Intraocular Pharmacokinetics of Ranibizumab Following a Single Intravitreal Injection in Humans
Intraocular Pharmacokinetics of Ranibizumab Following a Single Intravitreal Injection in Humans
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DOI：
10.1016/j.ajo.2012.03.047
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发表时间：
2012-10-01
影响因子：
4.2
通讯作者：
Meyer, Carsten H.
中科院分区：
文献类型：
--
作者：
Krohne, Tim U.;Liu, Zengping;Meyer, Carsten H.
目的：研究单次玻璃体内注射雷尼比单抗的眼内药物浓度和药代动力学。设计：前瞻性、非对照、干预性病例系列。方法：18例(年龄61~85岁)未行玻璃体切除手术的患者，均被诊断为继发于渗出性老年性黄斑变性、糖尿病黄斑病变或视网膜静脉阻塞的有临床意义的白内障和黄斑水肿。每只眼只接受一次玻璃体内注射0.5毫克的雷比珠单抗。在注药后1至37天的白内障手术中采集房水样本。结果：雷尼比珠单抗在房水中的浓度在注射后第1天达到峰值(范围为36.9-66.1µg/mL)，随后呈单指数下降。经非线性回归分析，初峰浓度(c(Max))为56.1微克/毫升，消除半衰期(t(1/2))为7.19天，决定系数(R-2)为0.90。根据眼轴测量计算的眼体积雷尼比珠单抗浓度的校正没有显著改变回归分析结果(t(1/2)，7.15天；R-2，0.89)。结论：在未玻璃体切除的人眼中，玻璃体内注射0.5 mg雷尼比珠单抗的房水半衰期为7.19天，略短于先前通过可比方法测定的贝伐单抗9.82天的半衰期。《眼科杂志》2012；154：682-686。(C)2012年由Elsevier Inc.保留所有权利。)
PURPOSE: To investigate intraocular concentrations and pharmacokinetics of ranibizumab after a single intravitreal injection in humans.DESIGN: Prospective, noncomparative, interventional case series.METHODS: We included 18 nonvitrectomized eyes of 18 patients (age range, 61-85 years) that were diagnosed with both clinically significant cataract and macular edema secondary to either exudative age-related macular degeneration, diabetic maculopathy, or retinal vein occlusion. Each eye received a single intravitreal injection of 0.5 mg ranibizumab. An aqueous humor sample was obtained during cataract surgery between 1 and 37 days after injection. Concentrations of unbound ranibizumab in these samples were quantified by enzyme-linked immunosorbent assay.RESULTS: Ranibizumab concentration in aqueous humor peaked the first day after injection (range, 36.9-66.1 mu g/mL) and subsequently declined in a mono-exponential fashion. Nonlinear regression analysis determined an initial peak concentration (c(max)) of 56.1 mu g/mL and an elimination half-life (t(1/2)) of 7.19 days with a coefficient of determination (R-2) of 0.90. Correction of ranibizumab concentrations for ocular volume as calculated from axial length measurements did not alter regression analysis results significantly (t(1/2), 7.15 days; R-2, 0.89).CONCLUSIONS: In human nonvitrectomized eyes, the aqueous half-life of 0.5 mg intravitreally injected ranibizumab is 7.19 days, slightly shorter than the half-life of 9.82 days previously determined for bevacizumab by comparable methods. (Am J Ophthalmol 2012;154: 682-686. (C) 2012 by Elsevier Inc. All rights reserved.)