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

机译:从pH触发的原位胶凝系统持续眼部注射司帕沙星

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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 grampositive 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.
机译:目的-本研究工作是开发和评估司帕沙星的原位凝胶。方法/方法根据pH触发凝胶化系统的概念,使用HPMC和carbopol制备原位凝胶,评估制剂的凝胶容量,药物含量,透明度,粘度和体外释放。 FTIR研究结果表明该药物和赋形剂是相容的。实验部分表明,溶胶的粘度随着聚合物浓度的增加而增加,溶液表现出假塑性行为。在pH 7.4的模拟泪液存在下,发生了溶胶-凝胶转变。发现药物含量令人满意。与制剂S2相比,S3制剂中Sparfloxacin的体外释放曲线显示在8小时内药物释放最低(72.34%)为77.30%,相关系数``r''表明药物释放遵循In的扩散控制机制原位凝胶。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。对金黄色链球菌的抗菌研究显示出积极的结果。该制剂是治疗有效的,无菌的并且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,开发的系统是常规药物输送系统的替代方案。

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