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使用胶原盾提高局部用妥布霉素的眼内生物利用度。

Enhancement of the ocular bioavailability of topical tobramycin with use of a collagen shield.

作者信息

Chen C C, Takruri H, Duzman E

机构信息

Chiron IntraOptics, Irvine, California 92718-1903.

出版信息

J Cataract Refract Surg. 1993 Mar;19(2):242-5. doi: 10.1016/s0886-3350(13)80949-2.

Abstract

We compared the ocular bioavailability in rabbits of 0.3% tobramycin applied with a collagen shield with eyedrop tobramycin application. Groups of rabbits received either (1) a collagen shield presoaked in tobramycin with a tobramycin drop before and after shield application (Shield) or (2) three drops of tobramycin (Drops). Postmortem samples of the cornea, conjunctiva, and aqueous humor were obtained at various intervals after shield application or drop instillation. The corneas in a second set of rabbits were anesthetized and then chemically abraded with n-heptanol before receiving the same two dosing regimens as in the groups with intact corneas. At nearly all times in all three tissues, the Shield groups had higher mean concentrations of tobramycin than the Drops groups. The area under the concentration-time curve for the Shield group relative to the Drops group was 5.0- to 16.1-fold greater for rabbits with intact corneas (P < .05), and 1.8- to 3.7-fold greater for rabbits with abraded corneas (P < .05). The use of collagen shields together with standard ophthalmic concentrations of tobramycin may be useful in achieving higher concentrations of topically delivered drugs into the anterior segment of the eye.

摘要

我们比较了兔眼应用含0.3%妥布霉素的胶原盾与滴眼剂妥布霉素的眼内生物利用度。兔分组后分别接受:(1) 预先浸泡在妥布霉素中的胶原盾,在应用胶原盾前后滴用妥布霉素滴眼液(胶原盾组);或 (2) 滴用三滴妥布霉素(滴眼剂组)。在应用胶原盾或滴入滴眼液后的不同时间间隔采集角膜、结膜和房水的死后样本。第二组兔的角膜先麻醉,然后用正庚醇化学擦伤,之后接受与角膜完整组相同的两种给药方案。在所有三个组织的几乎所有时间点,胶原盾组的妥布霉素平均浓度均高于滴眼剂组。胶原盾组相对于滴眼剂组的浓度-时间曲线下面积,角膜完整的兔高5.0至16.1倍(P <.05),角膜擦伤的兔高1.8至3.7倍(P <.05)。将胶原盾与标准眼科浓度的妥布霉素联合使用,可能有助于使局部给药的药物在眼前节达到更高浓度。

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