【摘要】 <正> 无环鸟苷(Acyclorir.ACV)系一选择性抗单纯疱疹病毒(HSV)药物,具有作用强,毒副作用小的优点。眼科配成滴眼液点眼用于治疗各型HSV角膜炎取得良好效果。本文用[~3H]—ACV配成滴眼液(0.1%)给家兔点眼,观察其眼内透性并进行药代动力学分析。更多还原

【Abstract】 Selective antiviral agent ACV has high activity against HSV and low host toxiclity. The intraocular penetratiOn of ACV Was observed and pharmacokinetic analysis was performed following rabit topically applied ³H—labeled ACV （O.1% drop）.The radioactivities in lacrimal fluid, cornea, aqueous humour, iris—ciliary, len and vitreum were determined at O.25, 0.5, 1, 2, 3, 4, 5, 6th hour after topical administration of 01.% ³H—ACV drop, respectively. The result showed that ACV can rapidly penetrateinto rabbit Ocular tissue. The concentrational order was cornea, lacrimal fluid, iris, aqueous humour. Scarcely any ACV was detected in len and vitterm. The highest Concentration of ACV Was found in cornea. There was 38.61ug/g at 15th minute after droping and still 12.5ug/g at 6th hour. The pharmacokinetic paramers of cornea were KA=69.61h^-1, K=0.25h^-1, t/2=2.82h, TPK=0.08h, C（TPK）=35.10ug, Kep=H7×10^-4, respectively. ACV is an effective drug in treatment of HSV keratitis. Its target tissue is cornea. This experiment indicates that ACV can maintain high concentration in cornea, so it has good effect.更多还原