利奈唑胺滴眼液兔眼内组织分布及其药动学

王延东,黄楚龙,曾夏芸,叶成添

中国药学杂志 ›› 2014, Vol. 49 ›› Issue (6) : 380-384.

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中国药学杂志 ›› 2014, Vol. 49 ›› Issue (6) : 380-384. DOI: 10.11669/cpj.2013.05.012
论 著

利奈唑胺滴眼液兔眼内组织分布及其药动学

  • 王延东1,黄楚龙1,曾夏芸2,叶成添1
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Pharmacokinetics of Linezolid in Rabbit Eyes

  • WANG Yan-dong1, HUANG Chu-long1, ZENG Xia-yun2, YE Cheng-tian1
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文章历史 +

摘要

目的 探讨利奈唑胺滴眼液单次滴兔眼后在眼组织中的药动学特征。 方法 40只新西兰大白兔,局部滴入利奈唑胺滴眼液50 μL,采用高效液相色谱法测定兔眼泪液、房水、角膜和结膜中利奈唑胺的药物浓度,用DAS2.1.1软件计算药动学参数。 结果 给药后0~120 h,利奈唑胺在兔眼泪液、房水、角膜和结膜中的达峰浓度( c max)分别为(2 861.15±669.43)μg·g-1、(165.71±115.04)μg·mL-1、(58.62±15.48) μg·g-1、(305.02±287.64)μg·g-1,消除半衰期t1/2分别为(60.67±25.59)、(36.81±37.39)、(38.09±11.59)、(19.85±7.06)h,药-时曲线下面积AUC0~∞为(4 211.92±806.09)μg·h·g-1、(1 634.65±1 174.85)μg·h·mL-1、(2 834.13±578.96)μg·h·g-1、(3 883.84±1 846.13)μg·h·g-1。空白泪液、房水、角膜和结膜中的内源性物质不干扰利奈唑胺的含量测定。 结论 利奈唑胺滴眼液单次滴兔眼后在兔眼组织中具有良好的药动学特征和组织通透性。

Abstract

Objective To study the pharmacokinetics of linezolid eye drops in rabbit eyes after a single dose administration. METHODS Forty New Zealand rabbits are topically applied 50 μL of linezolid eye drops. Ocular tears,aqueous humour,cornea and conjunctiva are sampled at different intervals after drug instillation,and the drug levels are assayed by HPLC. The pharmacokinetic parameters are calculated by DAS 2.1.1 process. RESULTS The peak concentrations of linezolid in tears,aqueous humour,cornea and conjunctiva are (2 861.15±669.43)μg·g-1,(165.71±115.04)μg·mL-1,(58.62±15.48) μg·g-1,and(305.02±287.64)μg·g-1,respectively. The half-lives of elimination are(60.67±25.59),(36.81±37.39),(38.09±11.59),and (19.85±7.06)h and AUC0~∞ are (4 211.92±806.09)μg·h·g-1,(1 634.65±1 174.85)μg·h·mL-1,(2 834.13±578.96)μg·h·g-1,and(3 883.84±1 846.13)μg·h·g-1,respectively. Blank tears,aqueous humour,cornea and conjunctiva didn’t interfere with the determination of linezolid. CONCLUSION Linezolid has a good pharmacokinetic character and permeability in rabbit eyes

关键词

利奈唑胺 / 滴眼液 / / / 药动学

Key words

linezolid / eye drop / rabbit / eye / pharmacokinetics

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导出引用
王延东,黄楚龙,曾夏芸,叶成添. 利奈唑胺滴眼液兔眼内组织分布及其药动学[J]. 中国药学杂志, 2014, 49(6): 380-384 https://doi.org/10.11669/cpj.2013.05.012
WANG Yan-dong, HUANG Chu-long, ZENG Xia-yun, YE Cheng-tian. Pharmacokinetics of Linezolid in Rabbit Eyes[J]. Chinese Pharmaceutical Journal, 2014, 49(6): 380-384 https://doi.org/10.11669/cpj.2013.05.012
中图分类号: R996.1   

参考文献

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