兔眼玻璃体内注射三氟胸苷后的半衰期及玻璃体清除率

Half-life and vitreous clearance of trifluorothymidine after intravitreal injection in the rabbit eye.

作者信息

Pang M P, Branchflower R V, Chang A T, Peyman G A, Blatt H, Minatoya H K

机构信息

Pacific Eye Surgery Center, Inc., Honolulu, HI 96817.

出版信息

Can J Ophthalmol. 1992 Feb;27(1):6-9.

PMID:1555136

Abstract

To determine the half-life and vitreous clearance of trifluorothymidine, a drug that demonstrates good toxicity against cytomegalovirus (CMV), we injected 200 micrograms of the drug intravitreally in the eyes of nine New Zealand white rabbits. None of the rabbits showed any adverse reactions to the injection or the drug. The rabbits were killed at 3, 6, 12, 24 or 72 hours. High-performance liquid chromatography was used to measure the vitreous trifluorothymidine concentration. The half-life of the drug was found to be 3.15 hours, and the vitreous concentration remained above the ID50 (concentration required to inhibit cytopathic effects by 50% compared with control cultures) for CMV for about 30 hours. We conclude that trifluorothymidine may be of future benefit in the management of CMV retinitis.

摘要

为了确定三氟胸苷（一种对巨细胞病毒（CMV）显示出良好毒性的药物）的半衰期和玻璃体内清除率，我们向9只新西兰白兔的眼内玻璃体内注射了200微克该药物。没有一只兔子对注射或该药物表现出任何不良反应。在3、6、12、24或72小时处死兔子。使用高效液相色谱法测量玻璃体内三氟胸苷的浓度。发现该药物的半衰期为3.15小时，并且玻璃体内浓度在约30小时内保持高于CMV的ID50（与对照培养物相比抑制细胞病变效应50%所需的浓度）。我们得出结论，三氟胸苷在CMV视网膜炎的治疗中可能具有未来应用价值。