利奈唑胺滴眼液在兔眼角膜内的药动学

Pharmacokinetics of Linezolid in Ocular Cornea of Rabbit

摘要: 目的探讨利奈唑胺滴眼液单次滴兔眼后在角膜中的药动学特征。方法 40只新西兰大白兔，局部滴入利奈唑胺滴眼液50 mL，采用高效液相色谱法测定兔眼角膜中利奈唑胺的药物浓度，用DAS 2.1.1软件计算药动学参数。结果给药后0~120 h，利奈唑胺在兔眼角膜中的最高浓度为(58.62±15.48)μg·g^-1，消除半衰期t_1/2为(38.09±11.59)h，药时曲线下面积AUC_0-t为(2 459.02±508.95)μg·h·g^-1，AUC_0-∞为(2 834.13±578.96)μg·h·g^-1。结论利奈唑胺滴眼液单次滴兔眼后在角膜中具有良好的药代动力学特征和组织通透性。

Abstract: OBJECTIVE To study pharmacokinetics of linezolid in ocular cornea of rabbit after ocular instillation. METHODS Forty New England rabbits were topically applied 50 mL of linezolid eye drops. Ocular cornea was sampled at different intervals after drug instillation, and the drug levels were assayed by HPLC. The pharmacokinetics parameters were figured out by DAS 2.1.1 process. RESULTS The peak concentration of linezolid in cornea was (58.62±15.48)μg·g^-1 in 0-120 h. The t_1/2 was (38.09±11.59)h. The AUC_0-t was (2 459.02±508.95)μg·h·g^-1, and AUC_0-∞ was (2 834.13±578.96)μg·h·g^-1. CONCLUSION Linezolid has a good pharmacokinetics character and permeability in ocular cornea of rabbit.