Bucci Laser Vision Institute, Wilkes-Barre, PA 18702, USA.
Curr Med Res Opin. 2011 Dec;27(12):2235-9. doi: 10.1185/03007995.2011.626018. Epub 2011 Oct 12.
To compare the peak to-aqueous penetration of three nonsteroidal anti-inflammatory drugs: ketorolac tromethamine 0.45%, bromfenac 0.09%, nepafenac 0.1%, and amfenac (the active metabolite of nepafenac) in patients undergoing phacoemulsification.
A single center, double-masked study randomized 122 patients to receive one of three treatment arms. On-label dosing of ketorolac (BID), bromfenac (BID), and nepafenac (TID) was instructed for 1 day prior to surgery. Patients were instructed to instill one drop the morning of surgery. The patients received four additional doses 1 hour prior to phacoemulsification. After completion of the paracentesis site with a superblade, aqueous humor (0.15 cc) was collected through the peripheral clear cornea with a 30-gauge needle attached to a TB syringe. Following collection, aqueous samples were stored at -40°C prior to analysis. Drug concentrations were analyzed by liquid chromatography tandem mass spectrometry using positive turbo-ion spray ionization and multiple reaction monitoring mode for quantification. An independent sample Student's t-test was used to detect between-group differences.
The peak aqueous concentration of ketorolac 0.45% was 10 times the concentration of bromfenac 0.09%, and five times the concentration of and 54% greater than the metabolically inactive nepafenac 0.1%. The mean peak aqueous concentration of ketorolac 0.45% was 688.87 ± 749.6 ng/ml. Bromfenac achieved a mean peak aqueous concentration of 67.64 ± 62.4 ng/ml. The mean peak aqueous concentrations of nepafenac and amfenac were 447.10 ± 225.7 ng/ml and 140.37 ± 56.6 ng/ml, respectively. The peak concentration of ketorolac was statistically significantly greater than bromfenac (P ≤ 0.0005), nepafenac (P ≤ 0.05), and amfenac (P ≤ 0.005). A limitation of this study is that aqueous samples were collected just prior to surgery and not during the postoperative period due to ethical considerations.
Ketorolac 0.45% achieved significantly greater aqueous concentrations when compared to bromfenac 0.09% and the active metabolite of nepafenac 0.1% (amfenac) in patients undergoing phacoemulsification.
比较三种非甾体抗炎药（酮咯酸氨丁三醇 0.45%、溴芬酸 0.09%、奈帕芬酸 0.1%和奈帕芬酸的活性代谢物氨芬酸）在接受超声乳化术的患者中的峰至房水穿透率。
这是一项单中心、双盲研究，将 122 名患者随机分为 3 个治疗组。在手术前一天，按标签剂量给予酮咯酸（bid）、溴芬酸（bid）和奈帕芬酸（tid）。告知患者在手术当天早上滴注一滴。在完成超刀片的房水穿刺部位后，通过连接 TB 注射器的 30 号针头从周边透明角膜采集 0.15 毫升房水。收集后，将房水样本储存在-40°C 下，以备分析。通过正离子涡轮喷雾电离和多重反应监测模式的液相色谱串联质谱法分析药物浓度，用于定量。采用独立样本学生 t 检验检测组间差异。
酮咯酸 0.45%的峰值房水浓度是溴芬酸 0.09%的 10 倍，是代谢无活性的奈帕芬酸 0.1%的 5 倍，比其高出 54%。酮咯酸 0.45%的平均峰值房水浓度为 688.87±749.6ng/ml。溴芬酸达到的平均峰值房水浓度为 67.64±62.4ng/ml。奈帕芬酸和氨芬酸的平均峰值房水浓度分别为 447.10±225.7ng/ml和 140.37±56.6ng/ml。酮咯酸的峰值浓度显著高于溴芬酸（P≤0.0005）、奈帕芬酸（P≤0.05）和氨芬酸（P≤0.005）。本研究的一个局限性是，由于伦理考虑，房水样本仅在手术前采集，而不在术后采集。
在接受超声乳化术的患者中，与溴芬酸 0.09%和奈帕芬酸的活性代谢物 0.1%（氨芬酸）相比，酮咯酸 0.45%的房水浓度显著更高。
