Sultana Yasmin, Aqil M, Ali Asgar
Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi, India.
Drug Deliv. 2006 May-Jun;13(3):215-9. doi: 10.1080/10717540500309164.
The purpose of our work was to develop an ophthalmic delivery system of a flouroquinolone antibiotic, pefloxacin mesylate, based on the concept of ion-activated in situ gelation. Gelrite gellan gum, a novel ophthalmic vehicle, that gels in the presence of mono- or divalent-cations present in the lacrimal fluid, was used as the gelling agent. The developed formulation was compared with marketed eye drops in efficacy of treatment of bacterial conjunctivitis that was induced artificially in rabbits. The formulations were evaluated for rheological characteristics, in vitro release behavior, antimicrobial efficacy, and efficacy against bacterial conjunctivitis. We found that in situ gelling formulations passed the test for sterility. The formulations exhibited a first-order release pattern over 12 hr in in vitro release studies. The developed formulation was effective against selected micro-organisms in antimicrobial efficacy studies. The shelf lives of formulation was >2 years. The formulation demonstrated better therapeutic efficacy compared with standard eye drops because it improved the clinical parameters monitored for prolonged periods. The developed formulations can be considered as a viable alternative to conventional eye drops.
我们工作的目的是基于离子激活原位凝胶化的概念，开发一种氟喹诺酮抗生素甲磺酸培氟沙星的眼部给药系统。结冷胶，一种新型的眼部给药载体，在泪液中存在的单价或二价阳离子的作用下会发生凝胶化，被用作胶凝剂。将所开发的制剂与市售眼药水在兔人工诱发的细菌性结膜炎治疗效果方面进行比较。对这些制剂进行流变学特性、体外释放行为、抗菌效果以及对细菌性结膜炎的疗效评估。我们发现原位凝胶化制剂通过了无菌测试。在体外释放研究中，这些制剂在12小时内呈现出一级释放模式。所开发的制剂在抗菌效果研究中对选定的微生物有效。制剂的保质期大于2年。与标准眼药水相比，该制剂表现出更好的治疗效果，因为它改善了长期监测的临床参数。所开发的制剂可被视为传统眼药水的一种可行替代品。
