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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 in vivo kinetics and serum drug content of methimazole cream transdermally. Methods: The transdermal administration of thyroid in rabbits was performed by topical administration. The concentration of methimazole in serum was determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters of drugs were calculated by 3P87 pharmacokinetic software. Results: The drug-drug curve was consistent with one-compartment model. The drug absorption rate constant (Ka) was 2.590 h-1, the elimination half-life was 2.258 h, and the peak concentration was 1.480 μg · ml- (Tmax) was 0.934h; the area under the curve (AUC) was 6.230μg · ml-1 · h. Conclusion: Topical imazamide cream has good transdermal absorbability for topical administration.