关键词: Analytical method anti-MRSA fluoroquinolone antibiotic levonadifloxacin

Mesh : Anti-Bacterial Agents / pharmacology therapeutic use Methicillin-Resistant Staphylococcus aureus Quinolizines / therapeutic use Quinolones

来  源:   DOI:10.1080/10408347.2020.1855412   PDF(Sci-hub)

Abstract:
Increased use of antibiotics globally has led to the threat of antibiotic resistance; this drove the urge of researchers toward discovering more potent and broad-spectrum antibiotics. Levonadifloxacin (LND) is the very first antibiotic developed by an Indian company Wockhardt. It is S (-) isomer of another broad-spectrum antibiotic Nadifloxacin which is used topically for skin, soft tissue bacterial infection. LND belongs to the benzo quinolizine category which is a subclass of fluoroquinolone, indicated for ABSSIS, CABP, and other infections including diabetic foot infection; formulated as l-arginine salt of levonadifloxacin (WCK177) for IV and l-alanine ester mesylate salt as alalevonadifloxacin (WCK2349) for oral administration. It generally shows dominant antibacterial activity against Gram-negative, and positive bacterial infections, particularly toward methicillin-resistant Staphylococcus aureus (MRSA) by dual inhibition of DNA gyrase and topoisomerase IV. Producing quality product that complies to regulatory requirements is a big concern for pharma industries. To this context, validated analytical methods for routine quality control are essential for quantification of LND as an API alone and together with pharmaceutical formulations. This review suggests therapeutic, pharmacological, and analytical aspects regarding the novel drug LND and particularly focuses on discussing various reported analytical methods present for analytical or bioanalytical estimation of the drug and suggest to develop a simple and validated method which also complies to green chemistry.
摘要:
全球抗生素使用的增加导致了抗生素耐药性的威胁;这促使研究人员迫切需要发现更有效和广谱的抗生素。左旋阿霉素(LND)是印度公司Wockhardt开发的第一种抗生素。它是另一种广谱抗生素纳地沙星的S(-)异构体,局部用于皮肤,软组织细菌感染。LND属于苯并喹唑啉类,是氟喹诺酮的一个亚类,指示为ABSSIS,CABP,和其他感染,包括糖尿病足感染;配制为左旋甲氧氟沙星的L-精氨酸盐(WCK177)用于IV和1-丙氨酸酯甲磺酸盐作为阿莱酮二氟沙星(WCK2349)用于口服。它通常对革兰氏阴性,细菌感染呈阳性,特别是通过DNA促旋酶和拓扑异构酶IV的双重抑制对甲氧西林耐药的金黄色葡萄球菌(MRSA)。生产符合监管要求的优质产品是制药行业的一大关注点。在这种情况下,用于常规质量控制的经过验证的分析方法对于定量LND作为单独的API以及与药物制剂一起是必不可少的。这篇评论建议治疗,药理学,和有关新药LND的分析方面,特别着重于讨论用于药物分析或生物分析评估的各种报道的分析方法,并建议开发一种简单且经过验证的方法,该方法也符合绿色化学。
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