环胞苷滴眼液点眼的眼内药代动力学研究

Pharmacokinetics of Topically Applied Cyclocytidine Eyedrop in the Rabbit Eye

本文用[~3H]环胞苷滴眼液(0.1%)给兔点眼,观察了它的眼内通遥性和眼内药代动力学。结果表明,环胞苷滴眼液点眼后迅速透入兔眼各组织,其中角膜浓度最高,其次为虹膜一睫状体、房水,品状体和玻璃体中浓度极低。测得角膜上皮渗透性为3.19×10^(-4)。各组织中药物浓度半衰期分别为:泪液0.04hr、角膜3.04hr、房水1.77hr。

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.