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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Pharmacokinetics and safety of intravitreal caspofungin
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Pharmacokinetics and safety of intravitreal caspofungin

机译：玻璃体内卡泊芬净的药代动力学和安全性

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摘要

Caspofungin exhibits potent antifungal activities against Candida and Aspergillus species. The elimination rate and retinal toxicity of caspofungin were determined in this study to assess its pharmacokinetics and safety in the treatment of fungal endophthalmitis. Intravitreal injections of 50 -g/0.1 ml of caspofungin were administered to rabbits. Levels of caspofungin in the vitreous and aqueous humors were determined using high-performance liquid chromatography (HPLC) at selected time intervals (10 min and 1, 2, 4, 8, 16, 24, and 48 h), and the half-lives were calculated. Eyes were intravitreally injected with caspofungin to obtain concentrations of 10 -g/ml, 50 -g/ml, 100 -g/ml, and 200 -g/ml. Electroretinograms were recorded 4 weeks after injections, and the injected eyes were examined histologically. The concentrations of intravitreal caspofungin at various time points exhibited an exponential decay with a half-life of 6.28 h. The mean vitreous concentration was 6.06 - 1.76 -g/ml 1 h after intravitreal injection, and this declined to 0.47 - 0.15 -g/ml at 24 h. The mean aqueous concentration showed undetectable levels at all time points. There were no statistical differences in scotopic a-wave and b-wave responses between control eyes and caspo-fungin- injected eyes. No focal necrosis or other abnormality in retinal histology was observed. Intravitreal caspofungin injection may be considered to be an alternative treatment for fungal endophthalmitis based on its antifungal activity, lower retinal toxicity, and lower elimination rate in the vitreous. More clinical data are needed to determine its potential role as primary therapy for fungal endophthalmitis.
机译：卡泊芬净具有针对念珠菌和曲霉菌的有效抗真菌活性。在这项研究中确定了卡泊芬净的消除率和视网膜毒性，以评估其在真菌性眼内炎治疗中的药代动力学和安全性。给兔子玻璃体内注射50μg/ 0.1ml卡泊芬净。在选定的时间间隔（10分钟和1、2、4、8、16、24和48小时）使用高效液相色谱（HPLC）测定玻璃体和房水中的卡泊芬净水平被计算。向玻璃体内注射卡泊芬净，以得到10 -g / ml，50 -g / ml，100 -g / ml和200 -g / ml的浓度。注射后4周记录视网膜电图，并对注射的眼睛进行组织学检查。玻璃体内卡泊芬净的浓度在不同时间点呈指数衰减，半衰期为6.28 h。玻璃体内注射后1 h，玻璃体平均浓度为6.06-1.76 -g / ml，24 h降至0.47-0.15 -g / ml。平均水浓度在所有时间点均显示出不可检测的水平。对照眼和经卡斯波夫菌素注射的眼睛之间的暗视a波和b波反应无统计学差异。在视网膜组织学中未观察到局灶性坏死或其他异常。玻璃体腔注射卡泊芬净可因其抗真菌活性，较低的视网膜毒性和较低的玻璃体清除率而被认为是真菌性眼内炎的替代疗法。需要更多的临床数据来确定其作为真菌性眼内炎主要疗法的潜在作用。

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