汉防己甲素的兔眼内药代动力学研究

汉防己甲素的兔眼内药代动力学研究

黄正;杜之渝;刘玺;向一旻

【期刊名称】《中国实用眼科杂志》 【年(卷),期】2010(028)002

【摘要】目的 研究汉防己甲素(Tet)滴眼液单次滴眼后在兔眼内的药代动力学行为.方法 采用0.3%Tet滴眼液单次滴眼后,利用高效液相色谱法(HPLC)检测其在兔眼内各组织中的药物浓度变化过程,并计算其在眼内各组织中的药代动力学参数.结果 Tet在眼内各组织中的浓度变化均符合血管外给药一室模型一级动力学过程.其在角膜组织中的浓度最高,消除半衰期为115.140min,消除速率常数为0.060/min.Tel在角膜中的AUC为2336.294μg/(g·min),约为房水中AUC的8倍,虹膜睫状体的5倍,晶状体的15倍,玻璃体的25倍.结论 Tet滴眼液单次滴眼后,在角膜中能够达到较高的浓度,Tet在眼内的药代动力学参数为其临床应用以及用药方案选择提供了实验依据.%Objective To investigate pharmacokinetics

of

Tet

eye

drops

after

single

topical

administration.Methods one 50μ l drop of 0.3%Tet was instilled in the eyes of rabbits in each group.The chang of drug concentrations were assayed by high-pressure liquid chromatography (HPLC).At last,to get pharmacokinetic parameters of Tet in rabbit eyes by 3p87.Results The concentration-time processes of Tet were found to fit extravascular does single compartment model., The concentrations of Tet in cornea were highest, which half life time and elimination rate constant were 115.140min and 0.060/min respectively,and the AUC in cornea which