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局部滴眼和胶原盾给药后环孢素A在兔角膜和房水中的渗透情况。

Penetration of cyclosporin A into the rabbit cornea and aqueous humor after topical drop and collagen shield administration.

作者信息

Kanpolat A, Batioglu F, Yilmaz M, Akbas F

机构信息

Faculty of Medicine, Department of Ophthalmology, University of Ankara, Turkey.

出版信息

CLAO J. 1994 Apr;20(2):119-22.

PMID:8044977
Abstract

We used commercially available 12-hour collagen shields to deliver cyclosporin A (CsA) to the cornea and aqueous humor in rabbit eyes. Six New Zealand white rabbits were divided into three groups. The first group (four eyes) received 6 mg of CsA in castor oil and the second group (four eyes) received 6 mg of CsA in olive oil applied as topical drops to rabbit eyes within 12 hours. In the third group (four eyes) 12-hour collagen shields soaked in 6 mg CsA in olive oil were applied to rabbit eyes. The amount of CsA in corneal and aqueous samples from eyes treated with CsA castor oil and CsA olive oil were compared with each other and with collagen shield treated eyes. CsA concentrations were measured by radioimmunoassay. After the total dose of 6 mg CsA, percentage penetration was measured as follows: CsA castor oil--0.51% in aqueous and 20.75% in cornea; CsA olive oil--0.17% in aqueous and 11.13% in cornea; and with collagen shields--0.44% in aqueous and 11.84% in cornea. These results show that the CsA levels of castor oil drops were higher than those obtained with olive oil drops. In eyes with collagen shields, CsA levels were higher than olive oil drops but nearly equal to the castor oil drops. Collagen shields may be useful as an ocular delivery system for CsA.

摘要

我们使用市售的12小时胶原盾,将环孢素A(CsA)递送至兔眼的角膜和房水中。六只新西兰白兔被分为三组。第一组(四只眼)接受蓖麻油中6毫克的CsA,第二组(四只眼)在12小时内接受橄榄油中6毫克的CsA作为局部滴眼液滴入兔眼。第三组(四只眼)将浸泡在橄榄油中6毫克CsA的12小时胶原盾应用于兔眼。将用CsA蓖麻油和CsA橄榄油处理的眼睛的角膜和房水样本中的CsA量相互比较,并与胶原盾处理的眼睛进行比较。通过放射免疫测定法测量CsA浓度。在给予6毫克CsA的总剂量后,测量穿透百分比如下:CsA蓖麻油——房水中为0.51%,角膜中为20.75%;CsA橄榄油——房水中为0.17%,角膜中为11.13%;胶原盾——房水中为0.44%,角膜中为11.84%。这些结果表明,蓖麻油滴剂的CsA水平高于橄榄油滴剂。在使用胶原盾的眼中,CsA水平高于橄榄油滴剂,但几乎与蓖麻油滴剂相等。胶原盾可能作为CsA的眼部给药系统有用。

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