玻璃体内注射依那西普的药代动力学及安全性
Pharmacokinetics and safety of intravitreally delivered etanercept.
作者信息
Fauser Sascha, Kalbacher Hubert, Alteheld Nils, Koizumi Kan, Krohne Tim U, Joussen Antonia M
机构信息
Abteilung für Netzhaut- und Glaskörperchirurgie des Zentrums für Augenheilkunde und Zentrum für Molekulare Medizin (ZMMK), Universität zu Köln, Joseph-Stelzmann-Strasse 9, 50931 Cologne, Germany.
出版信息
Graefes Arch Clin Exp Ophthalmol. 2004 Jul;242(7):582-6. doi: 10.1007/s00417-004-0895-x. Epub 2004 Mar 17.
BACKGROUND
The anti-inflammatory drug etanercept may be an effective therapeutic agent in diabetic retinopathy. In order to further evaluate its potential, the pharmacokinetics and safety of this drug after intravitreal delivery were investigated.
METHODS
After intravitreal administration of etanercept in rabbits, clinical examination, electroretinography (ERG), visually evoked potentials (VEP) and histology were evaluated. The pharmacokinetics and distribution of etanercept were analyzed using fluorescence-coupled protein at 0, 2, 4, and 8 weeks after injection in vitreous, retina, and choroid.
RESULTS
No adverse effects and signs of toxicity were found. Etanercept showed peak concentrations after 4 weeks in the retina and choroid.
CONCLUSIONS
Intravitreally delivered etanercept is safe and results in high concentrations in the retina and choroid over a long period of time.
背景
抗炎药物依那西普可能是治疗糖尿病性视网膜病变的有效药物。为了进一步评估其潜力，研究了玻璃体内注射该药物后的药代动力学和安全性。
方法
在兔眼玻璃体内注射依那西普后，评估临床检查、视网膜电图（ERG）、视觉诱发电位（VEP）和组织学。在注射后0、2、4和8周，使用荧光偶联蛋白分析玻璃体内、视网膜和脉络膜中依那西普的药代动力学和分布。
结果
未发现不良反应和毒性迹象。依那西普在视网膜和脉络膜中4周后达到峰值浓度。
结论
玻璃体内注射依那西普是安全的，并且能在很长一段时间内在视网膜和脉络膜中产生高浓度。
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