Department of Ophthalmology, Gavin Herbert Eye Institute, University of California Irvine, Irvine, California 92697, USA.
Retina. 2013 Mar;33(3):522-31. doi: 10.1097/IAE.0b013e3182647f69.
To compare the durability of Kenalog, Trivaris, Triesence, and compounding pharmacy preservative-free triamcinolone acetonide in pigmented rabbits with syneretic vitreous using direct visualization, pharmacodynamics, and pharmacokinetics.
Twenty-five Dutch-belted rabbits were used. Pharmacokinetic experiment: Rabbits were intravitreally injected with one of four 4-mg triamcinolone acetonide formulations. Wide-field imaging was serially performed to document residual drug mass. Pharmacodynamics experiment: Four triamcinolone acetonide groups and one control group received intravitreal recombinant human vascular endothelial growth factor 165 every 2 weeks and were followed with fluorescein angiography to assess vascular endothelial growth factor retinal vasculopathy as a measure of residual steroid effect. Particle size of the formulations was measured with Mastersizer 2000.
Remaining triamcinolone acetonide mass after 19 weeks: 12,091 ± 2,512 pixels for the Kenalog group, 1,307.36 ± 695.57 for Trivaris, 5577 ± 1477 for Triesence, and 1,535 ± 329 for compounded preservative-free triamcinolone acetonide. Kenalog suppressed recombinant human vascular endothelial growth factor-induced retinopathy more effectively than the other triamcinolone acetonide groups at Week 39, the final time point assessed. Particle size (90th percentile) was 47 μm for Kenalog, 26 μm for Triesence, and 22 μm for both compounded preservative-free triamcinolone acetonide and Trivaris.
Triamcinolone acetonide formulations do not have the same pharmacokinetics/pharmacodynamics. Kenalog has the longest vitreous visibility and durability. Particle size appears to correlate with efficacy and durability.
通过直接可视化、药效学和药代动力学比较在伴有增生性玻璃体视网膜病变的色素兔中 Kenalog、Trivaris、Triesence 和复方无防腐剂曲安奈德的耐用性。
使用 25 只荷兰兔。药代动力学实验：兔子玻璃体腔内注射四种 4mg 曲安奈德制剂之一。进行宽场成像以连续记录残留药物质量。药效学实验：四组曲安奈德组和一组对照组每 2 周接受玻璃体腔内重组人血管内皮生长因子 165，并进行荧光血管造影以评估血管内皮生长因子视网膜血管病变作为残留类固醇作用的衡量标准。用 Mastersizer 2000 测量制剂的粒径。
19 周后剩余的曲安奈德质量：Kenalog 组为 12091±2512 像素，Trivaris 组为 1307.36±695.57，Triesence 组为 5577±1477，复方无防腐剂曲安奈德组为 1535±329。Kenalog 在第 39 周（最后一次评估时间点）时比其他曲安奈德组更有效地抑制了重组人血管内皮生长因子诱导的视网膜病变。粒径（90%分位数）为 Kenalog 47μm，Triesence 26μm，复方无防腐剂曲安奈德和 Trivaris 均为 22μm。
曲安奈德制剂的药代动力学/药效学并不相同。Kenalog 具有最长的玻璃体可见度和耐用性。粒径似乎与疗效和耐用性相关。
