甲巯咪唑灌服与外用给药对比观察及体内药动学

Study on pharmacokinetics for percutaneous absorption of thiamazole ointment in rabbits

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(Cmax)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(T1／2)灌服组为2.486 h,外 用组为2.645 h;达峰时间(Tmax)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 dose of thiamazolum in plasma and thyroid gland tissue. METHODS After thiamazolum of idetical dose oral and neck smearing to rat, thiamazolum in plasma and thyroid gland tissue was determined by HPLC. The parameters of phar macokinetics were calculated by 3P87 softwa re. RESULTS The concentration-time curves properly accord with the on e-room model,compared with oral group,the conce ntration of thiamazolum of neck smearing group was higher than the th yroid gl and tissue( P <0.05) , but C max and AUC valuaes in the plasma wa s lower( P < 0.05).The other parameters of the two groups were: T 1/2ke 2.486 h and 2.645 h; T max 1.894 h and 1.784 h.The two groups was not obviously different. CONCLUSIONS The drug action time could be extended by percutane ous adminstration.