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含诺氟沙星的透皮贴剂的制备与评价:一种烧伤创面愈合的新疗法。

Preparation and evaluation of transdermal plasters containing norfloxacin: a novel treatment for burn wound healing.

作者信息

Mpharm Kamal Dua, Ramana M V, Sara U V S, Agrawal D K, Mpharm Kavita Pabreja, Chakravarthi Srikumar

出版信息

Eplasty. 2010 Jun 21;10:e44.

PMID:20596234
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2890388/
Abstract

OBJECTIVE

In an attempt for better treatment of bacterial infections and burn wounds, plaster formulations containing different concentrations of norfloxacin were prepared using polymers like polyvinylpyrrolidone and polyvinyl alcohol and evaluated for physicochemical parameters, in vitro drug release, antimicrobial activity, and burn wound healing properties. The prepared formulations were compared with silver sulfadiazine cream 1%, USP.

METHODS

Plaster formulations containing different concentrations of norfloxacin were prepared by solvent casting method using combination of polymers like polyvinylpyrrolidone and polyvinyl alcohol. These plasters were characterized for drug content, thickness, percentage elongation, tensile strength, in vitro drug release properties, and antimicrobial activity against various strains of aerobic and anaerobic microorganisms. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction.

RESULTS

The in vitro release and in vitro skin permeation followed the first-order kinetics followed by diffusion as dominant release mechanism. In spite of the significant antimicrobial and wound healing effects produced by plasters, the observed values were less than the values obtained with silver sulfadiazine 1% cream (P < .05). Various histopathological changes observed during the study period (days 1, 4, 8, and 12) also supported the wound healing process.

CONCLUSION

Based on the observed in vitro performances along with antimicrobial and wound healing effects, the 5% norfloxacin transdermal plasters could be employed as an alternative to commercial silver sulfadiazine 1% cream.

摘要

目的

为了更好地治疗细菌感染和烧伤创面,使用聚乙烯吡咯烷酮和聚乙烯醇等聚合物制备了含不同浓度诺氟沙星的膏药制剂,并对其理化参数、体外药物释放、抗菌活性和烧伤创面愈合特性进行了评估。将制备的制剂与1%的磺胺嘧啶银乳膏(美国药典)进行比较。

方法

采用溶剂浇铸法,使用聚乙烯吡咯烷酮和聚乙烯醇等聚合物的组合制备含不同浓度诺氟沙星的膏药制剂。对这些膏药进行药物含量、厚度、伸长率、拉伸强度、体外药物释放特性以及对各种需氧和厌氧微生物菌株的抗菌活性的表征。通过组织病理学检查和测量伤口收缩来评估伤口愈合特性。

结果

体外释放和体外皮肤渗透遵循一级动力学,随后以扩散作为主要释放机制。尽管膏药产生了显著的抗菌和伤口愈合效果,但观察到的值低于1%磺胺嘧啶银乳膏获得的值(P <.05)。在研究期间(第1、4、8和12天)观察到的各种组织病理学变化也支持伤口愈合过程。

结论

基于观察到的体外性能以及抗菌和伤口愈合效果,5%诺氟沙星透皮膏药可作为市售1%磺胺嘧啶银乳膏的替代品。

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