Enrofloxacin hydrochloride dihydrate

Miranda-Calderón, Jorge E.; Gutiérrez, Lilia; Flores-Álamo, Marcos; García-Gutiérrez, Ponciano; López, Héctor Sumano

doi:10.1107/s1600536814006059

Cited by 10 publications

(19 citation statements)

References 8 publications

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“…Polymorphic forms are determined with identical chemical manipulation of enrofloxacin. As previously reported (Miranda‐Calderon et al ., ), structure of enro C elicited by X‐ray diffraction analysis corresponds to solvate form of enrofloxacin hydrochloride with two water molecules (see Fig. ).…”

Section: Resultsmentioning

confidence: 98%

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Gutiérrez¹,

Miranda-Calderón²,

García-Gutiérrez

et al. 2014

Vet Pharm & Therapeutics

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Enrofloxacin, a key antimicrobial agent in commercial avian medicine, has limited bioavailability (60%). This prompted its chemical manipulation to yield a new solvate-recrystallized enrofloxacin hydrochloride dihydrate entity (enroC ). Its chemical structure was characterized by means of mass spectroscopy, Fourier transformed infrared spectroscopy, X-ray powder diffraction, and thermal analysis. Comparative oral pharmacokinetics (PK) of reference enrofloxacin (enroR ) and enroC in broiler chickens after oral administration revealed noticeable improvements in key parameters and PK/PD ratios. Maximum serum concentration values were 2.61 ± 0.21 and 5.9 ± 0.42 μg/mL for enroR and enroC , respectively; mean residence time was increased from 5.50 ± 0.26 h to 6.20 ± 0.71 h and the relative bioavailability of enroC was 336%. Considering Cmax /MIC and AUC/MIC ratios and the MIC values for a wild-type Escherichia coli O78/H12 (0.25 μg/mL), optimal ratios will only be achieved by enroC (Cmax /MIC = 23.6 and AUC/MIC = 197.7 for enroC ; vs. Cmax /MIC = 10.4 and AUC/MIC = 78.1 for enroR ). Furthermore, enroC may provide in most cases mutant prevention concentrations (Cmax /MIC ≥ 16). Ready solubility of powder enroC in drinking water at concentrations regularly used (0.01%) to provide an additional advantage of enroC in the field. Further development of enroC is warranted before it can be recommended for clinical use in veterinary medicine.

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Section: Resultsmentioning

confidence: 98%

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Gutiérrez¹,

Miranda-Calderón²,

García-Gutiérrez

et al. 2014

Vet Pharm & Therapeutics

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“…Failure to attain these ratios has been linked to an increase in bacterial resistance and lack of clinical efficacy (20). Synthesis of a solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C) (13) with improved pharmacokinetics has been advanced as means to obtain improved PK/PD ratios (14,15) and, ideally, to achieve theoretical mutant-preventive concentrations (C MAX ≥ 16 MIC) (21). Enro-C exhibits different physicochemical properties from the parent compound, mainly water solubility (13) and pharmacokinetics, as has been so far shown in broilers (15).…”

Section: Discussionmentioning

confidence: 99%

“…A new solvate of enrofloxacin is already available for research (enrofloxacin hydrochloridedihydrate, enro-C) (14), and it has shown improved PK values in broilers (15). Hence, the aim of this trial was to determine the PK and the PK/PD ratios of enrofloxacin from enro R and from enro-C in Syrian golden hamsters while assessing as pharmacodynamic markers the MIC values for methicillin-resistant Staphylococcus aureus, Leptospira interrogans, and Escherichia coli.…”

