J Vet Sci.  2007 Dec;8(4):353-356. 10.4142/jvs.2007.8.4.353.

Clinical pharmacokinetics of norfloxacin-glycine acetate after intravenous and oral administration in pigs

Affiliations
  • 1College of Veterinary Medicine, Kyungpook National University, Daegu 702-701, Korea. parksch@knu.ac.kr
  • 2Lee Gil Ya Cancer and Diabetes Institute, Gachon University of Medicine and Science, Incheon 406-840, Korea.
  • 3College of Veterinary Medicine, Chonnam National University, Kwangju 500-757, Korea.
  • 4National Veterinary Research and Quarantine Service, Anyang 430-824, Korea.
  • 5College of Veterinary Medicine, Chungnam National University, Daejeon 302-305, Korea.

Abstract

The pharmacokinetics and dosage regimen of norfloxacin-glycine acetate (NFLXGA) was investigated in pigs after a single intravenous (i.v.) or oral (p.o.) administration at a dosage of 7.2 mg/kg body weight. After both i.v. and p.o. administration, plasma drug concentrations were best fitted to an open two-compartment model with a rapid distribution phase. After i.v. administration of NFLXGA, the distribution (t1/2alpha) and elimination half-life (t1/2beta) were 0.36 +/- 0.07 h and 7.42 +/- 3.55 h, respectively. The volume of distribution of NFLXGA at steady state (Vdss) was 4.66 +/- 1.39 l/kg. After p.o. administration of NFLXGA, the maximal absorption concentration (Cmax) was 0.43 +/- 0.06 microgram/ ml at 1.36 +/- 0.39 h (Tmax). The mean absorption (t1/2ka) and elimination half-life (t1/2beta) of NFLXGA were 0.78 +/- 0.27 h and 7.13 +/- 1.41 h, respectively. The mean systemic bioavailability (F) after p.o. administration was 31.10 +/- 15.16%. We suggest that the optimal dosage calculated from the pharmacokinetic parameters is 5.01 mg/kg per day i.v. or 16.12 mg/kg per day p.o.

Keyword

norfloxacin; pharmacokinetics; pig

MeSH Terms

Administration, Oral
Animals
Anti-Bacterial Agents/administration & dosage/blood/*pharmacokinetics
Biological Availability
Cross-Over Studies
Glycine/administration & dosage/*analogs & derivatives/blood/pharmacokinetics
Half-Life
Injections, Intravenous/veterinary
Male
Norfloxacin/administration & dosage/*analogs & derivatives/blood/pharmacokinetics
Swine/*metabolism
Time Factors

Figure

  • Fig. 1 Serum concentration of norfloxacin following i.v. (▲) or p.o. (■) administration of 7.2 mg NFLXGA per kg body weight (n = 6).


Cited by  1 articles

Modification of pharmacokinetics of norfloxacin following oral administration of curcumin in rabbits
B. H. Pavithra, N. Prakash, K. Jayakumar
J Vet Sci. 2009;10(4):293-297.    doi: 10.4142/jvs.2009.10.4.293.


