双氯芬酸钠眼用制剂的眼内组织分布及药动学  

Distribution of diclofenac sodium ophthalmic preparation in ocular tissues and its pharmacokinetics in rabbit

作　　者：彭绍民[1] 王绍伟[1] 孙大卫[1] 

机构地区：[1]哈尔滨医科大学附属第二临床医院眼科,黑龙江哈尔滨150086

出　　处：《食品与药品》2006年第05A期42-44,共3页Food and Drug

摘　　要：目的测定双氯芬酸钠眼用制剂在兔眼组织内的浓度,进行眼内药动学研究。方法48只家兔分为2大组,每大组分8个时间组,每个时间组3只、6眼,用0.1%双氯芬酸钠滴眼液和眼膏点眼后于不同时间抽取房水、虹膜-睫状体,采用高效液相色谱法测定眼组织中的药物浓度。结果经3p87拟合,双氯芬酸钠在眼内的药动学过程为二房室模型,滴眼液和眼膏在房水、虹膜-睫状体的最大峰浓度分别为0.32±0.11μg/ml、0.41±0.15μg/ml、4.18±1.01μg/mg、5.95±2.09μg/mg;达峰时间基本相同,均约在给药后1h。结论双氯芬酸钠眼用制剂能很好渗透到眼组织中,因此,在临床上该制剂可以很好的抑制眼科炎症反应。Objective To determine the concentration of diclofenac sodium ophthalmic preparation in ocular tissues of rabbit and evaluate its pharmacokinetics. Methods 48 rabbits were divided into two groups and each group included eight time groups with three rabbits. 0.1% diclofenac sodium ointment and diclofenac sodium eye drops were applied topically to rabbit eyes and aqueous humor and iris-ciliary were collected at various time. The concentration of diclofenac sodium in ocular tissues was measured by high performance liquid chromatography. Results The blood concentration- time curve of diclofenac sodium fitted in with the two compartment model. Diclofenac sodium ointment had a higher concentration and a longer half-time than diclofenac sodium eye drops, but the peak time was the same at about lh. Cmax of diclofenac sodium ointment and eye drops in aqueous humor and iris-ciliary were 0.32 ± 0.11 μg/ml, 0.41 ± 0.15 μg/ml and 4.18 ± 1.01 μg/mg, 5.95 ± 2.09 μg/mg, respectively. Conclusion Diclofenac sodium ointment and eye drops can be well absorbed into the ocular tissues for treating various ophthalmological inflammation.

关 键 词：双氯芬酸钠 眼用制剂 药动学 

分 类 号：R988.1[医药卫生—药品]