Ocular pharmacokinetic study of a corticosteroid by 19F MR.
Ocular pharmacokinetic study of a corticosteroid by 19F MR.
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DOI：
10.1016/j.exer.2010.05.022
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发表时间：
2010-09
影响因子：
3.4
通讯作者：
Jeong, Eun-Kee
中科院分区：
文献类型：
--
作者：
Liu, Xin;Li, S. Kevin;Jeong, Eun-Kee
传统的眼部药代动力学研究是侵入性的，不容易应用于人体活体。为了非侵入性地获取活体眼部药代动力学数据，使用3T临床扫描仪上的19F磁共振来跟踪眼部皮质类固醇的实时动力学。同时行1HMR检查，以确定给药部位。模型药物为曲安奈德磷酸盐(TAP)，通过玻璃体内和结膜下注射给药。通过眼内药物的~(19)F谱的变化实时监测TAP的药代动力学。TAP在体内的消除半衰期分别为8h和0.5h，死后分别为17h和6.0h。玻璃体内给药的半衰期为14h，结膜下给药的半衰期为0.5h。
Traditional ocular pharmacokinetic studies are invasive and cannot be easily applied to humans in vivo. To acquire in vivo ocular pharmacokinetic data noninvasively, 19F MR on a 3T clinical scanner was used to follow the real time dynamics of a corticosteroid in the eye. 1H MR was also performed to locate the site of administration. Triamcinolone acetonide phosphate (TAP) was the model drug, administered by intravitreal and subconjunctival injections. TAP pharmacokinetics were monitored by changes in the 19F spectrum of the intraocular drug in real time. The elimination half-lives of TAP in the eye after intravitreal and subconjunctival injections were 8 and 0.5 h in vivo and 17 and 6.0 h postmortem, respectively. The half-lives associated with clearance were 14 h for intravitreal injection and 0.5 h for subconjunctival injection.
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