双氯酚酸钠滴眼液的眼内组织分布及药代动力学

Distribution and Pharmacokinetics of Topically Applied Diclofenac Sodium Eyedrop in Rabbit Eye

目的：测定双氯酚酸钠点眼后兔眼组织的浓度并进行眼内药代动力学研究。方法：２４只家兔分为８个时间组，每组３只（６只眼），用０．１％双氯酚酸钠滴眼液点眼后于不同时间抽取房水，分离角膜，虹膜－睫状体和玻璃体，采用高效液相色谱法测定眼组织中的药物浓度。结果：经双氯酚酸钠在眼内的药代动力学过程为二房室模型，在角膜，房水，虹膜－睫状体和玻璃体的峰浓度分别为１８．８４± ４．５６ μｇ·ｇ－１， ０３０± ０．１２ ｍｇ·Ｌ－１， ３．８４± ２．３０ μｇ·ｇ－１， ０．０３± ０．０１ｍｇ·Ｌ－１。达峰时分别为０．５２±０．３５，１．１７±０．４５，０．９６±０．４３，１．７３±０．７８ｈ。结论：双氟酚酸钠滴眼后能很好渗透到各眼组织中，临床上用于眼科治疗是可行的。

OBJECTIVE: To determine diclofenac sodium in various tissues of rabbit eye and evaluate pharmacokinetics following its topical application.METHODS: 24 rabbits(48 eyes) for the experiment were divided into & groups(by time of collecting sample). Aqueous humor, cornea, iris-ciliary body and vitreous humor were collected at 0.25, 0.5, 0.75, 1 .0, 2.0, 4.0, 8.0, 12h following topically applying 0. 1% diclofenac sodium eyedrop to rabbit eye and concentration ofdiclofenac sodium were measured in the tissueby high performance liquid chromatography.RESULTS: The pharmacokinetic behaviour of diclofenac sodium in eye were described by two-compartment model.The peak concentrations of diclofenac sodium in cornea, aqueous humor, iris-ciliarybody and vitreous humor were 18.84 ｑ± 4.56μg·g-1,0.30 ± 0. 12μg·1-1,,3.84 ± 2.30μg·g-1,0.03 ± 0.01μg·1-1 and peak time were 0.52 ± 0. 35, 1. 17 ± 0.45,0.96 ± 0.43, 1 .73 ± 0.78h,respectively.CONCLUTION :Diclofenac sodium can penetrate intraocular various tissue and can be used in ophthalmology therapy.