时曲线均属二室开放模型,其 t_(1/2β)分别为大鼠8.41min、家兔38.4min、狗105min。天麻素 iv 100mg/kg 和200mg/kg 时大鼠和家兔血浆中的药代动力学行为均属线性范围。该药在上述三种动物体内的分布和消除较迅速。大鼠 ig 的生物利用度为81%,同样剂量给家兔 ig,血浆中未检出原形药,但十二指肠给药后血浆中可测得天麻素,其生物利用度为2.8%。家兔 iv 天麻素后血浆中可测得少量甙元,而在大鼠、狗血浆中均未检出。三种动物的药代动力学有明显的种属差异。
In this paper, we established the separation and determination of gastrodin and its metabolite p-hydroxybenzyl alcohol in the plasma of rabbits, rats and dogs by RP-HPLC. The method is simple, rapid, sensitive, and high in precision. The drug-temporal curve of three animals after iv gastrodin was a two-compartment open model. The t_(1/2β) was 8.41 min for rats, 38.4 min for rabbits and 105 min for dogs. The pharmacokinetic behavior of plasma in rats and rabbits at the gastrodins iv 100 mg/kg and 200 mg/kg was linear. The distribution and elimination of the drug in the above three animals are relatively rapid. The bioavailability of rat ig was 81%. The same dose was given to rabbits. No prototype drug was detected in plasma, but gastrodin was measured in plasma after duodenal administration. Its bioavailability was 2.8%. Rabbits iv Gastrodin can be measured after a small amount of aglycone, but not in rat, dog plasma. The pharmacokinetics of the three species have distinct species differences.