[^3H]—洛非西定在大鼠的绝对生物利用度

The absolute bioavailability of [ ~3H]-lofexidin-HCl in rats

目的 研究了 [3H] 洛非西定的吸收和绝对生物利用度。方法 分二剂量组 ( 0 2mg·kg-1,0 0 5mg·kg-1) ,用统计矩法测定 po及iv给予大鼠 [3H] 洛非西定后的药物动力学参数 ,计算生物利用度。结果 高剂量组绝对生物利用度F为 5 4 0 % ;低剂量F为 5 4 7%。结论 口服给药后吸收较快 ,吸收率较高 。

AIM To detemine absorption and absolute bioavilability of [ 3H]lofexidine(LOF) in rats. METHODS To derive unchanged drug from blood samples by TLC method , to detemine the radioactivity of [ 3H]lofexidine by liquid scintillation counter and to calculate the pharmacokinetic parameters of LOF by statistical moments method. RESULTS Absolute bioavilability of high dosage group(02 mg·kg -1 ) is about 540% and that of low dosage group (005 mg·kg -1 ) is about 547%. CONCLUSION The absorption was rapider and more complete and showed a linear process within the dosage 005 mg·kg -1 to 02 mg·kg -1 .