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Home / Equine Research Bank / Can J Vet Res / Pharmacokinetics of orbifloxacin and its concentration in bo...
Canadian journal of veterinary research = Revue canadienne de recherche veterinaire2001; 65(3); 181-187;

Pharmacokinetics of orbifloxacin and its concentration in body fluids and in endometrial tissues of mares.

Abstract: Pharmacokinetics and distribution of orbifloxacin into body fluids and endometrium was studied in 6 mares after intragastric (IG) administration at a single dose rate of 7.5 mg/kg body weight. Orbifloxacin concentrations were serially measured in serum, synovial fluid, peritoneal fluid, urine, cerebrospinal fluid, and endometrial tissues over 24 hours. Minimum inhibitory concentrations of orbifloxacin were determined for 120 equine pathogens over an 11-month period. The mean peak serum concentration (Cmax) was 2.41+/-0.30 microg/mL at 1.5 hours after administration and decreased to 0.17+/-0.01 microg/mL (Cmin) at 24 hours. The mean elimination half-life (t1/2) was 9.06+/-1.33 hours and area under the serum concentration vs time curve (AUC) was 20.54+/-1.70 mg h/L. Highest mean peritoneal fluid concentration was 2.15+/-0.49 microg/mL at 2 hours. Highest mean synovial fluid concentration was 1.17+/-0.28 microg/mL at 4 hours. Highest mean urine concentration was 536.67+/-244.79 microg/mL at 2 hours. Highest mean endometrial concentration was 0.72+/-0.23 microg/g at 1.5 hours. Mean CSF concentration was 0.46+/-0.55 microg/mL at 3 hours. The minimum inhibitory concentration of orbifloxacin required to inhibit 90% of isolates (MIC90) ranged from 8.0 microg/mL, with gram-negative organisms being more sensitive than gram-positive organisms. Orbifloxacin was uniformly absorbed in the 6 mares and was well distributed into body fluids and endometrial tissue. At a dosage of 7.5 mg/kg once a day, many gram-negative pathogens, such as Actinobacillus equuli, Escherichia coli, Pasteurella spp., and Salmonella spp. would be expected to be susceptible to orbifloxacin.
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Publication Date: 2001-08-02 PubMed ID: 11480524PubMed Central: PMC1189673
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  • Non-U.S. Gov't

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research article focuses on the pharmacokinetics and distribution of the drug orbifloxacin in mares after a single dosage, and how this drug’s concentration varies in different body fluids and endometrial tissues over a 24-hour period. The study also looks at the minimum inhibitory concentrations of orbifloxacin required to inhibit common equine pathogens.

Pharmacokinetics of Orbifloxacin

  • The experiment was conducted on 6 mares given a single intragastric administration of orbifloxacin at a dosage of 7.5 mg/kg body weight.
  • The researchers measured the concentrations of orbifloxacin in different body fluids (serum, synovial fluid, peritoneal fluid, urine, cerebrospinal fluid) and endometrial tissues over a 24-hour period.
  • Results showed that the mean peak concentration of orbifloxacin in serum was 2.41 micrograms/mL at 1.5 hours after administration, which decreased to 0.17 micrograms/mL at 24 hours.
  • The mean elimination half-life was 9.06 hours and the area under the serum concentration vs time curve (AUC) was 20.54 mg h/L, indicating that the drug was reasonably sustained in the bloodstream.

Orbifloxacin Concentration in Body Fluids and Endometrial Tissues

  • The highest mean concentration of orbifloxacin in peritoneal fluid was 2.15 micrograms/mL at 2 hours after administration
  • The highest concentration in synovial fluid was 1.17 micrograms/mL at 4 hours after administration
  • The highest concentration in urine was 536.67 micrograms/mL at 2 hours after administration
  • The highest concentration in endometrial tissues was 0.72 micrograms/g at 1.5 hours after administration
  • A mean cerebrospinal fluid concentration of 0.46 micrograms/mL was noted at 3 hours after administration.

Inhibitory Concentration of Orbifloxacin on Equine Pathogens

  • The researchers determined the minimum inhibitory concentrations of orbifloxacin on 120 equine pathogens over an 11-month period.
  • The minimum inhibitory concentration required to inhibit 90% of the equine pathogens (MIC90) ranged from less than or equal to 0.12 to over 8.0 micrograms/mL.
  • Gram-negative organisms were found to be more sensitive to orbifloxacin than gram-positive organisms, implying orbifloxacin could be particularly effective against these pathogens.

Implication of the Study

  • The researchers concluded that orbifloxacin was uniformly absorbed by the mares and well-distributed across body fluids and endometrial tissues.
  • Given the dosage of 7.5 mg/kg once a day, many gram-negative pathogens, including Actinobacillus equuli, Escherichia coli, Pasteurella spp., and Salmonella spp. are expected to be susceptible to orbifloxacin treatment.

Cite This Article

APA
Haines GR, Brown MP, Gronwall RR, Merritt KA, Baltzley LK. (2001). Pharmacokinetics of orbifloxacin and its concentration in body fluids and in endometrial tissues of mares. Can J Vet Res, 65(3), 181-187.

Publication

Canadian journal of veterinary research = Revue canadienne de recherche veterinaire
ISSN: 0830-9000
NlmUniqueID: 8607793
Country: Canada
Language: English
Volume: 65
Issue: 3
Pages: 181-187

Researcher Affiliations

Haines, G R
  • Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville 32610-0136, USA.
Brown, M P
    Gronwall, R R
      Merritt, K A
        Baltzley, L K

          MeSH Terms

          • Animals
          • Area Under Curve
          • Ascitic Fluid / chemistry
          • Ascitic Fluid / metabolism
          • Bacteria / drug effects
          • Body Fluids / chemistry
          • Body Fluids / metabolism
          • Ciprofloxacin / analogs & derivatives
          • Ciprofloxacin / analysis
          • Ciprofloxacin / pharmacokinetics
          • Ciprofloxacin / pharmacology
          • Endometrium / chemistry
          • Endometrium / metabolism
          • Female
          • Half-Life
          • Horses / metabolism
          • Intestinal Absorption
          • Microbial Sensitivity Tests / veterinary
          • Synovial Fluid / chemistry
          • Synovial Fluid / metabolism
          • Tissue Distribution

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          Citations

          This article has been cited 4 times.
          1. Yang YR, Yang F, Sun N, Wang GY. Disposition kinetics of orbifloxacin in tissues of crucian carp (Carassius auratus) following a single intramuscular administration.. Iran J Vet Res 2019 Spring;20(2):131-135.
            pubmed: 31531036
          2. Cazedey EC, Salgado HR. Development and validation of a microbiological agar assay for determination of orbifloxacin in pharmaceutical preparations.. Pharmaceutics 2011 Aug 29;3(3):572-81.
            doi: 10.3390/pharmaceutics3030572pubmed: 24310597google scholar: lookup
          3. Gebru E, Lee JS, Chang ZQ, Hwang MH, Cheng H, Park SC. Integration of pharmacokinetic and pharmacodynamic indices of orbifloxacin in beagle dogs after a single intravenous and intramuscular administration.. Antimicrob Agents Chemother 2009 Jul;53(7):3024-9.
            doi: 10.1128/AAC.01346-08pubmed: 19398644google scholar: lookup
          4. Adams AR, Haines GR, Brown MP, Gronwall R, Merritt K. Pharmacokinetics of difloxacin and its concentration in body fluids and endometrial tissues of mares after repeated intragastric administration.. Can J Vet Res 2005 Jul;69(3):229-35.
            pubmed: 16187554
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