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抗肿瘤药物1,3-双(2-氯乙基)-1-亚硝基脲(BCNU)在兔眼房水和玻璃体中的药代动力学

Pharmacokinetics of the antineoplastic agent 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in the aqueous and vitreous of rabbit.

作者信息

Ueno N, Refojo M F, Liu L H

出版信息

Invest Ophthalmol Vis Sci. 1982 Aug;23(2):199-208.

PMID:7096015
Abstract

1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU), an anticancer drug, was assayed in the aqueous and vitreous of rabbits after intravenous injection, subconjunctival injection, and topical application. Pharmacokinetic parameters were calculated from the time-course curves. The penetration into aqueous and vitreous across the blood-aqueous barrier and the blood-retinal barrier after intravenous injection was related to the anatomic dimensions of the eye (the volume of tissue involved and the surface area through which BCNU diffuses). To evaluate the three routes of administration, the area under the time-course curve was calculated from the simulated time-course curve. The results suggest that topical application of BCNU is the best and subconjunctival injection the second best route for treating an iris tumor, and that intravenous injection is the best route for choroidal and retinal tumors.

摘要

1,3-双(2-氯乙基)-1-亚硝基脲(卡莫司汀,BCNU)是一种抗癌药物,在兔静脉注射、结膜下注射和局部应用后,对其在房水和玻璃体中的含量进行了测定。根据时间进程曲线计算药代动力学参数。静脉注射后,BCNU通过血-房水屏障和血-视网膜屏障进入房水和玻璃体的情况与眼睛的解剖学尺寸(涉及的组织体积和BCNU扩散通过的表面积)有关。为了评估这三种给药途径,根据模拟的时间进程曲线计算时间进程曲线下的面积。结果表明,对于虹膜肿瘤的治疗,BCNU局部应用是最佳途径,结膜下注射是次佳途径;对于脉络膜和视网膜肿瘤,静脉注射是最佳途径。

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Pharmacokinetics of the antineoplastic agent 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in the aqueous and vitreous of rabbit.抗肿瘤药物1,3-双(2-氯乙基)-1-亚硝基脲(BCNU)在兔眼房水和玻璃体中的药代动力学
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引用本文的文献

1
Sustained release of carmustine (BCNU) for treatment of experimental intraocular malignancy.卡莫司汀(BCNU)缓释剂用于治疗实验性眼内恶性肿瘤
Br J Ophthalmol. 1983 Jul;67(7):479-84. doi: 10.1136/bjo.67.7.479.
2
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.