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目的:研究甲巯咪唑不同给药途径的血及甲状腺组织中药物 含量。方法: 用HPLC法测定大鼠在同剂量下, 灌服甲巯咪唑与颈部外涂甲巯咪唑乳膏后的不同时间血及甲 状腺组织中甲巯咪唑的含量, 以3P87药动学软件计算动力学参数。 结果:灌服给药与颈部外用给药,血清药时曲线均符合一室模型。 甲巯咪唑透皮吸收乳膏单剂量给 药后, 甲状腺组织中药物 浓度明显高于灌服给药组(P<0.05);血中药物峰浓度(Cmax)和曲线下 面积(AUC)均显著高于 灌服给药组(P<0.01);药物消除半衰期(T1/2)灌服组为2.486 h,外 用组为2.645 h;达峰时间(Tmax)灌服组为1.894 h,外用组为1.784 h,两种方法无明 显差异。结论:甲巯咪唑经皮给药可提高靶组织浓度,延长药物作用时间。
Objective: To study the drug content in blood and thyroid tissue of different methimazole routes of administration. Methods: The contents of methimazole in blood and thyroid tissue were measured by HPLC at different doses of methimazole and thimerosal cream administered at the same dose in rats. The pharmacokinetics of 3P87 was calculated Kinetic parameters. Results: The results of gavage administration and external application to the neck showed that the curve of serum drug time was consistent with one-compartment model. Methimazole transdermal absorption cream after single-dose administration, the thyroid tissue drug concentration was significantly higher than that of the oral administration group (P <0.05); the peak concentration of blood drug (Cmax) and the area under the curve (T1 / 2) was 2.486 h in the control group and 2.645 h in the topical administration group. The peak time (T max) was 1.894 h in the gavage group and 1.784 h in the external group. There was no significant difference between the two methods. Conclusion: Methimazole transdermal delivery can increase the concentration of target tissue and prolong the action time of drug.