Panahi Yunes, Naderi Mostafa, Jadidi Khosrow, Hoseini Hadise, Abrishami Mojtaba
Chemical Injuries Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.
Eye Research Center, Farabi Eye Hospital, Tehran University of Medical Sciences, Tehran, Iran.
Int Ophthalmol. 2018 Feb;38(1):99-104. doi: 10.1007/s10792-016-0428-8. Epub 2017 Jan 10.
Nonsteroidal anti-inflammatory drugs (NSAIDs), as an alternative, are replacing corticosteroids in ocular inflammatory diseases. Diclofenac has been used mainly topically, and recent focus has been on intravitreal delivery. Both of these methods have been shown to have complications in long-term application.
To assess the efficacy of slow release oral diclofenac sodium on intravitreal concentration in experimental model of chemically injured eyes.
In an experimental double-masked clinical trial, right eyes of 24 albino rabbits were chemically injured by 1 N NaOH. One hour after chemical injury, 10 cc suspension gavage containing 100 mg slow release diclofenac sodium was administered in all cases. 2, 4, 6, 12, 24, 48 h after gavage, vitreous samples were obtained in all cases. Intravitreal concentration of diclofenac sodium was evaluated in all samples using high-performance liquid chromatography (HPLC) method.
Intravitreal diclofenac levels by oral intake were enhanced by the inflammation in all the measurements. In inflamed eyes, diclofenac concentration was ten times more than control eye (2.658 ± 0.344 vs. 0.242 ± 0.0279 and 1.617 ± 0.527 vs. 0.148 ± 0.095; in 2 and 4 h, respectively). After 6 h, diclofenac concentration was statistically different, although it reduced below 1 μg/ml.
Diclofenac is delivered to the inflamed eye more than healthy eye. It seems that by oral diclofenac consumption, it is possible to make a significant intravitreal concentration.
非甾体类抗炎药（NSAIDs）作为一种替代药物，正在取代皮质类固醇用于眼部炎症性疾病。双氯芬酸主要用于局部给药，近来人们的关注点在于玻璃体内给药。这两种方法在长期应用中均已显示出有并发症。
在化学性损伤眼的实验模型中评估缓释口服双氯芬酸钠对玻璃体内浓度的疗效。
在一项实验性双盲临床试验中，24只白化兔的右眼被1N氢氧化钠化学性损伤。化学损伤1小时后，所有病例均给予含100mg缓释双氯芬酸钠的10cc悬浮液灌胃。灌胃后2、4、6、12、24、48小时，所有病例均采集玻璃体液样本。使用高效液相色谱（HPLC）法评估所有样本中双氯芬酸钠的玻璃体内浓度。
在所有测量中，口服摄入的双氯芬酸在玻璃体内的水平因炎症而升高。在炎症眼中，双氯芬酸浓度比对照眼高10倍（分别在2小时和4小时时为2.658±0.344对0.242±0.0279以及1.617±0.527对0.148±0.095）。6小时后，双氯芬酸浓度虽降至1μg/ml以下，但仍有统计学差异。
双氯芬酸在炎症眼中的递送量多于健康眼。看来通过口服双氯芬酸，有可能使玻璃体内达到显著浓度。
