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目的探讨西罗莫司滴眼液单次滴兔眼后在房水中的药动学特征。方法 40只新西兰大白兔,局部滴入西罗莫司滴眼液50μL,采用高效液相色谱法测定兔眼房水中西罗莫司的药物浓度,用DAS1.0软件计算药动学参数。结果给药后0～120 h,西罗莫司在兔眼房水中的ρ_(max)为(84.92±37.04)μg·mL~(-1)(-1),t_(1/2)为(43.28±18.11)h,AUC_(0-6)为(1 747.44±571.36)μg·h·mL~(-1),AUC_(0-∞)为(2 335.25±702.42)μg·h·mL~(-1)。空白房水不干扰西罗莫司的含量测定。结论单次滴眼后西罗莫司可以快速穿透眼组织到达前房,并在房水中达到较高的药物浓度。
Objective To investigate the pharmacokinetics of sirolimus in aqueous humor after a single drop of rabbit eye. Methods 40 New Zealand white rabbits were treated with local injection of 50 μL of sirolimus eye drops. The drug concentration of sirolimus in rabbit aqueous humor was determined by HPLC. Pharmacokinetic parameters were calculated by DAS 1.0 software. Results ρ max of sirolimus in aqueous humor of rabbits was (84.92 ± 37.04) μg · mL -1 (-1) and t 1/2 was (0-120) 43.28 ± 18.11) h, AUC_ (0-6) was (1 747.44 ± 571.36) μg · h · mL -1 and AUC_ (0-∞) was (2 335.25 ± 702.42) μg · h · mL ~ -1). Blank room water does not interfere with the determination of sirolimus content. Conclusion After a single eye drop, sirolimus can rapidly penetrate the ocular tissue to reach the anterior chamber and reach a higher drug concentration in aqueous humor.