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玻璃体内注射贝伐单抗在玻璃体切割眼中的药代动力学。

Pharmacokinetics of intravitreally injected bevacizumab in vitrectomized eyes.

机构信息

Department of Ophthalmology, Seoul National University College of Medicine, Seoul, Republic of Korea.

出版信息

J Ocul Pharmacol Ther. 2013 Sep;29(7):612-8. doi: 10.1089/jop.2013.0009. Epub 2013 Jun 4.

Abstract

PURPOSE

To compare the pharmacokinetics (PKs) of intravitreally injected bevacizumab in vitrectomized versus nonvitrectomized control rabbit eyes.

METHODS

Twenty-five-gauge pars plana vitrectomy without lensectomy was performed in 17 right rabbit eyes (V) and 18 nonvitrectomized right rabbit eyes served as controls (C). After 1.25 mg/0.05 mL intravitreal bevacizumab (IVB) injections, eyes were enucleated at 1 h, 1, 2, 5, 14, and 30 days after the injection and immediately frozen at -80°C. Bevacizumab concentrations were determined after separation of frozen vitreous and aqueous humor (AH) compartments using indirect enzyme-linked immunosorbent assay. Bevacizumab concentration-time data were analyzed to obtain PK data.

RESULTS

Vitreous clearance of IVB consisted of 2 phases, the first fast distribution and second slow elimination phase. Clearance of IVB was accelerated in V eyes only during the first phase and not in the second phase. The vitreous concentration percent ratios between V and C eyes were 94.7% (1 h), 70.5% (1 day), 89.2% (2 days), 94.2% (5 days), 99.2% (14 days), and 79.1% (30 days). Overall vitreous half-lives were 6.99 and 7.06 days for V and C eyes, respectively (1.6-h difference).

CONCLUSION

Overall IVB PKs in rabbit eyes after vitrectomy without lensectomy are not substantially different from nonvitrectomized control eyes.

摘要

目的

比较玻璃体切割术与非玻璃体切割术对照兔眼玻璃体内注射贝伐单抗的药代动力学(PKs)。

方法

在 17 只右眼(V 组)行 25 号经睫状体平坦部玻璃体切除术,不切除晶状体,18 只右眼作为非玻璃体切割术对照(C 组)。玻璃体内注射 1.25mg/0.05mL 贝伐单抗(IVB)后,于注射后 1h、1、2、5、14 和 30 天眼球摘除,立即于-80°C 冷冻。采用间接酶联免疫吸附法分离冷冻玻璃体和房水(AH)后,测定贝伐单抗浓度。分析贝伐单抗浓度-时间数据,得出 PK 数据。

结果

IVB 的玻璃体清除由 2 个相组成,第一相快速分布,第二相缓慢消除。仅在第一相中,V 眼中 IVB 的清除速度加快,而在第二相中则没有。V 眼与 C 眼玻璃体浓度比分别为 94.7%(1h)、70.5%(1d)、89.2%(2d)、94.2%(5d)、99.2%(14d)和 79.1%(30d)。V 眼和 C 眼的总体玻璃体半衰期分别为 6.99 和 7.06 天(相差 1.6 小时)。

结论

无晶状体玻璃体切除术后兔眼总体 IVB PKs 与非玻璃体切割术对照眼无明显差异。

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