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Review of Properties and Analytical Methods for the Determination of Norfloxacin

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Review of Properties and Analytical Methods for the Determination of Norfloxacin Critical Reviews in Analytical Chemistry ISSN: 1040-8347 (Print) 1547-6510 (Online) Journal homepage: https://www.tandfonline.com/loi/batc20 Review of Properties and Analytical Methods for the Determination of Norfloxacin Lucas Chierentin & Hérida Regina Nunes Salgado To cite this article: Lucas Chierentin & Hérida Regina Nunes Salgado (2016) Review of Properties and Analytical Methods for the Determination of Norfloxacin, Critical Reviews in Analytical Chemistry, 46:1, 22-39, DOI: 10.1080/10408347.2014.941456 To link to this article: https://doi.org/10.1080/10408347.2014.941456 Accepted author version posted online: 23 Sep 2015. Published online: 08 Feb 2016. Submit your article to this journal Article views: 223 Citing articles: 12 View citing articles Full Terms & Conditions of access and use can be found at https://www.tandfonline.com/action/journalInformation?journalCode=batc20 CRITICAL REVIEWS IN ANALYTICAL CHEMISTRY 2016, VOL. 46, NO. 1, 22–39 http://dx.doi.org/10.1080/10408347.2014.941456 Review of Properties and Analytical Methods for the Determination of Norfloxacin Lucas Chierentin and Herida Regina Nunes Salgado School of Pharmaceutical Sciences, S~ao Paulo State University, Araraquara, S~ao Paulo, Brazil ABSTRACT KEYWORDS The first-generation quinolones have their greatest potency against Gram-negative bacteria, but newly Analytical methods; developed molecules have exhibited increased potency against Gram-positive bacteria, and existing fluoroquinolones; agents are available with additional activity against anaerobic microorganisms. Norfloxacin is a broad- norfloxacin; spectrum antimicrobial fluoroquinolone used against Gram-positive and Gram-negative organisms pharmacokinetics; quality control (aerobic organisms). There are different analytical methods available to determine norfloxacin applied in quality control of this medicine in order to ensure its effectiveness and safety. The authors present an overview of the fourth generation of quinolones, followed by the properties, applications, and analytical methods of norfloxacin. These results show several existing analytical techniques that are flexible and broad-based methods of analysis in different matrices. This article focuses on bionalytical and pharmaceutical quality-control applications, such as thin-layer chromatography, microbiological assay, spectrophotometry, capillary electrophoresis (CE), and high-performance liquid chromatography (HPLC). Introduction important goals of quality control is to report the analytical method validation to ensure confidence in the analytical data Quinolones and fluoroquinolones are chemical groups related throughout product development (International Conference on to nalidixic acid derivatives. The first quinolone to be intro- Harmonization, 2005; World Health Organization, n.d.) and duced was nalidixic acid (1-ethyl-1,4-dihydro-7-methyl-4-oxo- ensure that the procedures of good manufacturing practices 1,8-naphthyridine-3-carboxylic acid) in 1962; it is derived from guides as well as good laboratory practice required by the U.S. the antimalarial drug chloroquine (Andriole, 2005; Ball, 2003; FDA are applied in the pharmaceutical industry (Shabir, 2003). Chen and Lo, 2003; Hawkey, 2003; Izawa et al., 1980). Current This article is not intended to be a systematic review of the agents were developed following fluoridation of the quinolone literature on these subjects. Rather, it provides an overview of molecule, and the first to receive approval by the U.S. Food and relevant published literature and a discussion of data, highlight- Drug Administration (FDA) was norfloxacin (1-ethyl-6-fluoro- ing progress in quinolone and fluoroquinolone development 1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic and the challenges to provide these drugs as high-quality prod- acid) in 1984 and it was patented by the pharmaceutical com- ucts, with a focus on the norfloxacin. pany Kyorin Seiyaku Kabushiki Kaisha (Bolon, 2011; U.S. Food and Drug Administration, n.d.). Norfloxacin is a broad-spectrum antimicrobial used in sev- Structural modification eral countries to effectively treat infections in humans and ani- mals. It has been used for treatment of several bacterial The generation of quinolones can be demonstrated in two infections, such as Escherichia coli, Citrobacter freundi, Staphy- ways, the naphthyridones group and the fluoroquinolone group lococcus aureus, Pseudomonas aeruginosa, and Shigella (Vijan (Table 1). The quinolone basic molecular structure is composed and Conci, 2008). In Brazil, this antimicrobial agent is com- of a carboxylic acid ring, pyridine ring, carbon or nitrogen, and monly used as 400 mg pharmaceutical tablets and was