Section: Introduction Enrofloxacinmentioning

confidence: 99%

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Carrascosa¹,

Peã'a²,

Gutiérrez³

et al. 2015

Turk J Vet Anim Sci

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Pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD ratios of a new solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C), were studied in hamsters. Enrofloxacin from Baytril® 5% (enro R) served as the reference preparation. Two groups of 60 Syrian golden hamsters were intramuscularly injected individually with 10 mg/kg of enro R or with enro-C. Tissue and serum samples were obtained for 72 h; enrofloxacin concentrations were determined by HPLC with UV detection. Ninety percent minimum inhibitory concentrations (MIC 90 ) were determined for strains of methicillin-resistant Staphylococcus aureus, Leptospira interrogans, and Escherichia coli. All PK variables were statistically different between groups (P < 0.01). C MAX of enrofloxacin for enro-C was 17.3 µg/mL and it was 2.6 µg/mL for enro R . AUC was considerably higher for enro-C (459.2 µg/mL h vs. 19.9 µg/mL h). There were no statistically significant differences in MIC 90 values between enro R and enro-C. Tissue concentrations of enro-C in all cases were higher and remained above the MIC for longer periods than those of enro R . Relevant PK/PD ratios for enrofloxacin (AUC/MIC ≥ 125 and C MAX > MIC = 10-12) are consequently superior for enro-C. Given the outstanding PK/PD ratios of enro-C, this new moiety is proposed as a possible solution when high tissue concentrations of enrofloxacin are necessary.

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“…However, to the best of our knowledge, no commercial preparations Serum and milk concentrations of enrofloxacin in cows intramammarily treated with a new enrofloxacin-polymorph 1) for this route exist in most countries, and the available products for parenteral administration have a pH at or above 10.4; a fact that makes intramammary administration of the drug rather unadvisable (28). However, a new recrystallized enrofloxacin polymorphic form, enrofloxacin hydrochloride-dihydrate (enro-C) (19), has shown higher water solubility than the parent compound and a superior bioavailability than reference enrofloxacin in broiler chicken (12). As a 1.5% suspension, enro-C exhibits a pH of 5.5, and it does not irritate the mammary gland when intramammarily administered (17).…”

Section: Praca Oryginalnamentioning

confidence: 99%

“…The physicochemical characteristics of enro-C include higher water solubility than that of the parent molecule (19). Yet, this feature was not sufficient to make it possible to prepare a solution rather than a suspension of 300 mg of enro-C in 20 mL.…”

Section: Tab 4 Serum Pharmacokinetic Parameters For Enrofloxacin Anmentioning

confidence: 99%

Serum and milk concentrations of enrofloxacin in cows intramammarily treated with a new enrofloxacin-polymorph

Martínez-Cortés¹,

Gutiérrez²,

Tapia³

et al. 2016

Medycyna Weterynaryjna

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SummaryThe success rate in treatment against Staphylococcus aureus mastitis with antibacterial drugs is marginal. Low antibacterial drug concentrations in the mammary tissue is part of the reason for this failure. Enrofloxacin has only been administered on few occasions through the intramammary route i.e., combined with gentamicin in an undisclosed vehicle or dose. A new solvate form of enrofloxacin (enrofloxacin hydrochloride-dihydrate (enro-C)) prepared as 1.5% suspension pH 5.5 was tested in a field mastitis outbreak due to coagulase-negative S. aureus (CNS) in F1 (Holstein/Zebu) cows aged 5-8 years destined to be culled. Enro-C was administered intramammarily daily (300 mg/infected quarter) for 8 days both to healthy and mastitic cows; milk and serum enro-C concentrations were determined on days 1 and 8. Maximum serum concentration (C MAX ) values were similar in both groups (9.4 to 10.7 µg/mL). The area under the moment curve (AUMC) for enrofloxacin increased only by 11% in healthy cows and by 10% in infected cows from day 1 to day 8, a fact that suggests little accumulation with this dose regime. Peak concentrations in milk ranged from 18.5 to 19.8 µg/mL on day 1 and from 20.2 to 22 µg/mL on day 8. Cure rates on day 21 after treatment were 75% (12 out of 16 cows) or 69.4% (26 out of 36 glands). Somatic cell counts and California mastitis test showed a positive trend in cured animals. Uniquely high milk enrofloxacin and ciprofloxacin concentrations were obtained after intramammary administration of enro-C. These concentrations seem effective for treating CNS mastitis. The feasibility of incorporating this experimental pharmaceutical preparation of enrofloxacin is discussed.

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Enrofloxacin hydrochloride dihydrate

Cited by 10 publications

References 8 publications

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate

Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters

Serum and milk concentrations of enrofloxacin in cows intramammarily treated with a new enrofloxacin-polymorph

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