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首页> 外文期刊>European journal of ophthalmology >Rufloxacin eyedrops: Effect of different formulations on ocular pharmacokinetics in rabbits.
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Rufloxacin eyedrops: Effect of different formulations on ocular pharmacokinetics in rabbits.

机译：卢氟沙星滴眼液：不同制剂对兔眼药代动力学的影响。

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PURPOSE. To evaluate the aqueous humor pharmacokinetics of rufloxacin in rabbits after topical administration of different formulations, and to individuate the ones showing the best pharmacokinetic profile. METHODS. Six formulations were instilled in rabbit eyes: two pH 7.2 suspensions of non-salified rufloxacin base, or zwitterion (RUF), one of which was viscosized with tamarind seed polysaccharide (TSP); two pH 7.2 solutions of RUF obtained using hydroxypropyl-b-cyclodextrin (CD), one of which was viscosized with TSP; and two pH 5.0 solutions of rufloxacin hydrochloride (RUF-HCl ), one of which was viscosized with TSP. At different times after administration, samples of aqueous humor were withdrawn and analyzed by high-pressure liquid chromatography. The main pharmacokinetic parameters of RUF in the aqueous humor produced by the different formulations were calculated and statistical differences were assessed. RESULTS. The best results, in terms of aqueous humor bioavailability, were observed with two TSP-viscosized formulations: a solution of the hydrochloride (TSP/RUF-HCl) and a suspension of the base (TSP/RUF), followed by the non-viscosized solution of RUF-HCl. The formulations containing CD-solubilized RUF were much less effective. CONCLUSIONS. The present data confirm the significant availability-enhancing properties of tamarind seed polysaccharide, and indicate that solubilization of RUF with hydroxypropyl-b-cyclodextrin (CD/RUF) results in decreased drug availability with respect to standard formulations. Two of the TSP-viscosized formulations (RUF suspension and RUF-HCl solution) produced aqueous humor RUF concentrations in the range of activity against Enterobacteriaceae and Pseudomonas aeruginosa, thus warranting further studies on applications of rufloxacin in ocular therapy.
机译：目的。在局部给药不同制剂后，评估卢氟沙星在兔体内的房水药代动力学，并区分表现出最佳药代动力学特征的个体。方法。将六种制剂滴入兔眼：两种非盐化鲁氟沙星碱或两性离子（RUF）的pH 7.2悬浮液，其中一种用罗望子种子多糖（TSP）粘稠;用羟丙基-b-环糊精（CD）获得的两种RUF的pH 7.2溶液，其中一种用TSP粘稠。盐酸鲁氟沙星的两种pH 5.0溶液（RUF-HCl），其中一种用TSP粘稠。给药后的不同时间，取出房水样品并通过高压液相色谱法分析。计算了由不同制剂产生的房水中RUF的主要药代动力学参数，并评估了统计学差异。结果。用两种TSP增粘配方可观察到最佳的房水生物利用度结果：盐酸盐溶液（TSP / RUF-HCl）和碱悬浮液（TSP / RUF），然后是非增粘配方RUF-HCl溶液。含有CD可溶解的RUF的制剂效果要差得多。结论。本数据证实了罗望子种子多糖具有显着的可用性提高特性，并且表明相对于标准制剂，RUF与羟丙基-b-环糊精（CD / RUF）的溶解导致药物利用率降低。 TSP粘稠的两种制剂（RUF悬浮液和RUF-HCl溶液）产生的房水中RUF浓度在针对肠杆菌科细菌和铜绿假单胞菌的活性范围内，因此有必要进一步研究卢氟沙星在眼科治疗中的应用。

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