autho- side chain. Nalidixic acid is the original naphthyridine core, rized by the National Agency for Sanitary Surveillance with a ketone function at C-4, which determines antibacterial (ANVISA) in 1983. The drug is represented by pharmaceutical activity by influencing the affinity for bacterial enzymes. This companies such Uni~ao Quımica, Sigma Pharma, Merck, Med- antibacterial agent has a modest activity against Gram-negative ley, and Biosintetica (ANVISA, n.d.). bacteria, low activity against Gram-positive bacteria, and no With the large number of products marketed by different activity against Pseudomonas aeruginosa. Due to its low oral companies in several countries, providing high-quality prod- absorption and high concentration in urine, its therapeutic use ucts remain a challenge. Quality control is an important task in has been restricted to the treatment of urinary tract infections the pharmaceutical industry, not only to protect the manufac- (Bolon, 2009; Christian, 1996; Oliphant and Green, 2002; Van turer against compensation claims, but also to guarantee the Oort et al., 1983). Nalidixic acid (discontinued) structure patient the use of safe and effective products. One of the changes in position N-1 affect drug potency and CONTACT Lucas Chierentin [email protected] School of Pharmacy, Faculty of Pharmaceutical Sciences, S~ao Paulo State University, Rodovia Araraquara-Jau, km 1, 14801-902, Araraquara, S~ao Paulo, Brazil. © 2016 Taylor & Francis Group, LLC CRITICAL REVIEWS IN ANALYTICAL CHEMISTRY 23 Table 1. Quinolone classification used in human medicine. Quinolones Fluoroquinolones 1st Generation (naphthyridines) 2nd Generation 3rd Generation 4th Generation Nalidixic acid Norfloxacin Tosufloxacin Trovafloxacin Oxolinic acid Pefloxacin Temafloxacin Moxifloxacin Piromidic acid Enoxacin Sparfloxacin Prulifloxacin Cinonaxin Ofloxacin Grepafloxacin Sitafloxacin Miloxacin Ciprofloxacin Pazufloxacin Gemifloxacin Rosoxacin Flumequine Balofloxacin Clinafloxacin Pipemidic acid Lomefloxacin Levofloxacin Besifloxacin Droxacin Nadifloxacin Garenoxacin Rufloxacin Gatifloxacin Fleroxacin Alatrofloxacin pharmacokinetics. Positions C-2, C-3, and C-4 determine anti- levofloxacin, balofloxacin, tosufloxacin, pazufloxacin, and bacterial activity by influencing the affinity for bacterial temafloxacin. They were subsequently developed and are all enzymes; also positions C-3 and C-4 are involved in metal che- active against penicillin-resistant Streptococcus pneumoniae lation and the consequent interaction with divalent and triva- and have been proven highly effective in the treatment of lower lent cations (Andriole, 2005). respiratory tract infections (acute sinusitis and acute exacerba- The agents from the first generation (Figure 1) such as oxo- tions of chronic bronchitis) (Ball, 1999). Position C-5 of the linic acid, piromidic acid, cinoxacin (discontinued), miloxacin, quinolone ring is important in determining in vitro potency, rosoxacin (discontinued), pipemidic acid, and droxacin have especially against Gram-positive bacteria (as is found on spar- analogue structures with nalidixic acid (discontinued) and floxacin). Grepafloxacin contains a methyl group at C-5 that showed no advantage in therapy over the precursor (Gade- increases the potency against Gram-positive organisms to a less busch and Shungu, 1991; King et al., 2000; Souza et al., 2012; extent (Bolon, 2009, 2011; Domagala, 1994). Zhanel et al., 1999). The final group of fluoroquinolones, including trovafloxacin The new classification of quinolone antibiotics takes into (discontinued), sitafloxacin, prulifloxacin, gatifloxacin (discon- account the expanded antimicrobial spectrum of the new fluo- tinued), clinafloxacin, gemifloxacin (tentative approval), moxi- roquinolones (Andriole, 2005). floxacin, besifloxacin, garenoxacin, and alatrofloxacin As was highlighted by Bolon (2011) the long period of fluo- (discontinued), is termed fourth generation (Figure 4). This roquinolone development provides considerable insight into generation has potent activity against anaerobes and increased the effect of structural modification upon the antimicrobial activity against pneumococci (Higgins et al., 1978). The addi- activity and pharmacologic properties of these agents. tion an alkyl substitution of either ring type improves solubility The second-generation fluoroquinolones (Figure 2) have (causing less risk of crystalluria), and activity of the fluoroquin- increased Gram-negative activity as well as some Gram-positive olone also prolongs the half-life (Bolon, 2009, 2011; Domagala, and atypical pathogen coverage. The addition of a fluorine 1994). atom to position C-6 transforms a quinolone into a fluoroquin- Molecule substitutions have resulted in advanced genera- olone, enhancing drug penetration into the bacterial cell. Posi- tions of fluoroquinolone that have expanded the spectra of tion N-1 presents low or
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