盐酸苯噁唑在鹿体内的药代动力学研究

Study on Pharmacokinetics of Idazoxan Hydrochloric in Deer

本研究的主要目的是建立鹿血浆盐酸苯噁唑浓度反相高效液相色谱紫外检测法,探讨盐酸苯噁唑在鹿血浆中的药代动力学。6只临床健康的梅花鹿,同一环境下饲养后肌内注射盐酸苯恶唑(0.44mg.kg-1),颈静脉采血8mL后分离血浆,通过建立的高效液相色谱检测法,测定各采血时间的血浆药物浓度。结果表明,盐酸苯噁唑单剂量肌内注射给药后,药代动力学符合吸收一室模型,药代动力学参数吸收半衰期(t1/2Ka)、消除半衰期(t1/2Ke)分别为(2.09±0.34)、(13.18±0.24)min,血浆药时曲线下面积(AUC0→∞)为(70±3.50)(μg.mL-1).min,最大血药浓度(Cmax)为(4.70±0.50)μg.mL-1,血药达峰时间(Tpeak)为(12.46±0.12)min。试验结果提示,盐酸苯噁唑在鹿体内吸收快,消除迅速,4h后血浆中无药物残留。

This experiment was to establish a method for the determination of idazoxan hydrochloric in deer plasma by RP-HPLC,and to discuss pharmacokinetics of idazoxan hydrochloric in deer.Six clinical healthy Cervus nippon Temmincks（breed in a room） were injected with the idazoxan solution at the dose of 0.44 mg·kg-1.8 mL blood sample was taken from a jugular vein and plasma was separated for drug analysis using high liquid chromatography with ultraviolet detection.The results showed that the kinetics of idazoxan hydrochloric was fitted to one compartment model with first order absorption by route of administration.The main pharmacokinetic parameters were as follows： the half-lives of absorption（t1/2ka） and elimination（t1/2ke） were（2.09±0.34） and（13.18±0.24） min,respectively,area under the plasma drug concent ration-time curve from 0 to ∞（AUC） was（70±3.50）（μg·mL-1）·min,the peak plasma concent ration（Cmax） was（4.70±0.50） μg·mL-1,peaking at（12.46±0.12） min after dosing.The results indicated that idazoxan hydrochloric is characterized by rapid drug action,fast metabolism with little residue in the blood.