经眼局部滴入微米化莫西沙星后兔房水中莫西沙星的超高压液相色谱分析法。
Ultra high-pressure liquid chromatographic assay of moxifloxacin in rabbit aqueous humor after topical instillation of moxifloxacin nanoparticles.
机构信息
Department of Pharmaceutics, F/O Pharmacy, Hamdard University, Hamdard Nagar, New Delhi 110062, India.
出版信息
J Pharm Biomed Anal. 2010 May 1;52(1):110-3. doi: 10.1016/j.jpba.2009.12.008. Epub 2009 Dec 11.
The present report describes a rapid and sensitive ultra high-pressure liquid chromatography (UHPLC) method with UV detection to quantify moxifloxacin in rabbit aqueous humor. After deproteinisation with acetonitrile, gradient separation of moxifloxacin was achieved on a Waters Acquity BEH C18 (50mmx2.1mm, 1.7microm) column at 50 degrees C. The mobile phase consisted of 0.1% trifluoroacetic acid in water and acetonitrile at a flow rate of 0.4ml/min. Detection of moxifloxacin was done at 296nm. Method was found to be selective, linear (r=0.9997), accurate (recovery, 97.30-99.99%) and precise (RSD, <or=1.72%) in the selected concentration range of 10-1000ng/ml. Detection and quantitation limit of moxifloxacin in aqueous humor were 0.75 and 2.5ng/ml, respectively. The aqueous humor levels of moxifloxacin after single topical instillation in three formulations, i.e. moxifloxacin solution (Moxi-SOL), anionic nanoparticles (Moxi-ANP) and cationic nanoparticles (Moxi-CNP) were investigated. A fourfold increase in the relative bioavailability was observed with the Moxi-CNP (AUC(0-->t), 3.14microg h/ml) compared with Moxi-SOL (AUC(0-->t), 0.79microg h/ml) and Moxi-ANP (AUC(0-->t), 0.72microg h/ml) formulation. The results indicate that the cationic nanoparticle increases ocular bioavailability of moxifloxacin and prolong its residence time in the eye.
本报告描述了一种快速灵敏的超高效液相色谱（UHPLC）法，结合紫外检测，可用于定量检测兔眼房水中的莫西沙星。经乙腈沉淀蛋白后，在 Waters Acquity BEH C18（50mmx2.1mm，1.7μm）柱上以 50°C 进行梯度洗脱，实现莫西沙星的分离。流动相由 0.1%三氟乙酸水溶液和乙腈组成，流速为 0.4ml/min。莫西沙星的检测波长为 296nm。该方法选择性好、线性范围宽（r=0.9997）、准确度高（回收率 97.30-99.99%）、精密度好（RSD<or=1.72%），所选浓度范围为 10-1000ng/ml。莫西沙星在房水中的检测限和定量限分别为 0.75 和 2.5ng/ml。通过单次局部滴注三种制剂（莫西沙星溶液（Moxi-SOL）、阴离子纳米粒（Moxi-ANP）和阳离子纳米粒（Moxi-CNP）），研究了莫西沙星在兔眼房水中的水平。与 Moxi-SOL（AUC（0-->t），0.79μg h/ml）和 Moxi-ANP（AUC（0-->t），0.72μg h/ml）制剂相比，Moxi-CNP（AUC（0-->t），3.14μg h/ml）的相对生物利用度提高了 4 倍。结果表明，阳离子纳米粒可提高莫西沙星在眼部的生物利用度，并延长其在眼部的滞留时间。
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