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Journals / Turkish Journal of Veterinary and Animal Sciences / 2015 / Cilt: 39 - Sayı: 6

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

Alma CARRASCOSA
Alejandro De La PEÃ'A
Lilia GUTIERREZ
Hector SUMANO
Pages
661–667
Publication Date
2015-12-04
DOI
—
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

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.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Pharmacokinetics (PK), pharmacodynamics (PD), and PK/PD ratios of a new solvate of enrofloxacin (enrofloxacin hydrochloride-dihydrate; enro-C), were studied in hamsters.
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Key Findings & Data:Enrofloxacin from Baytril1397904493 5% (enroR) served as the reference preparation.
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Conclusion & Impact: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.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Enrofloxacin · enro-C · hamster

Abstract

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 Baytril1397904493 5% (enroR) served as the reference preparation. Two groups of 60 Syrian golden hamsters were intramuscularly injected individually with 10 mg/kg of enroR 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 (MIC90) 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). CMAX of enrofloxacin for enro-C was 17.3 &mu;g/mL and it was 2.6 &mu;g/mL for enroR. AUC was considerably higher for enro-C (459.2 &mu;g/mL h vs. 19.9 &mu;g/mL h). There were no statistically significant differences in MIC90 values between enroR and enro-C. Tissue concentrations of enro-C in all cases were higher and remained above the MIC for longer periods than those of enroR. Relevant PK/PD ratios for enrofloxacin (AUC/MIC ? 125 and CMAX > 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.

Özet

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 Baytril1397904493 5% (enroR) served as the reference preparation. Two groups of 60 Syrian golden hamsters were intramuscularly injected individually with 10 mg/kg of enroR 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 (MIC90) 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). CMAX of enrofloxacin for enro-C was 17.3 &mu;g/mL and it was 2.6 &mu;g/mL for enroR. AUC was considerably higher for enro-C (459.2 &mu;g/mL h vs. 19.9 &mu;g/mL h). There were no statistically significant differences in MIC90 values between enroR and enro-C. Tissue concentrations of enro-C in all cases were higher and remained above the MIC for longer periods than those of enroR. Relevant PK/PD ratios for enrofloxacin (AUC/MIC ? 125 and CMAX > 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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Cite This Article

CARRASCOSA, A., PEÃ'A, A. D. L., GUTIERREZ, L., SUMANO, H. (2015). Serum pharmacokinetics and tissue concentrations of a newrecrystallized enrofloxacin hydrochloride-dihydrate in hamsters. Turkish Journal of Veterinary and Animal Sciences, Cilt: 39 - Sayı: 6, 661–667. https://ajindex.com/articles/121321

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References (10)

  1. Wolfson S, Hooper DC. The fluoroquinolones: structures, mechanisms of action and resistance, and spectra of activity in vitro. Antimicrob Agents Chemother 1985; 28: 581–586. 2. O’Donnell JA, Gelone SP. Fluoroquinolones. Infect Dis Clin N Am 2000; 14: 489–513. 3. Lizondo M, Pons M, Gallardo, M, Estelrich J. Physicochemical properties of enrofloxacin. J Pharm Biomed An 1997; 15: 1845–1849.
  2. Sumano LH, Gutiérrez OL, Zamora MA. Bioequivalence of four preparations of enrofloxacin in poultry. J Vet Pharmacol Ther 2001; 24: 309–313.
  3. Sumano LH, Ocampo CL, Gutierrez OL. Non-bioequivalence of 9 trademarks of enrofloxacin and Baytril® in cows. Dtsch Tierarzt Woschernscrift 2001; 108: 311–314.
  4. Sumano LH, Gutierrez OL, Zamora QM. Strategic administration of enrofloxacin in poultry to achieve higher maximal serum concentrations. Vet J 2003; 65: 143–148. 7. Sumano H, Gutierrez L, Ocampo L. Bioequivalence comparison of seventeen commercial oral enrofloxacins against the original pioneer preparation in broilers. J Poultry Sci 2006; 43: 23–28.
  5. Karanam M, Choudhury AR. Structural landscape of pure enrofloxacin and its novel salts: enhanced solubility for better pharmaceutical applicability. Cryst Growth Des 2013; 13: 1626–1637. Sárközy G. Quinolones: a class of antimicrobial agents. Vet Med 2001; 46: 257–274.
  6. Wright DH, Brown GH, Peterson ML, Rotschafer JC. Application of fluoroquinolone pharmacodynamics. J Antimicrob Chemother 2000; 46: 669–683.
  7. Randall P, Cooles SW, Coldham C, Stapleton KS, Piddock LJV, Woodward MJ. Modification of enrofloxacin treatment regimens for poultry experimentally infected with Salmonella enterica serovar typhimurium DT104 to minimize selection of resistance. Antimicrob Agents Chemother 2006; 50: 4030– 4037. Sumano H, Cortes-Cuevas A, Rosario C, Gutiérrez L. Assessment of key pharmacokinetic variables of bioequivalent and non-bioequivalent enrofloxacin preparations under various water management conditions. J Poultry Sci 2010; 47: 262–268.
  8. Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharm 2012; 1: 1–10.
  9. Miranda-Calderon JE, Gutierrez L, Flores-Alamo MP, García- Gutierrez P, Sumano H. Enrofloxacin hydrochloride dihydrate. Acta Crystallogr E 2014; 70: 468–469.
  10. Gutierrez L, Miranda-Calderon JE, Garcia-Gutierrez P, Sumano H. Physicochemical characterization and pharmacokinetics in broiler chickens of a new recrystallized enrofloxacin hydrochloride dihydrate. J Vet Pharmacol Ther 2015; 38: 183– 189. El