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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

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【作者】 陈祖基高长凤宋洁贞丁祖锐王德喜

【Author】 Chen Zuji,et al Henan Institute of Ophthalmology,Zhengzhou

【机构】 河南省眼科研究所河南省人民医院河南省同位素研究所 郑州450003郑州450003郑州450003

【摘要】 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。

【Abstract】 The intraocular penetration of Cyclocytidine(CC)was observed and pharmacokineticanalysis was performed following topically applying 3H-labeled CC(0.1% eyedrop)torabbit eyes.The results showed that CC can rapidly penetrate into rabbit ocular tissues.The concentrational order was cornea,iris-cillary,aqueous humour.The highest concen-tration of CC was found in cornea.The concentration of the drug in lens and vitreouswas very low.The pharmacokinetic parameters were calculated with nonlinear least squaremethod by digital computer.The permeability of the corneal epithelial barrier(Kep)was3.19×10-4.The half-life(t 1/2)of the tissue concentration was lacrimal fluid 0.04 hr,cornea 3.04 hr and aqueous humour 1.77 hr,respectively.The experiment indicates thatCC can maintain higher concentration in cornea,so it has good effect on HSV keratitis.

  • 【文献出处】 眼科研究 ,Chinese Ophthalmic Research , 编辑部邮箱 ,1992年04期
  • 【被引频次】3
  • 【下载频次】60
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