Easy-Assessment of Levofloxacin and Minocycline in Relevant Biomimetic Media by HPLC–UV Analysis
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Simple, economic and environmental friendly high-performance liquid chromatography methods for levofloxacin and minocycline quantification in biomimetic media were developed and validate including their stability at body temperature, an often neglected evaluation parameter. Both methods are similar only differing in the wavelength setting, i.e., for levofloxacin and minocycline quantification the UV detection was set at 284 and at 273 nm, respectively. The separation of both antibiotics was achieved using a reversed-phase column and a mobile phase consisting of acetonitrile and water (15:85) with 0.6% triethylamine, adjusted to pH 3. As an internal standard for levofloxacin quantification, minocycline was used and vice versa. The calibration curves for both methods were linear (r = 0.99) over a concentration range of 0.3–16 μg/mL and 0.5–16 μg/mL for levofloxacin and minocycline, respectively, with precision, accuracy and recovery in agreement with international guidelines requirement. Levofloxacin revealed stability in all media and conditions, including at 37°C, with exception to freeze–thaw cycle conditions. Minocycline presented a more accentuated degradation profile over prolonged time courses, when compared to levofloxacin. Reported data is of utmost interest for pharma and biomaterials fields regarding the research and development of new local drug-delivery-systems containing either of these two antibiotics, namely when monitoring the in vitro release studies of those systems. Simple, economic and environmental friendly high-performance liquid chromatography methods for levofloxacin and minocycline quantification in biomimetic media were developed and validate including their stability at body temperature, an often neglected evaluation parameter. Both methods are similar only differing in the wavelength setting, i.e., for levofloxacin and minocycline quantification the UV detection was set at 284 and at 273 nm, respectively. The separation of both antibiotics was achieved using a reversed-phase column and a mobile phase consisting of acetonitrile and water (15:85) with 0.6% triethylamine, adjusted to pH 3. As an internal standard for levofloxacin quantification, minocycline was used and vice versa. The calibration curves for both methods were linear (r = 0.99) over a concentration range of 0.3–16 μg/mL and 0.5–16 μg/mL for levofloxacin and minocycline, respectively, with precision, accuracy and recovery in agreement with international guidelines requirement. Levofloxacin revealed stability in all media and conditions, including at 37°C, with exception to freeze–thaw cycle conditions. Minocycline presented a more accentuated degradation profile over prolonged time courses, when compared to levofloxacin. Reported data is of utmost interest for pharma and biomaterials fields regarding the research and development of new local drug-delivery-systems containing either of these two antibiotics, namely when monitoring the in vitro release studies of those systems. This is a sample of graphical abstract. Simple, economic and fast HPLC methods for levofloxacin and minocycline analysis. Levofloxacin and minocycline quantification in NaCl, PBS and Müeller-Hinton media. Analytes quantification using the internal standard method. Stability studies of both antibiotics, including at body temperature. Validated methods with acceptable linearity, precision, accuracy and recovery. Useful for antibiotics monitoring through in vitro drug release and microbiological assays.Keywords:
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The purpose of this study was to compare the concentrations of levofloxacin and azithromycin in steady-state plasma, epithelial lining fluid (ELF), and alveolar macrophage (AM) after intravenous administration. Thirty-six healthy, nonsmoking adult subjects were randomized to either intravenous levofloxacin (500 or 750 mg) or azithromycin (500 mg) once daily for five doses. Venipuncture and bronchoscopy with bronchoalveolar lavage were performed in each subject at either 4, 12, or 24 h after the start of the last antibiotic infusion. The mean concentrations of levofloxacin and azithromycin in plasma were similar to those previously published. The dosing regimens of levofloxacin achieved significantly (P < 0.05) higher concentrations in steady-state plasma than azithromycin during the 24 h after drug administration. The respective mean (+/- standard deviation) concentrations at 4, 12, and 24 h in ELF for 500 mg of levofloxacin were 11.01 +/- 4.52, 2.50 +/- 0.97, and 1.24 +/- 0.55 micro g/ml; those for 750 mg of levofloxacin were 12.94 +/- 1.21, 6.04 +/- 0.39, and 1.73 +/- 0.78 micro g/ml; and those for azithromycin were 1.70 +/- 0.74, 1.27 +/- 0.47, and 2.86 +/- 1.75 micro g/ml. The differences in concentrations in ELF among the two levofloxacin groups and azithromycin were significantly (P < 0.05) higher at the 4- and 12-h sampling times. The respective concentrations in AM for 500 mg of levofloxacin were 83.9 +/- 53.2, 18.3 +/- 6.7, and 5.6 +/- 3.2 micro g/ml; those for 750 mg of levofloxacin were 81.7 +/- 37.0, 78.2 +/- 55.4, and 13.3 +/- 6.5 micro g/ml; and those for azithromycin were 650 +/- 259, 669 +/- 311, and 734 +/- 770 micro g/ml. Azithromycin achieved significantly (P < 0.05) higher concentrations in AM than levofloxacin at all sampling times. The concentrations in ELF and AM following intravenous administration of levofloxacin and azithromycin were higher than concentrations in plasma. Further studies are needed to determine the clinical significance of such high intrapulmonary concentrations in patients with respiratory tract infections.
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The bactericidal activities and postantibiotic effects (PAEs) of levofloxacin and gatifloxacin at concentrations corresponding to those in antibiotic eye drops against methicillin-resistant Staphylococcus aureus strains were determined. Levofloxacin and gatifloxacin at concentrations simulating those in eye drops showed lower bactericidal activities and shorter PAEs against fluoroquinolone-resistant strains than against fluoroquinolone-sensitive strains.
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Twelve volunteers received a single oral dose of 1,000 mg extended-release (XR) ciprofloxacin versus 500 mg levofloxacin to assess urinary bactericidal titers (UBTs) against common uropathogens. Areas under UBT-time curves were significantly larger for Proteus mirabilis with XR ciprofloxacin and for staphylococci with levofloxacin.
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AbstractThis open study was conducted in 72 outpatients with acne vulgaris, to compare the clinical efficacy and tolerability of azithromycin and minocycline. Azithromycin was administered as a single oral dose (500 mg/day) for 4 days in four cycles every 10 days and minocycline was administered 100 mg daily for 6 weeks. Improvement was assessed 6 weeks after initiation of treatment with a four-graded scale. A satisfactory clinical response was observed in 75.8% of the patients treated with azithromycin and in 70.5% of those treated with minocycline. There were no significant differences between these two acne treatments in terms of reduction of the number of lesions (p> 0.05). Both agents were well tolerated and mild side effects were reported in 10.3% of azithromycin and 11.7% of minocycline treated patients. We conclude that azithromycin is at least as clinically effective and well tolerated as minocycline as treatment of facial comedonic and papulopustular acne.
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Tetracycline, doxycycline, and minocycline were evaluated for their antibacterial activity against methicillin-susceptible and -resistant isolates of Staphylococcus . At clinically achievable levels both doxycycline and minocycline were more active than tetracycline against methicillin-susceptible organisms. Tetracycline and doxycycline had no activity against methicillin-resistant staphylococci, whereas minocycline at 2 μg/ml inhibited six of 13 strains and, at 3 μg/ml, 10 of 13 strains.
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