Development and validation of a new method for the quantification of norfloxacin by HPLC-UV and its application to a comparative pharmacokinetic study in human volunteers

Bedor, Danilo César Galindo; Gonçalves, Talita Mota; Bastos, Leila Leal; Sousa, Carlos Eduardo Miranda de; Abreu, Luis Renato Pires de; Oliveira, Eliza; Santana, Davi Pereira de

doi:10.1590/s1516-93322007000200009

Cited by 4 publications

(3 citation statements)

References 15 publications

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“…One has to take into consideration that norfloxacin and moxifloxacin concentrations found to have an inhibitory effect on melanogenesis and antioxidant defense system in normal human melanocytes are about 16-, 160-fold higher [ 41 ], and 8-, 80-fold higher [ 42 ] for norfloxacin and moxifloxacin, respectively, than the concentrations normally observed in vivo. However, we have previously demonstrated that norfloxacin [ 28 ] and moxifloxacin [ 29 ] form complexes with melanin, what may lead to the accumulation of these drugs in melanin reach tissues.…”

Section: Discussionmentioning

confidence: 99%

Effect of norfloxacin and moxifloxacin on melanin synthesis and antioxidant enzymes activity in normal human melanocytes

et al. 2014

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Fluoroquinolone antibiotics provide broad-spectrum coverage for a number of infectious diseases, including respiratory as well as urinary tract infections. One of the important adverse effects of these drugs is phototoxicity which introduces a serious limitation to their use. To gain insight the molecular mechanisms underlying the fluoroquinolones-induced phototoxic side effects, the impact of two fluoroquinolone derivatives with different phototoxic potential, norfloxacin and moxifloxacin, on melanogenesis and antioxidant enzymes activity in normal human melanocytes HEMa-LP was determined. Both drugs induced concentration-dependent loss in melanocytes viability. The value of EC50 for these drugs was found to be 0.5 mM. Norfloxacin and moxifloxacin suppressed melanin biosynthesis; antibiotics were shown to inhibit cellular tyrosinase activity and to reduce melanin content in melanocytes. When comparing the both analyzed fluoroquinolones, it was observed that norfloxacin possesses greater inhibitory effect on tyrosinase activity in melanocytes than moxifloxacin. The extent of oxidative stress in cells was assessed by measuring the activity of antioxidant enzymes: SOD, CAT, and GPx. It was observed that norfloxacin caused higher depletion of antioxidant status in melanocytes when compared with moxifloxacin. The obtained results give a new insight into the mechanisms of fluoroquinolones toxicity directed to pigmented tissues. Moreover, the presented differences in modulation of biochemical processes in melanocytes may be an explanation for various phototoxic activities of the analyzed fluoroquinolone derivatives in vivo.

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Section: Discussionmentioning

confidence: 99%

Effect of norfloxacin and moxifloxacin on melanin synthesis and antioxidant enzymes activity in normal human melanocytes

et al. 2014

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“…The flow rate, injection volume and column temperature were 1.2 mL/min, 20 L and 40 • C, respectively. Ciprofloxacin was used as an internal standard [28]. The various pharmacokinetic parameters were calculated for each individual set of data by noncompartmental analysis using WinNonLin version 4.0 (Pharsight, Mountain View, CA,).…”

Section: Methodsmentioning

confidence: 99%

Norfloxacin mixed solvency based solid dispersions: An in-vitro and in-vivo investigation

Kamble

Sharma

Mehta

2017

Journal of Taibah University for Science

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Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urinary tract infections. However, due to its poor aqueous solubility, it has low oral bioavailability. The aim of the present study was to improve the aqueous solubility and dissolution profile of NF by formulating its mixed-solvency based solid dispersions (SDs). The NF-loaded SDs were prepared by a solvent evaporation technique using urea, sodium benzoate and a niacinamide hydrotropic mixture. The prepared SDs were evaluated regarding their solubility, mean particle size, in-vitro drug release and oral bioavailability. The optimized batch showed a high percentage yield of 99.04% , with a mean particle size of 132.91 m. Optimized SDs Exhibit 96.48% drug release. The oral bioavailabilities of NF from the optimized SDs, drug alone and marketed formulation were evaluated in Wistar rats at a dose of 20.0 mg/kg. In comparison to the drug alone, approximately 6.90-and 5.0-fold increases in AUC and C max , respectively, were observed for NF from mixed-solvency based SDs. The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability.

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“…This drug is chemically known as 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)–3-quinolinecar-boxylicacid1,2 and commonly prescribed for the treatment of urinary, respiratory, and gastrointestinal tracts infections 4. It is also active against clinically relevant pathogens responsible for causing sexually transmitted diseases, sinuses, and prostate infections 5,6…”

Section: Introductionmentioning

confidence: 99%

<p>In vitro comparative quality assessment of different brands of norfloxacin tablets available in Jimma, Southwest Ethiopia</p>

Hambisa¹,

Belew²,

Suleman³

2019

DDDT

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Background Pharmaceuticals play a pivotal role in maintaining human health and promoting well-being. However, safety, efficacy, and quality of the drugs should be ascertained to provide a desired pharmacological effect. Aim The aim of the present study was to determine the quality as well as the physicochemical equivalence of nine brands of norfloxacin tablets marketed in Jimma, Ethiopia. Methods Nine norfloxacin brands were subjected to in vitro tests associated with quality of tablet dosage form, and the tests were conducted according to procedures described in the United States Pharmacopeia (USP). Results This study indicated that all brands of norfloxacin complied with the USP for uniformity of weight, friability, hardness, and assay of active ingredient. However, two of the nine brands evaluated failed to release 80% of their drug contents within 30 minutes as outlined in the USP. Correspondingly, all of the brands studied were within the specification for hardness test. Furthermore, different dissolution profile comparison methods have proven the similarity in dissolution profile of Negaflox and Norcin with the comparator product (Trizolin). Mathematical models-dependent approaches have shown that the drug release data fit well to the Weibull release model. Conclusion The physicochemical evaluation showed that all the norfloxacin brands met the quality specification with respect to uniformity of weight, hardness, friability, and assay. With regard to dissolution test, two brands of norfloxacin were found to be out of the specified pharmacopeial requirement. The study also revealed the similarity in the dissolution profile of two brands of norfloxacin with the comparator product.

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Development and validation of a new method for the quantification of norfloxacin by HPLC-UV and its application to a comparative pharmacokinetic study in human volunteers

Cited by 4 publications

References 15 publications

Effect of norfloxacin and moxifloxacin on melanin synthesis and antioxidant enzymes activity in normal human melanocytes

Effect of norfloxacin and moxifloxacin on melanin synthesis and antioxidant enzymes activity in normal human melanocytes

Norfloxacin mixed solvency based solid dispersions: An in-vitro and in-vivo investigation

<p>In vitro comparative quality assessment of different brands of norfloxacin tablets available in Jimma, Southwest Ethiopia</p>

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