兔眼内注射甲氨蝶呤的药代动力学实验研究。
Intravitreal injection of methotrexate in an experimental rabbit model: determination of pharmacokinetics.
机构信息
Department of Ophthalmology, University of Cukurova, Adana, Turkey.
出版信息
Indian J Ophthalmol. 2011 May-Jun;59(3):197-200. doi: 10.4103/0301-4738.81026.
PURPOSE
To investigate the pharmacokinetics of intravitreally administered methotrexate.
MATERIALS AND METHODS
Twenty-one New Zealand white rabbits were used in the study. The pharmacokinetics of intravitreally injected 800 μg/0.1 ml of methotrexate was investigated. Intravitreal concentration of the drug was measured at seven different times, in six eyes at each occasion, on a total of 42 eyes of 21 rabbits from a period of 30 minutes to 72 hours.
RESULTS
The volume of distribution was calculated as 1.33 ml following intravitreal injection of 800 μg methotrexate. Vitreous concentrations of the drug were found to be decreasing related to the specific mathematical equation; drug concentration= 1426.73 e -0.1182(time) and remained over effective dose by 81 hours with a half life of 5.9 hours.
CONCLUSIONS
These findings evidenced those vitreous levels of methotrexate at various time intervals after 800 μg intravitreal injections which formulated a mathematical equation for calculation of vitreous level of the drug at each hour.
目的
研究玻璃体内给予甲氨蝶呤的药代动力学。
材料和方法
本研究使用了 21 只新西兰白兔。研究了玻璃体内注射 800μg/0.1ml 甲氨蝶呤后的药代动力学。在总共 42 只 21 只兔子的 72 小时内的 30 分钟至 72 小时的七个不同时间点，在六个眼睛的每个时间点测量药物的眼内浓度。
结果
玻璃体内注射 800μg 甲氨蝶呤后，分布容积计算为 1.33ml。发现眼内药物浓度与特定的数学方程呈下降相关；药物浓度=1426.73e-0.1182（时间），半衰期为 5.9 小时，有效剂量持续 81 小时。
结论
这些发现证明了在玻璃体内注射 800μg 后不同时间间隔的眼内甲氨蝶呤水平，为计算每个小时眼内药物水平制定了数学方程。
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