透明质酸对左氧氟沙星滴眼液眼部吸收的促进作用

Pharmacokinetics and bioavailability of levofloxacin-SA in rabbit eyes

目的:考察0.3%的左氧氟沙星透明质酸滴眼液与0.5%普通左氧氟沙星滴眼液的眼部药动学行为,比较二者的相对生物利用度和眼组织分布特性,评价透明质酸对左氧氟沙星滴眼液的药动学和组织分布的影响。方法:采用新西兰大白兔,双侧眼滴入药物后,于不同时间取房水、角膜和结膜。高效液相色谱法测定各组织样本中的左氧氟沙星药物浓度,计算药物在不同组织中的药动学参数。结果:利用高效液相色谱法可以很好的测定房水、角膜和结膜中左氧氟沙星的药物浓度,经计算,0.3%的左氧氟沙星透明质酸滴眼液组的房水、角膜和结膜中药物浓度-时间曲线下面积AUC0-240分别是普通滴眼液组的187%、125%和114%。结论:0.3%左氧氟沙星透明质酸滴眼液相对于0.5%普通左氧氟沙星滴眼液生物利用度有显著提高,透明质酸显著提高药物在眼部各组织的吸收。

OBJECTIVE The pharmacokinetics and biodistribution of 0. 3% levofloxacin-hyaluronic acid eye drops and 0. 5% levofloxacin eye drops were observed to evaluate the hyaluronic acid＇s biological effect in ophthalmic solutions. METHODS 0. 3% levofloxacin-SA and 0. 5 % levofloxaein eye drops was dropped binocularly in New Zealand rabbits. The rabbit aqueous humor, corneas and conjunctivas were collected at 5, 10, 15, 30, 45, 60, 120, 180 and 240 minutes for the quantification analysis of drugs by reverse phase high performance liquid chromatography （HPLC）. The pharmacokinetic parameters were calculated. RESULTS The areas under curve （AUG0-240 ） of levofloxacin-SA in aqueous humor, corneas and conjunctivas were 1.87, 1.25, 1. 14 times higher than those of common 0. 5% levofloxacin. CONCLUSION The ocular bioavailability of 0. 3% levofloxacin-hyaluronic acid eye drops was significantly higher than that of 0. 5% levofloxacin eye drops.