西红花甙-Ⅰ在大鼠体内的药代动力学

The Pharmacokinetics of Crocin-Ⅰ in Rats

建立了在生物洋品中西红花甙-Ⅰ的HPLC测定法,并研究了其在大鼠体内药代动力学。杂质不干扰样品测定,回收率>80%,日间、日内RSD<5%。大鼠iv西红花甙-Ⅰ后,血药浓度-时间曲线符合二房室开放模型,在肺、肾组织中浓度较高,而脑和睾丸中浓度在检测限以下。药物自胆和粪的排泄甚少,24h尿排泄约占药剂量的1/3。

A reverse-phase high-performance liquid chromatography(HPLC) method for determination of crocin-Ⅰ in biological samples was developed using a Nave-pack-C_(18) column (150×3.9mm, 4.0μm) and mobile phase of methanol and 5% acetic acid(50 : 50) in 10 min with a detection wave length at 440 nm. The recovery of crocin-Ⅰ in plasma is over 80%. The RSD of method (%) is no more than 5%. The plasma concentration-time curve was found to be fitted with a two compartment open model after iv administration of crocin- 1 in rats. Dosing 2,4,8 mg/kg crocin-Ⅰ, its elimina tion from plasma accorde with linear kinetics, and the elimination half-lives were 2.42 h(2 mg/kg), 1.51 h(4mg/kg) and 2. 14 h(8 mg/kg). The volumes of distribution were 0. 25 L/kg(2 mg/kg) 0. 40 L/kg(4mg/kg) and 0.51 L/kg(8 mg/kg). The drug concentrations were high in the kidney and lung, moderate in heart, liver, spleen gastro-intestine and muscle, and not found in brain and fat. A large amount of unchanged crocin-Ⅰ was found in urine, but it was almost not detected in faces and bile. The results showed that crocin-Ⅰ was metabolized in vivo.