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结膜下注射与静脉注射后5-氟尿嘧啶的药代动力学及代谢情况

Pharmacokinetics and metabolism of 5-fluorouracil following subconjunctival versus intravenous administration.

作者信息

Rootman J, Ostry A, Gudauskas G

出版信息

Can J Ophthalmol. 1984 Jun;19(4):187-91.

PMID:6744104
Abstract

Two groups of six rabbits each were given 6.25 mg/kg of 6-carbon-14-labelled 5-fluorouracil (5-FU) either subconjunctivally or intravenously. The levels of the drug in the serum, the urine and the ocular humours 0.5, 1, 2, 4, 8 and 12 hours later were measured by high-pressure liquid chromatography, which distinguished between 5-FU and its metabolites. The peak levels of the parent drug in the serum and the urine were similar with the two routes of administration; however, compared with intravenous injection, subconjunctival injection resulted in 125 and 380 times the peak concentration of 5-FU in the anterior chamber aqueous and the vitreous respectively.

摘要

将两组各六只兔子分别通过结膜下或静脉内给予6.25毫克/千克的6-碳-14标记的5-氟尿嘧啶(5-FU)。在给药后0.5、1、2、4、8和12小时,通过高压液相色谱法测量血清、尿液和眼房水中药物的水平,该方法可区分5-FU及其代谢产物。两种给药途径下,血清和尿液中母体药物的峰值水平相似;然而,与静脉注射相比,结膜下注射导致前房水和玻璃体中5-FU的峰值浓度分别是其125倍和380倍。

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Cancer Chemother Pharmacol. 1995;36(1):27-34. doi: 10.1007/BF00685728.
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Response of an ocular melanoma to subconjunctival injection of 5-thio-D-glucose or cis-platin.
眼部黑色素瘤对结膜下注射5-硫代-D-葡萄糖或顺铂的反应。
Br J Cancer. 1987 May;55(5):499-502. doi: 10.1038/bjc.1987.101.
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Ocular drug delivery. Pharmacokinetic considerations.眼部药物递送。药代动力学考量。
Clin Pharmacokinet. 1990 Apr;18(4):255-69. doi: 10.2165/00003088-199018040-00001.