甲巯咪唑乳膏透皮吸收的体内动力学

Study of pharmacokinetics for percutanous absorption of thiamazole ointment in rabbits

目的:研究甲巯咪唑乳膏经皮给药体内动力学及血清药物含量测定。方法:兔颈前甲状腺局部经皮给药,以高效液相色谱法测定血清中甲巯咪唑浓度,以3P87药动学软件计算药物体内动力学参数。结果:药时曲线符合一室模型,药物吸收速率常数(Ka)为2.590h-1;消除半衰期(T1/2β)为2.258h;峰浓度(Cmax)为1.480μg·ml-1;达峰时间(Tmax)为0.934h;曲线下积分面积(AUC)为6.230μg·ml-1·h。结论:甲巯咪唑乳膏局部给药有良好的透皮吸收性。

OBJECTIVE:To study the pharmacokinetics for percutanous absorption of thiamazole ointment and determine the concentrations in plasma.METHODS:To apply some thiamazole ointment on the part of thyroid gland in rabbit neck and determine the concentration in plasma by HPLC.The parameter on pharmacokinetics was calculated by software 3P87.RESULTS:The pattern of drug releasing was accorded with singal compartment model, and the main parameters of pharmacokinetics were as follows:The K a was 6.234 h -1 ;The T 1/2 was 2.426 h;The C max was 1.615 μg·ml -1 ;The T max was 0.799 h; The AUC was 6.230 μg·h·ml -1 .CONCLUSION:The thiamazole ointment will play an important part in prevention as the result of its good percutanous absorption.