中文摘要：

目的：建立更昔洛韦的高效液相色谱测定法，研究其在Caco-2细胞上的转运特征。方法：采用Eurospher-100C18/（250mm×4．6mm，5μm）色谱柱，流动相为甲醇-水（8：92），流速为1．0mL·min^-1，检测波长为254nm，考察介质pH、药物浓度、P-gp抑制剂对更昔洛韦在Caco-2细胞上转运的影响。结果：更昔洛韦在Caco-2细胞单层膜上的转运量具有一定的浓度和时间依赖性，但介质pH对其跨膜转运无显著影响；更昔洛韦在50mg·L^-1质量浓度下AP-BL、BL-AP方向转运表观渗透系数分别为（0．59±0．11）×10^-6和（2．0±0．4）×10^-6cm·s^-1.P-gP抑制剂维拉帕米能够增加更昔洛韦跨膜转运量。结论：更昔洛韦在Caco-2细胞上转运表现为被动扩散且有外转运蛋白参与更昔洛韦跨膜转运。

英文摘要：

OBJECTIVE To establish an HPLC method for determination of ganciclovir and investigate its transport in Caco- 2 cell monolayer model. METHODS Separation of ganciclovir was carried out by a Eurospher-100 C18 （250 mmx 4. 6 ram, 5 μm） column. The mobile phase consisted of methanol-water （8：92） at the flow rate of 1.0 mL·min^-1. The detective wave- length was set at 254 nm. This HPLC method was applied to determine ganciclovir concentration in Caco-2 cell monolayer transport system under various conditions, including changing ganciclovir concentration and pH of DHank＇s. Furthermore, influence of positive P-gp inhibitor verapamil on ganciciolovir transport was involved in the study. RESULTS Ganciciclovir transport in Caco-2 cell monolayer was time and concentration dependent, but not pH dependent. The apparent permeability coefficient （Papp） of ganciclovir with the concentration of 50μg·mL^-1 transporting from Apical to Basolateral and Basolateral to Apical was （0. 59 ± 0. 11 ） × 10^-6 cm·s^-1 and （2. 0 ± 0. 4） × 10^-6 cm·s^-1 , respectively. The transport of ganciclovir was enhanced by verapamil, CONCLUSION Ganciclovir transport complied with the passive diffusion in Caco-2 cell monolayer model, and furthermore efflux transporters might be involved in the transepithelial transport of ganciclovir.