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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50μL,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(cmax)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AUC0～∞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。
Objective To investigate the pharmacokinetics of linezolid in ocular tissues after a single drop of rabbit eye. Methods Forty New Zealand white rabbits were treated with local instillation of linezolid 50 μL, and the drug concentration of linezolid in rabbit eyes, aqueous humor, cornea and conjunctiva was determined by high performance liquid chromatography (HPLC) Dynamic parameters. Results The peak cirefrin concentrations of linezolid in rabbits' tears, aqueous humor, cornea and conjunctiva were (0 861.15 ± 669.43) μg · g-1, (165.71 ± 115.04) The elimination half-life (t1 / 2) were (60.67 ± 25.59), (36.81 ± 37.39), (38.09 ± 11.59) and (19.85 ± 7.06) h respectively, the area under the drug-time curve was (4 211.92 ± 806.09) μg · h · g-1 and (1634.65 ± 1 174.85) μg · h · mL- 2 834.13 ± 578.96) μg · h · g-1, (3 883.84 ± 1 846.13) μg · h · g-1. Blank tears, aqueous humor, corneal and conjunctival endogenous substances do not interfere with linezolid determination. Conclusion Linezolid drops have good pharmacokinetic characteristics and tissue permeability in rabbit eyes after a single drop of rabbit eyes.