Krohne Tim U, Eter Nicole, Holz Frank G, Meyer Carsten H
Department of Ophthalmology, University of Bonn, Bonn, Germany.
Am J Ophthalmol. 2008 Oct;146(4):508-12. doi: 10.1016/j.ajo.2008.05.036. Epub 2008 Jul 17.
To investigate intraocular concentrations and pharmacokinetics of bevacizumab after a single intravitreal injection in humans.
Prospective, noncomparative, interventional case series.
We included 30 nonvitrectomized eyes of 30 patients (age range, 43 to 93 years) diagnosed with clinically significant cataract and concurrent macular edema secondary to neovascular age-related macular degeneration, diabetic retinopathy, or retinal venous occlusion in the same eye. All patients received an intravitreal injection of 1.5 mg bevacizumab. Between one and 53 days after injection, an aqueous humor sample was obtained during elective cataract surgery. Concentrations of unbound bevacizumab in these samples were quantified by enzyme-linked immunosorbent assay.
Concentration of bevacizumab in aqueous humor peaked on the first day after injection with a mean concentration (c(max)) of 33.3 microg/ml (range, 16.6 to 42.5 microg/ml) and subsequently declined in a monoexponential fashion. Nonlinear regression analysis determined an elimination half-time (t(1/2)) of 9.82 days (R(2) = 0.81). No significant differences between diagnosis subgroups were noted.
In human nonvitrectomized eyes, the aqueous half-life of 1.5 mg intravitreally injected bevacizumab is 9.82 days.
研究单次玻璃体内注射贝伐单抗后在人体内的眼内浓度及药代动力学。
前瞻性、非对比性、干预性病例系列研究。
我们纳入了30例患者（年龄范围43至93岁）的30只未行玻璃体切割术的眼睛，这些患者被诊断患有具有临床意义的白内障，并伴有同一眼的新生血管性年龄相关性黄斑变性、糖尿病性视网膜病变或视网膜静脉阻塞继发的黄斑水肿。所有患者均接受了1.5毫克贝伐单抗的玻璃体内注射。在注射后1至53天之间，在择期白内障手术期间采集房水样本。通过酶联免疫吸附测定法定量这些样本中游离贝伐单抗的浓度。
房水中贝伐单抗的浓度在注射后第一天达到峰值，平均浓度（c(max)）为33.3微克/毫升（范围为16.6至42.5微克/毫升），随后呈单指数方式下降。非线性回归分析确定消除半衰期（t(1/2)）为9.82天（R(2)=0.81）。各诊断亚组之间未观察到显著差异。
在人类未行玻璃体切割术的眼中，玻璃体内注射1.5毫克贝伐单抗的房水半衰期为9.82天。
