Osmolarity of Prevalent Eye Drops, Side Effects, and Therapeutic Approaches
Osmolarity of Prevalent Eye Drops, Side Effects, and Therapeutic Approaches
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DOI：
10.1097/ico.0000000000000368
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发表时间：
2015-05-01
期刊：
影响因子：
2.8
通讯作者：
Schrage, Norbert
中科院分区：
文献类型：
--
作者：
Dutescu, Ralf M.;Panfil, Claudia;Schrage, Norbert
目的：眼用制剂的渗透压如何影响眼表，目前知之甚少。由于高渗滴眼液可用于治疗角膜水肿，因此本文提出了一种基于渗透压的体外角膜水肿模型，用于眼科药物的检测。本文还对德国市场上常见眼药水的渗透压进行了分析。方法：为了模拟角膜水肿，使用Ex Vivo Eye刺激性试验来模拟具有生理角膜屏障的眼前房。前房注入148mOsm/L低渗液24小时，造成角膜水肿。在该模型中，将保存的和不保存的5%氯化钠(高渗的Omnisorb和5%UD的Ocusalin)分别作用于5只角膜，观察其减轻角膜水肿的效果。用光学相干断层扫描仪测定角膜厚度。结果：在体外实验条件下，受试低渗液引起的角膜水肿从基线的450µm(+/-50µm)增加到851µm(+/-94µm，P<；0.0001)。欧米索尔组和5%奥沙林组的角膜厚度分别减少了279µm(+/-28µm，P<0.001)和258µm(+/-29µm，P<0.001)。43个(49%)产品的渗透压低于289mOsm/L的生理泪液渗透压，44个(51%)高于289mOsm/L的生理泪液渗透压，润滑剂滴液中的渗透压低于200mOsm/L。渗透压最高的是Omnisorb(1955mOsm/L)。结论：体外眼刺激试验是一种可靠的角膜水肿模型，可用于评价渗透眼药水。渗透压测量显示，常见眼科药物的渗透压范围很广，从低渗到高渗。
Purpose: Little is known about how the osmolarity of ophthalmic formulations affects the ocular surface. Because hyperosmolar eye drops could be therapeutic for treating corneal edema, this article presents an ex vivo model of corneal edema for testing ophthalmic drugs based on their osmolarity. The respective osmolarity of common eye drops found in the German market is also analyzed here.Methods: For modeling corneal edema, an Ex Vivo Eye Irritation Test was used to simulate an ocular anterior chamber with a physiological corneal barrier. To induce corneal edema, the anterior chamber was supplied with a hypoosmolar medium (148 mOsm/L) for 24 hours. Preserved and preservative-free 5% sodium chloride (hyperosmolar Omnisorb and Ocusalin 5% UD) were used for 1 hour, on 5 corneas each, to test their efficiency to reduce corneal edema in this model. Corneal thickness was determined by optical coherence tomography. Osmolarity of 87 common eye drops was measured by freezing point osmometry.Results: Ex vivo, the tested hypoosmolar condition induced corneal edema from 450 mu m (+/- 50 mu m) at baseline to 851 mu m (+/- 94 mu m, P < 0.0001). Omnisorb and Ocusalin 5% UD significantly reduced the corneal thickness by 279 mu m (+/- 28 mu m, P < 0.001) for Omnisorb and 258 mu m (+/- 29 mu m, P, 0.001) for Ocusalin 5% UD. Forty-three (49%) of the tested products had an osmolarity below and 44 (51%) above the physiological tear osmolarity of 289 mOsm/L. Osmolarity values of less than 200 mOsm/L were found in lubricant drops. The highest osmolarity was detected in Omnisorb (1955 mOsm/L).Conclusions: The Ex Vivo Eye Irritation Test has proven to be a reliable novel model of corneal edema for evaluating osmotic eye drops. Osmolarity measurements revealed a wide range from hypotonic to hypertonic formulations for commonly marketed ophthalmic drugs.