| 加替沙星眼用凝胶制剂与加替沙星滴眼液兔眼药动学的比较 |
| 投稿时间：2016-06-23 修订日期：2016-06-30 点此下载全文 |
| 引用本文：孙飒,周天洋,夏慧云,何继军,王丽娅,唐海,张俊杰.加替沙星眼用凝胶制剂与加替沙星滴眼液兔眼药动学的比较[J].医学研究杂志,2017,46(2):116-119 |
| DOI：
10.11969/j.issn.1673-548X.2017.02.030 |
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| 中文摘要:目的 比较加替沙星眼用凝胶制剂（G组）和加替沙星滴眼液（D组）单次给药后兔眼角膜、结膜和房水中的药物浓度。方法 日本大耳白兔双眼给药，分别于给药后5、10、15、30、45、60、120、180、240和360min处死兔子，采集角膜、结膜和房水，反相高效液相色谱法测定药物浓度。结果 G组角膜、结膜和房水中药物的达峰时间分别为10、10和60min；达峰浓度则分别为36.065±16.728μg/g、37.460±16.333μg/g和3.010±0.658μg/ml；G组各组织中4h前所有时间点的药物浓度均显著高于D组对应时间点的药物浓度（P<0.05）；AUC（0~360）分别为2296.617μg/（g·min）、1402.143μg/（g·min）和271.558μg/（ml·min），分别是D组相应组织中加替沙星AUC（0~360）的4.7、8.6和4.1倍。结论 加替沙星眼用凝胶与加替沙星滴眼液相比，可在兔眼结膜、角膜及房水中达到更高的药物浓度，进入兔眼组织和房水的速度更快。 |
| 中文关键词:加替沙星 眼用凝胶 药动学 |
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| Comparion of the Pharmacokinetics of Gatifloxacin Ophthalmic Gel with Gatifloxacin Rye Drops in Rabbbits |
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| Abstract:Objective To investigate and compare the concentrations in aqueous humor,cornea and conjunctiva after gatifioxacin ophthalmic gel and gatifilxacin eye drops single dose in rabbits. Methods Japanese white rabbit's eyes were topically applied with gatifioxacin ophthalmic gel or gatifilxacin eye drops according to groups and rabbits were sacrificed 5,10,15,30,45,60,120,180,240 and 360min after medication.Then aqueous humor,cornea and conjunctiva were obtained.All samples were analyzed by reversed-phase high performance liquid chromatography. Results In G group the drug concentration in cornea,conjunctiva and aqueous humor peaked at 10min(36.065±16.728μg/g),10min(37.460±16.333μg/g) and 60min(3.010±0.658μg/ml) respectively.G group maintained significantly higher concentrations before 4h in cornea、conjunctiva and aqueous humor as compared to D group(P<0.05).The AUC(0-360) of the drug level in tissue samples were 2296.617μg/(g·min),1402.143μg/(g·min) and 271.558μg/(ml·min) and 4.7 fold,8.6 fold and 4.1 fold higher as compared to D group in the corresponding eye tissue. Conclusion The concentrations of gatifloxacin ophthalmic gel were increased more significantly and which penetrated more fastely into cornea、conjunctiva and aqueous humor compared with gatifloxacin eye drops. |
| keywords:Gatifloxacin Ophthalmic gel Pharmacokinetics |
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