Weyenberg Wim, Vermeire An, Dhondt Marijke M M, Adriaens Els, Kestelyn Philippe, Remon Jean Paul, Ludwig Annick
Laboratory of Pharmaceutical Technology and Biopharmacy, University of Antwerp, Antwerp, Belgium.
Invest Ophthalmol Vis Sci. 2004 Sep;45(9):3229-33. doi: 10.1167/iovs.04-0206.
Evaluation in volunteers of ciprofloxacin-containing ocular gelling minitablets with prolonged release properties.
The irritation potential of ciprofloxacin-containing bioadhesive powder mixtures, used to prepare ocular bioerodible minitablets, was evaluated with a slug mucosal-irritation test. The tear pharmacokinetic profiles of ciprofloxacin were determined in six healthy volunteers after topical administration of a minitablet and a single eye drop in the lower fornix. The drug concentrations in the tear samples collected were measured by using a validated HPLC METHOD: Each volunteer was asked to give an evaluation of the preparations applied by answering a standard questionnaire.
The results of the mucosal-irritation test demonstrated the nonirritating properties of the bioadhesive powder mixtures. The ocular minitablet, applied in the fornix was in general well tolerated by the healthy volunteers. The mean tear concentration of ciprofloxacin was 33.0, 135.2, and 33.7 microg/g at 30, 300, and 480 minutes after application of the minitablet. Mean tear levels of 84.7, 45.6, and 8.4 microg/g were obtained at 5, 30, and 60 minutes after application of an eye drop.
Due to their prolonged drug release properties, the ocular minitablets containing ciprofloxacin can be considered as a promising drug delivery system to be used in the treatment of ulcerative bacterial keratitis.
对含环丙沙星的具有缓释特性的眼用凝胶型小片在志愿者中进行评估。
采用团块黏膜刺激试验评估用于制备眼用生物可蚀性小片的含环丙沙星生物黏附性粉末混合物的潜在刺激性。在6名健康志愿者于下穹窿局部给予一片小片和一滴眼药水后，测定环丙沙星的泪液药代动力学曲线。采用经过验证的高效液相色谱法测量所采集泪液样本中的药物浓度。方法：要求每位志愿者通过回答一份标准问卷对所应用的制剂进行评价。
黏膜刺激试验结果表明生物黏附性粉末混合物无刺激性。应用于穹窿的眼用小片总体上被健康志愿者很好地耐受。应用小片后30、300和480分钟时，环丙沙星的平均泪液浓度分别为33.0、135.2和33.7微克/克。应用眼药水后5、30和60分钟时，平均泪液水平分别为84.7、45.6和8.4微克/克。
由于其延长的药物释放特性，含环丙沙星的眼用小片可被视为一种有前景的药物递送系统，用于治疗溃疡性细菌性角膜炎。
