Sustained Ocular Delivery of Sparfloxacin from pH Triggered In Situ Gelling System

K. Reddy, M. Ahmed
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引用次数: 11

Abstract

Purpose: The present research work was to develop and evaluate In situ gels of Sparfloxacin . Method/approach: In situ gels were prepared by using HPMC and carbopol based on the concept of pH trigger gelation systems.Formulations were evaluated for gelling capacity, drug content, clarity, viscosity and In vitro release. Findings: FTIR studies showed that the drug and excipients were compatible. Experimental part showed that viscosity of sols was increased with increase in the concentration of polymers and the solutions showed pseudoplastic behaviour. Sol-to-gel transformation occurred in the presence of simulated tear fluid of pH 7.4. The drug content was found satisfactory. The In vitro release profile of Sparfloxacin from the S3 formulation have shown least drug release (72.34 %) in 8 hrs compared to formulation S2 that is 77.30%, the correlation coefficient ‘r’ indicated that the drug release followed diffusion controlled mechanism from the In situ gels. Sparfloxacin has In vitro activity against a wide range of gram-negative and gram-positive microorganisms.The antimicrobial studies against Streptococcus aureus were showed positive results. The formulations were therapeutically efficacious, sterile and provided sustained release of the drug over a period of time. Application/Value: These results demonstrate that the developed system is an alternative to conventional drug delivery system.
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pH触发原位胶凝系统持续眼内递送司帕沙星
目的:研制并评价司帕沙星原位凝胶。方法/途径:基于pH触发凝胶体系的概念,采用HPMC和carbopol制备原位凝胶。评价制剂的胶凝能力、药物含量、透明度、粘度和体外释放度。结果:FTIR研究表明,该药物与辅料配伍良好。实验部分表明,随着聚合物浓度的增加,溶胶的粘度增加,溶液表现出假塑性行为。在pH为7.4的模拟泪液存在下,发生了溶胶-凝胶转化。药物含量令人满意。S3剂型对斯帕沙星的体外释放率为72.34%,而S2剂型的体外释放率为77.30%,相关系数为r,表明S3剂型的体外释放遵循扩散控制机制。司帕沙星对多种革兰氏阴性和革兰氏阳性微生物具有体外活性。对金黄色链球菌的抑菌试验结果为阳性。该制剂在治疗上有效,无菌,并在一段时间内提供药物的持续释放。应用/价值:这些结果表明所开发的系统是传统给药系统的替代方案。
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