Reference

1. Al-Rashood K, Al-Khamis K, El-Sayed Y, Al-Bella S, Al-Yamani M, Alam S, Dham R. Bioequivalence evaluation of norfloxacin 400 mg tablets (Uroxin and Noroxin) in healthy human volunteers. Biopharm Drug Dispos. 2000. 21:175–179.
Article
2. Anadón A, Martinez-Larrañaga MR, Díaz MJ, Fernandez R, Martinez MA, Fernandez MC. Pharmacokinetics and tissue residues of norfloxacin and its N-desethyl- and oxo-metabolites in healthy pigs. J Vet Pharmacol Ther. 1995. 18:220–225.
Article
3. Anadón A, Martinez-Larrañaga MR, Velez C, Díaz MJ, Bringas P. Pharmacokinetics of norfloxacin and its N-desethyl- and oxo-metabolites in broiler chickens. Am J Vet Res. 1992. 53:2084–2089.
4. Brown SA, Cooper J, Gauze JJ, Greco DS, Weise DW, Buck JM. Pharmacokinetics of norfloxacin in dogs after single intravenous and single and multiple oral administrations of the drug. Am J Vet Res. 1990. 51:1065–1070.
5. Fang KC, Chen YL, Sheu JY, Wang TC, Tzeng CC. Synthesis, antibacterial and cytotoxic evaluation of certain 7-substituted norfloxacin derivatives. J Med Chem. 2000. 43:3809–3812.
Article
6. Freddo RJ, Dalla Costa T. Determination of norfloxacin free interstitial levels in skeletal muscle by microdialysis. J Pharm Sci. 2002. 91:2433–2440.
Article
7. Gilfillan EC, Pelak BA, Bland JA, Malatesta PF, Gadebusch HH. Pharmacokinetic studies of norfloxacin in laboratory animals. Chemotherapy. 1984. 30:288–296.
Article
8. Gips M, Soback S. Norfloxacin pharmacokinetics in lactating cows with sub-clinical and clinical mastitis. J Vet Pharmacol Ther. 1999. 22:202–208.
Article
9. Gips M, Soback S. Norfloxacin nicotinate pharmacokinetics in unweaned and weaned calves. J Vet Pharmacol Ther. 1996. 19:130–134.
Article
10. González F, San Andrés MI, Nieto J, San Andrés MD, Waxman S, Vicente ML, Lucas JJ, Rodríguez C. Influence of ruminal distribution on norfloxacin pharmacokinetics in adult sheep. J Vet Pharmacol Ther. 2001. 24:241–245.
Article
11. Hooper DC, Wolfson JS. Quinolone Antimicrobial Agents. 1995. 2nd ed. Washington DC: American Society of Microbiology Press.
12. Laczay P, Semjén G, Nagy G, Lehel J. Comparative studies on the pharmacokinetics of norfloxacin in chickens, turkeys and geese after a single oral administration. J Vet Pharmacol Ther. 1998. 21:161–164.
Article
13. Lavy E, Ziv G, Glickman A. Intravenous disposition kinetics, oral and intramuscular bioavailability and urinary excretion of norfloxacin nicotinate in donkeys. J Vet Pharmacol Ther. 1995. 18:101–107.
Article
14. Neuman M. Clinical pharmacokinetics of the newer antibacterial 4-quinolones. Clin Pharmacokinet. 1988. 14:96–121.
Article
15. Park SC. Comparative pharmacokinetic profiles of a newly formulated norfloxacin glycine acetate in various animal species. 1996. Korea: Chungnam National University;Ph.D Dissertation.
16. Park SC, Yun HI, Oh TK. Comparative pharmacokinetics and tissue distribution of norfloxacin-glycine acetate in flounder, (paralichthys olivaceus) at two different temperatures. J Vet Med Sci. 1996. 58:1039–1040.
Article
17. Park SC, Yun HI. Clinical pharmacokinetics of norfloxacin-glycine acetate after intravenous and intramuscular administration to horses. Res Vet Sci. 2003. 74:79–83.
Article
18. Park SC, Yun HI, Oh TK. Comparative pharmacokinetic profiles of two norfloxacin formulations after oral administration in rabbits. J Vet Med Sci. 1998. 60:661–663.
Article
19. Prescott JF, Yielding KM. In vitro susceptibility of selected veterinary bacterial pathogens to ciprofloxacin, enrofloxacin and norfloxacin. Can J Vet Res. 1990. 54:195–197.
20. Schentag JJ. Antimicrobial action and pharmacokinetics/pharmacodynamics: the use of AUIC to improve efficacy and avoid resistance. J Chemother. 1999. 11:426–439.
Article
21. Shem-Tov M, Ziv G, Gips M. Tissue distribution and binding to plasma proteins of norfloxacin nicotinate after intramuscular administration in pigs. Zentralbl Veterinarmed B. 1994. 41:257–263.
Article
22. Toutain PL, Del Castillo JRE, Bousquet-Melou A. The pharmacokinetic-pharmacodynamic approach to a rational dosage regimen for antibiotics. Res Vet Sci. 2002. 73:105–114.
Article
23. Wallis SC, Charles BG, Gahan LR, Filippich LJ, Bredhauer MG, Duckworth PA. Interaction of norfloxacin with divalent and trivalent pharmaceutical cations. In vitro complexation and in vivo pharmacokinetic studies in the dog. J Pharm Sci. 1996. 85:803–809.
Article
24. Wentland M. Siporin C, Heifetz CL, Domagala JM, editors. Structure-activity relationships of fluoroquinolones. The New Generation of Quinolones. 1990. New York: Marcel Dekker;1–43.
Full Text Links
  • JVS
Actions
Cited
CITED
export Copy
Close
Share
  • Twitter
  • Facebook
Similar articles
Copyright © 2024 by Korean Association of Medical Journal Editors. All rights reserved.     E-mail: koreamed@kamje.or.kr