左旋咪唑擦剂的药代动力学——离子对HPLC法研究

The Pharmacokinetics of Levamisole Liniment by Ion-Pair HPLC

给家兔背部皮肤涂擦左旋咪唑擦剂后,用离子对HPLC法测定了血浆左旋咪唑的含量.以μ-Bondapak C_(12)为固定相,以水-甲醇-庚烷磺酸(v/v为55/45/2)的0.2%乙酸液(pH3.5)为流动相,在波长291nm处检测.最低检测浓度为0.02μg/mL,平均回收率为71.25±3.79%(n=5).左旋咪唑经皮吸收后,其药动学符合—室模型,动力学方程为:(?)=1.75(e^(- 0.0025t)—e^(-0.5129t);其吸收达峰时间(T_(max))为4.03h;峰浓度(C_(max))为0.99μg/mL;消除半衰期(T_((1/2)β))7.49;曲线下面积(A_(mu))为15.57(μg·h)/mL.同时与肌注左旋咪唑的药动学进行了比较.

After the levamisole (LMS) liniment was spreaded on the dorsal skin of rabbits, the level of LMS in plasma was determined by an ion-pair HPLC. The separation was performed on the μ-Bondapak C18 with mobile of 0. 2% of acetic acid in water,methanol and heptane sul-fonic acid mixture (55 : 45 : 2,v/v/v). The detection was made at 291 nm. The detection limit of the method was 0. 02μg/mL, and the average recovery was 71. 25±3. 79% (n=5). The results showed that the pharmacokinetics of LMS liniment in normal rabbit fitted a one-compartment open model with an equation: C=1.75(e-0.0925t-e-0.5219t). The area under curve (Auc) was 15. 7 (μg · h)/mL. The elimination half-life was 7. 49 h and the peak concentration in rabbit was 0. 99 μg/mL at 4. 03 h after cutaneous application.