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一种含有具有抗菌、抗真菌和抗氧化特性天然产物的药物制剂的设计与质量控制。

Design and quality control of a pharmaceutical formulation containing natural products with antibacterial, antifungal and antioxidant properties.

作者信息

Ordoñez Adriana A L, Ordoñez Roxana M, Zampini Iris C, Isla María I

机构信息

Instituto de Farmacia Dr. Adolfo Rovelli, Universidad Nacional de Tucumán, Ayacucho 471, T4000INI, San Miguel de Tucumán, Tucumán, Argentina.

出版信息

Int J Pharm. 2009 Aug 13;378(1-2):51-8. doi: 10.1016/j.ijpharm.2009.05.040. Epub 2009 May 27.

DOI:10.1016/j.ijpharm.2009.05.040
PMID:19477252
Abstract

The aims of the present study were to determine the antibacterial and antifungal activity as well as mutagenicity of Sechium edule fluid extract and to obtain a pharmaceutical formulation with them. The extract exhibited antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Enterobacter cloacae, Serratia marcescens, Morganella morganii, Acinetobacter baumannii, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, Candida spp. and Aspergillus spp. isolated from clinical samples from two hospitals of Tucuman, Argentina. Non-toxicity and mutagenicity on both Salmonella typhimurium TA98 and TA 100 strains until 100 microg/plate were observed. A hydrogel with carbopol acrylic acid polymer containing S. edule fluid extract as antibacterial, antimycotic and antioxidant agent was obtained. Microbiological, physical and functional stability of pharmaceutical formulation conserved at room temperature for 1 year were determined. Addition of antioxidant preservatives to store the pharmaceutical formulation was not necessary. The semisolid system showed antimicrobial activity against all gram positive and gram negative bacteria and fungi assayed. The minimal inhibitory concentration (MIC) values ranged from 20 to 800 microg/mL. Its activity was compared with a pharmaceutical formulation containing commercial antibiotic and antifungal. A pseudoplastic behavior and positive thixotropy were observed. Our current finding shows an antimicrobial activity of hydrogel containing S. edule extract on a large range of gram negative and gram positive multi-resistant bacteria and fungi. This topical formulation may be used as antimycotic and as antibacterial in cutaneous infections.

摘要

本研究的目的是确定佛手瓜液提取物的抗菌和抗真菌活性以及致突变性,并获得含有该提取物的药物制剂。该提取物对从阿根廷图库曼两家医院的临床样本中分离出的大肠杆菌、肺炎克雷伯菌、奇异变形杆菌、阴沟肠杆菌、粘质沙雷氏菌、摩根氏摩根菌、鲍曼不动杆菌、铜绿假单胞菌、嗜麦芽窄食单胞菌、念珠菌属和曲霉菌属具有抗菌活性。在高达100微克/平板的剂量下,未观察到对鼠伤寒沙门氏菌TA98和TA100菌株的毒性和致突变性。获得了一种含有卡波姆丙烯酸聚合物的水凝胶,其中佛手瓜液提取物作为抗菌、抗真菌和抗氧化剂。测定了在室温下保存1年的药物制剂的微生物、物理和功能稳定性。储存该药物制剂无需添加抗氧化防腐剂。该半固体系统对所有检测的革兰氏阳性和革兰氏阴性细菌及真菌均显示出抗菌活性。最低抑菌浓度(MIC)值范围为20至800微克/毫升。将其活性与含有市售抗生素和抗真菌剂的药物制剂进行了比较。观察到其具有假塑性行为和正触变性。我们目前发现含佛手瓜提取物的水凝胶对多种革兰氏阴性和革兰氏阳性多重耐药细菌及真菌具有抗菌活性。这种局部用制剂可用于皮肤感染的抗真菌和抗菌治疗。

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