Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Levofloxacin

Koeppe, Marcelle O.; Cristofoletti, Rodrigo; Fernandes, Eduardo F.; Storpirtis, Sílvia; Junginger, Hans E.; Kopp, Sabine; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.22413

Cited by 39 publications

(16 citation statements)

References 41 publications

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“…It has been used in the treatment of community-acquired pneumonia, acute maxillary sinusitis and acute exacerbation of chronic bronchitis. Levofloxacin belongs to BCS class I, having pH dependent solubility in water (Koeppe et al, 2011). However, it is quickly absorbed and 87% of the oral dose is excreted unchanged in the urine (Neu, 1992).…”

Section: Introductionmentioning

confidence: 99%

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

et al. 2016

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Context: Vesicular systems have attracted great attention in drug delivery because of their amphiphilicity, biodegradability, non-toxicity and potential for increasing drug bioavailability. Objective: A novel sugar-based double-tailed surfactant containing renewable block was synthesized for preparing niosomal vesicles that could be exploited for Levofloxacin encapsulation, aiming to increase its oral bioavailability. Materials and methods: The surfactant was characterized by 1 H NMR, mass spectroscopy and Fourier transform infrared spectroscopy (FT-IR). Its biocompatibility was studied against cell cultures and human blood hemolysis. In vivo acute toxicity was evaluated in mice. The vesicle morphology, size, drug-excipients interaction and entrapment efficiency (EE) were examined using atomic force microscope (AFM), dynamic light scattering (DLS), FT-IR and HPLC. Oral bioavailability studies of Levofloxacin in surfactant-based niosomal formulation were carried out using rabbits and plasma samples were analyzed using HPLC. Results and discussion: Vesicles were spherical in shape and the size was 190.31 ± 4.51 nm with a polydispersity index (PDI) of 0.29 ± 0.03. The drug EE in niosomes was 68.28 ± 3.45%. When applied on cell lines, high cell viability was observed even after prolonged exposure at high concentrations. It caused 5.77 ± 1.34% hemolysis at 1000 mg/mL and was found to be safe up to 2000 mg/kg. Elevated Levofloxacin plasma concentration was achieved when delivered with novel vesicles. Conclusion:The surfactant was demonstrated to be safe and effective as carrier of Levofloxacin. The study suggests that this sugar-based double-tailed nonionic surfactant could be promising nano-vesicular system for delivery and enhancing oral bioavailability of the hydrophobic Levofloxacin.

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Section: Introductionmentioning

confidence: 99%

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

et al. 2016

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“…For acyclovir, atenolol, cimetidine, ciprofloxacin, furosemide, ibuprofen, lamivudine, levofloxacin, and ranitidine, the highest single dose recommended for administration in the SmPC is equal to the highest dosage strength available, so for these drugs, the BCS classification and hence the biowaiver recommendation is not altered . The solubility values for acetaminophen (paracetamol), chloroquine salts, doxycycline, ethambutol, isoniazid, metronidazole, propranolol, pyrazinamide, and quinidine are all very high.…”

Section: Resultsmentioning

confidence: 99%

The Impact of the EMA Change in Definition of “Dose” on the BCS Dose–Solubility Ratio: A Review of the Biowaiver Monographs

Sediq

Kubbinga

Langguth

et al. 2014

Journal of Pharmaceutical Sciences

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“…Ceftriaxone is a basic compound with pKa value of 1.72, 3.15, and 4.34 , its retention time decreased with the increase of pH because ceftriaxone molecule contains the ionizable groups (–OH, –COOH, –NH 2 ). Levofloxacin is a zwitterion at physiological pH, possessing a carboxylic group with pKa = 5.5, a piperazinyl group with pKa = 8.0, and another proton accepting function with pKa = 6.8 ± 0.3 . When pH increases from 3.5 to 4.5, its retention time increased from 6.0 to 6.25 min, but when pH increases to 5.3 its retention time increased to 7.4 min.…”

Section: Resultsmentioning

confidence: 99%

Simultaneous Determination of the Combined Drugs of Ceftriaxone Sodium, Metronidazole, and Levofloxacin in Human Urine by High‐Performance Liquid Chromatography

Sun

Wang

2012

Clinical Laboratory Analysis

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Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Levofloxacin

Cited by 39 publications

References 41 publications

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

The Impact of the EMA Change in Definition of “Dose” on the BCS Dose–Solubility Ratio: A Review of the Biowaiver Monographs

Simultaneous Determination of the Combined Drugs of Ceftriaxone Sodium, Metronidazole, and Levofloxacin in Human Urine by High‐Performance Liquid Chromatography

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