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氧氟沙星掩味微球:口腔崩解片的制剂与评价

Taste masked microspheres of ofloxacin: formulation and evaluation of orodispersible tablets.

作者信息

Malik Karan, Arora Gurpreet, Singh Inderbir

机构信息

School of Pharmaceutical Sciences, Chitkara University, Solan-174103, Himachal Pradesh, India.

出版信息

Sci Pharm. 2011 Jul-Sep;79(3):653-72. doi: 10.3797/scipharm.1104-11. Epub 2011 Jul 25.

Abstract

Ofloxacin is a synthetic chemotherapeutic antibiotic used for treatment of a variety of bacterial infections, but therapy suffers from low patients' compliance due to its unpleasant taste. This study was aimed to develop taste masked microspheres of ofloxacin using Eudragit and to prepare orodispersible tablets of the formulated microspheres using natural superdisintegrant. Taste masking Eudragit E100 microspheres were prepared by solvent evaporation technique with an entrapment efficiency ranging from 69.54 ± 1.98 to 86.52 ± 2.25%. DSC revealed no interaction between the drug and polymer. Microspheres prepared at a drug/polymer ratio of 1:4 and 1:5 revealed sufficient flow properties and better taste masking as compared to other ratios. Drug loaded microspheres were formulated as orodispersible tablets using locust bean gum as a natural superdisintegrant offering the advatages of biocompatibility and biodegrad-ability. The wetting time, water absorption ratio and in-vitro disintegration time of the tablets were found to range between 19 ± 2 to 10 ± 3 seconds, 59.11 ± 0.65 to 85.76 ± 0.96 and 22 ± 2 to 10 ± 2 seconds, respectively. The in-vitro ofloxacin release was about 97.25% within 2h. The results obtained from the study suggested the use of eudragit polymer for preparing ofloxacin loaded microspheres with an aim to mask the bitter taste of the drug and furthermore orodispersible tablets could be formulated using locust bean gum as a natural superdisintegrant.

摘要

氧氟沙星是一种合成化疗抗生素,用于治疗多种细菌感染,但由于其味道不佳,治疗时患者的依从性较低。本研究旨在使用丙烯酸树脂制备氧氟沙星的掩味微球,并使用天然超级崩解剂制备该微球的口腔崩解片。采用溶剂蒸发技术制备了掩味丙烯酸树脂E100微球,包封率在69.54±1.98%至86.52±2.25%之间。差示扫描量热法显示药物与聚合物之间无相互作用。与其他比例相比,以1:4和1:5的药物/聚合物比例制备的微球显示出足够的流动性和更好的掩味效果。以刺槐豆胶作为天然超级崩解剂,将载药微球制成口腔崩解片,具有生物相容性和生物可降解性的优点。片剂的润湿时间、吸水率和体外崩解时间分别在19±2至10±3秒、59.11±0.65至85.76±0.96以及22±2至10±2秒之间。体外氧氟沙星释放率在2小时内约为97.25%。该研究结果表明,使用丙烯酸树脂聚合物制备载氧氟沙星微球可掩盖药物的苦味,此外,以刺槐豆胶作为天然超级崩解剂可制备口腔崩解片。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a49/3163379/fe67d9c6666c/Scipharm-2011-79-653f1.jpg

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