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左旋那氟沙星的化学、生物学特性及分析方法研究进展。

Chemistry, Biological Properties and Analytical Methods of Levonadifloxacin: A Review.

机构信息

SVKM'S NMIMS School of Pharmacy and Technology Management, Shirpur, Maharashtra, India.

出版信息

Crit Rev Anal Chem. 2022;52(5):1069-1077. doi: 10.1080/10408347.2020.1855412. Epub 2020 Dec 13.

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 (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

全球抗生素使用量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。Levonadifloxacin(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 Nadifloxacin 的 S(-)异构体,用于治疗皮肤和软组织细菌感染。LND 属于苯并喹啉类,是氟喹诺酮类的一个子类,用于 ABSSIS、CABP 和其他感染,包括糖尿病足感染;作为 LND 的左旋精氨酸盐(WCK177)制成静脉注射制剂,以及作为 LND 的丙氨酸酯甲磺酸盐(WCK2349)制成口服制剂。它通常对革兰氏阴性和阳性细菌感染表现出主要的抗菌活性,特别是通过抑制 DNA 回旋酶和拓扑异构酶 IV 双重抑制对耐甲氧西林金黄色葡萄球菌(MRSA)具有活性。生产符合监管要求的高质量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单独作为 API 以及与药物制剂一起定量测定 LND 至关重要。本文综述了关于新型药物 LND 的治疗、药理学和分析方面的内容,特别侧重于讨论目前用于药物分析或生物分析测定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,同时符合绿色化学的要求。

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