In vitro and in vivo evaluation of levofloxacin sustained-release capsules

Yin, Lifang; Huang, Shi-Jing; Jiang, Shuguang; Zhao, Chunjie; Pei, Zhi-Qiang; Qiang, Zhang

doi:10.3109/03639045.2010.489562

Cited by 5 publications

(2 citation statements)

References 26 publications

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“…To our knowledge, there is only a single report of the pharmacokinetics of LFX after oral administration in dogs at supratherapeutic dose (Yin et al., ); therefore, the aims of this study were to describe LFX pharmacokinetics in dogs after single 2.5 mg/kg intravenous and 5 mg/kg subcutaneous and oral administration and, considering that dose proportionality has been reported for LFX in dogs (FDA, , Yin et al., ), to assess and foresee by applying Monte Carlo simulation the probability of a favourable outcome in a large population of two oral (5 and 10 mg/kg) and two SC (5 and 7.5 mg/kg) dosage regimens.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of levofloxacin after single intravenous, oral and subcutaneous administration to dogs

Landoni

Albarellos

2018

Vet Pharm & Therapeutics

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The pharmacokinetic properties of the fluoroquinolone levofloxacin (LFX) were investigated in six dogs after single intravenous, oral and subcutaneous administration at a dose of 2.5, 5 and 5 mg/kg, respectively. After intravenous administration, distribution was rapid (T½dist 0.127 ± 0.055 hr) and wide as reflected by the volume of distribution of 1.20 ± 0.13 L/kg. Drug elimination was relatively slow with a total body clearance of 0.11 ± 0.03 L kg−1 hr−1 and a T½ for this process of 7.85 ± 2.30 hr. After oral and subcutaneous administration, absorption half‐life and Tmax were 0.35 and 0.80 hr and 1.82 and 2.82 hr, respectively. The bioavailability was significantly higher (p ˂ 0.05) after subcutaneous than oral administration (79.90 vs. 60.94%). No statistically significant differences were observed between other pharmacokinetic parameters. Considering the AUC24 hr/MIC and Cmax/MIC ratios obtained, it can be concluded that LFX administered intravenously (2.5 mg/kg), subcutaneously (5 mg/kg) or orally (5 mg/kg) is efficacious against Gram‐negative bacteria with MIC values of 0.1 μg/ml. For Gram‐positive bacteria with MIC values of 0.5 μg/kg, only SC and PO administration at a dosage of 5 mg/kg showed to be efficacious. MIC‐based PK/PD analysis by Monte Carlo simulation indicates that the proposed dose regimens of LFX, 5 and 7.5 mg/kg/24 hr by SC route and 10 mg/kg/24 hr by oral route, in dogs may be adequate to recommend as an empirical therapy against S. aureus strains with MIC ≤ 0.5 μg/ml and E. coli strains with MIC values ≤0.125 μg/ml.

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Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of levofloxacin after single intravenous, oral and subcutaneous administration to dogs

Landoni

Albarellos

2018

Vet Pharm & Therapeutics

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“…Aqueous dispersions of ethylcellulose are often used to overcome environmental and economic challenges associated with organic systems. Surelease® is a fully formulated aqueous dispersion system containing ethylcellulose, plasticizers and stabilizers (Leng DE, Warner, G.L 1977;Leng DE, Mossbach, W., Sigelko, W.L, Sounders, F.L., Uirumaa, R.S, 1985) and is widely used in investigational and commercial controlled release dosage forms (Jagadeesh and Bala Ramesha Chary 2011;Paul et al 2011;Vonica et al 2011;Yin et al 2011;Melegari et al 2016;Afrasiabi Garekani et al 2017;Kazlauske et al 2017;Patil and Belsare 2017).…”

Section: Introductionmentioning

confidence: 99%

Multivariate analysis as a method to understand variability in a complex excipient, and its contribution to formulation performance

Tobyn

Ferreira

Lightfoot

et al. 2018

Pharmaceutical Development and Technology

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A key part of the Risk Assessment of excipients is to understand how raw material variability could (or does) contribute to differences in performance of the drug product. Here we demonstrate an approach which achieves the necessary understanding for a complex, functional, excipient. Multivariate analysis (MVA) of the certificates of analysis of an ethylcellulose aqueous dispersion (Surelease) formulation revealed low overall variability of the properties of the systems. Review of the scores plot to highlight batches manufactured using the same ethylcellulose raw material in the formulation, indicated that these batches tend to be more closely related than other randomly selected batches. This variability could result in potential differences in the quality of drug product lots made from these batches. Manufacture of a model drug product from Surelease batches coated using different lots of starting material revealed small differences in the release of a model drug, which could be detected by certain model dependent dissolution modelling techniques, but they were not observed when using model-independent techniques. This illustrates that the techniques are suitable for detecting and understanding excipient variability, but that, in this case, the product was still robust.

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Levofloxacin in veterinary medicine: a literature review

Sitovs

Sartini

Giorgi

2021

Research in Veterinary Science

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In vitro and in vivo evaluation of levofloxacin sustained-release capsules

Abstract: Statistical analysis indicated that the capsules containing Surelease-coated pellets had a satisfactory sustained-release behavior and a desired pharmacokinetic property.

Cited by 5 publications

References 26 publications

Pharmacokinetics of levofloxacin after single intravenous, oral and subcutaneous administration to dogs

Pharmacokinetics of levofloxacin after single intravenous, oral and subcutaneous administration to dogs

Multivariate analysis as a method to understand variability in a complex excipient, and its contribution to formulation performance

Levofloxacin in veterinary medicine: a literature review

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