目的研究盐酸左氧氟沙星即形凝胶在兔眼内的药动学行为,考察该制剂的释药特征。方法以高效液相色谱法测定盐酸左氧氟沙星即形凝胶给药后不同时间兔眼房水中的药物浓度,绘制药-时曲线,计算药动学参数。结果盐酸左氧氟沙星即形凝胶在兔眼内的吸收和消除过程呈线性动力学特征,其t_1/2(ke),MRT,t_max,ρ_max,AUC_0-τ和AUC_0-∞分别为(118.76±7.21)min,(208.40±13.46)min,(34.07±5.02)min,(2.56±0.14)mg·L^-1,(432.05±13.55)mg·min·L^-1及(501.52±25.24)mg·min·L^-1。结论盐酸左氧氟沙星眼用即形凝胶显著延长药物在眼部的滞留时间,可用之实现长效治疗的目的。

OBJECTIVE To study the pharmacokinetics of levofloxacin hydrochloride in-situ gel in aqueous humors of rabbit eyes.METHODS Levofloxacin hydrochloride concentration in aqueous humors of rabbit eyes at different sampling time was determined after the dose of in-situ gel by RP-HPLC. The mean aqueous humors concentration-time curve of levofloxacin hydrochloride was discribed and pharmacokinetic parameters were calculated.RESULTS The absorption and elimination of levofloxacin hydrochloride were fitted to a linear model with the main pharmacokinetic parameters as follows: t_1/2(ke), MRT, t_max,ρ_max, AUC_0-τ and AUC_0-∞ were (118.76±7.21) min, (208.40±13.46) min, (34.07±5.02) min, (2.15±0.075) mg·L^-1, (432.05±13.55) mg·min·L^-1 and (501.52±25.24) mg·min·L^-1,respectively. CONCLUSION The release of levofloxacin hydrochloride in the eyes can be significantly prolonged by the in-situ gel.