摘要
目的 研究[^3H]洛非西定在大鼠体内不同给药途径的药代动力学。方法 TLC分离原型药物，液闪法测定血浆中药物放射性强度，用3P87程序计算药动学参数。结果 大鼠iv[^3H]洛非西定，其时-量曲线符合开放3室模型。t1/2pi为0．031～0．042h，t1／2a为0．352～0．398h，t1/2β为10．982～11．763h。大鼠ig[^3H]洛非西定，其时-量曲线符合开放2室模型。t1／2Ka为1．037～1．102h，t1／2a为2．113～2.325h，t1／2β为11.805～10.465h，Tmax为2.448～2．196h，F为53％～55％。AUC和Cmax与剂量呈线性关系。结论 本方法适合洛非西定的药动学研究，测定结果为临床合理用药提供依据。
Objective To study the pharmacokinetics of [^3H] -lofexidine in rats. Methods Parent drug concentration of lofexidine in plasma and tissues were determined by TLC method. The radioactivity of [^3H]-lofexidine in plasma were determined with scintillation. The pharmacokinetic parameters of lofexidine in rats were calculated by 3P87 program. Results Concentration-time curves after iv administration at the dose of 0.05 or 0.2 mg/kg of [^3H] -lofexidine in rats were fitted to the three-compartment model with t1/2pi of 0.031 ～ 0. 042 h, t1/2a of 0.352 ～ 0.398 h and t1/2β of 10. 982 ～ 11. 763 h. Concentration-time curves after ig administration at the dose of 0.05 or 0.2 mg/kg of [^3H] -lofexidine in rats were fitted to the two-compartment model with t1/2Ka of 1. 037 ～ 1. 102 h, t1/2a of 2.113 - 2. 325 h, t1/2β of 11. 805 ～ 10.465 h, Tmax of 2.448 - 2. 196h and the bioavailability （F） of 53% ～ 55%. The area under curves （AUCs） and Cmax were linearly over the dosages. Conclusion The method can be used in the pharmacokinetic study of lofexidine and provides evidence for clinical application.
出处
《现代食品与药品杂志》
CAS
2006年第4期55-57,共3页
JOurnal of Modern Food and Pharmaceuticals
