Skip to main content
NCBI home page
Antimicrobial Agents and Chemotherapy logoLink to Antimicrobial Agents and Chemotherapy
. 1980 Feb;17(2):199–202. doi: 10.1128/aac.17.2.199

Absorption and disposition kinetics of amoxicillin in normal human subjects.

A Arancibia, J Guttmann, G González, C González
PMCID: PMC283758  PMID: 7387142

Abstract

Pharmacokinetic parameters of amoxicillin were studied in healthy fasted subjects afqer both oral and intravenous administration of a single 500-mg dose. Serum levels and urinary excretion rates were determined at various time intervals by a microbiological method. The conventional two-compartment model with elimination occurring from the central compartment was used to analyze the data. Mean values were 3.40 h-1 for alpha and 0.68 h-1 for beta. Distribution constants kappa 12 and kappa 21 were 0.92 h-1 and 1.99 h-1, respectively. The rate constant for elimination from the central compartment, kappa 10, was 1.16 h-1. The volume of distribution was 20.2 liters (0.30 liter/kg), and the serum clearance was 13.3 liters/h. The absorption rate constant, kappa a, in the oral study, calculated by the Loo-Riegelman method, was 1.02 h-1, and the absorption half-life was 0.72 h. Absolute bioavailability after the oral dose was determined by comparing both the areas under the curve (AUC) and fractions of the antibiotic excreted unchanged in the urine. The AUC after oral administration was 77.4% of the intravenous AUC. On the other hand, recovery from the urine was 43.4% after the oral dose and 57.4% after the intravenous dose, indicating 76.5% bioavailability.

Full text

PDF
199

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Barza M., Melethil S., Berger S., Ernst E. C. Comparative pharmacokinetics of cefamandole, cephapirin, and cephalothin in healthy subjects and effect of repeated dosing. Antimicrob Agents Chemother. 1976 Sep;10(3):421–425. doi: 10.1128/aac.10.3.421. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Bennett J. V., Brodie J. L., Benner E. J., Kirby W. M. Simplified, accurate method for antibiotic assay of clinical specimens. Appl Microbiol. 1966 Mar;14(2):170–177. doi: 10.1128/am.14.2.170-177.1966. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Bodey G. P., Nance J. Amoxicillin: in vitro and pharmacological studies. Antimicrob Agents Chemother. 1972 Apr;1(4):358–362. doi: 10.1128/aac.1.4.358. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Brogeden R. N., Speight T. M., Avery G. S. Amoxycillin: A review of its antibacterial and pharmacokinietic properties and therapeutic use. Drugs. 1975;9(2):88–140. doi: 10.2165/00003495-197509020-00002. [DOI] [PubMed] [Google Scholar]
  5. Brusch J. L., Bergeron M. G., Barza M., Weinstein L. An in vitro and pharmacological comparison of amoxicillin and ampicillin. Am J Med Sci. 1974 Jan;267(1):41–48. doi: 10.1097/00000441-197401000-00006. [DOI] [PubMed] [Google Scholar]
  6. Croydon E. A., Sutherland R. -amino-p-hydroxybenzylpenicillin (BRL 2333), a new semisynthetic penicillin: absorption and excretion in man. Antimicrob Agents Chemother (Bethesda) 1970;10:427–430. [PubMed] [Google Scholar]
  7. Gómez-Lus R., Rubio Calvo M. C., Gómez López L., Millán M. P. Diez casos de infecciones urinarias tratadas con alpha-aminohidroxibencilpenicilina. Chemotherapy. 1973;18(Suppl):47–51. [PubMed] [Google Scholar]
  8. Harding J. W., Lees L. J. Trial of a new broad-spectrum penicillin (amoxycillin) in general practice. Practitioner. 1972 Sep;209(251):363–368. [PubMed] [Google Scholar]
  9. Kerrebijn K. F., Michel M. F. Amoxycillin (BRL 2333) in children. Serum concentrations and clinical report. Chemotherapy. 1973;18(Suppl):92–96. [PubMed] [Google Scholar]
  10. Kirby W. M., Gordon R. C., Reagamey C. The pharmacology of orally administered amoxicillin and ampicillin. J Infect Dis. 1974 Jun;129(0):suppl–suppl:S155. doi: 10.1093/infdis/129.supplement_2.s154. [DOI] [PubMed] [Google Scholar]
  11. Loo J. C., Riegelman S. New method for calculating the intrinsic absorption rate of drugs. J Pharm Sci. 1968 Jun;57(6):918–928. doi: 10.1002/jps.2600570602. [DOI] [PubMed] [Google Scholar]
  12. MacLeod C., Rabin H., Ogilvie R., Ruedy J., Caron M., Zarowny D., Davies R. O. Practical concepts of drug absorption, distribution and loss. Can Med Assoc J. 1974 Aug 17;111(4):341–346. [PMC free article] [PubMed] [Google Scholar]
  13. Spyker D. A., Rugloski R. J., Vann R. L., O'Brien W. M. Pharmacokinetics of amoxicillin: dose dependence after intravenous, oral, and intramuscular administration. Antimicrob Agents Chemother. 1977 Jan;11(1):132–141. doi: 10.1128/aac.11.1.132. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Stam J. Preliminary clinical study with amoxycillin (BRL 2333) in complicated lower respiratory tract infections. Chemotherapy. 1973;18(Suppl):27–33. doi: 10.1159/000221291. [DOI] [PubMed] [Google Scholar]
  15. Till A. E., Benet L. Z., Kwan K. C. An integrated approach to the pharmacokinetic analysis of drug absorption. J Pharmacokinet Biopharm. 1974 Dec;2(6):525–544. doi: 10.1007/BF01070946. [DOI] [PubMed] [Google Scholar]
  16. Vallejos C., Rodriguez V., Gottlieb J. A., Bodey G. P. Amoxicillin therapy of infections. Clin Pharmacol Ther. 1973 Nov-Dec;14(6):962–965. doi: 10.1002/cpt1973146962. [DOI] [PubMed] [Google Scholar]
  17. Welling P. G., Huang H., Koch P. A., Craig W. A., Madsen P. O. Bioavailability of ampicillin and amoxicillin in fasted and nonfasted subjects. J Pharm Sci. 1977 Apr;66(4):549–552. doi: 10.1002/jps.2600660423. [DOI] [PubMed] [Google Scholar]
  18. Zarowny D., Ogilvie R., Tamblyn D., MacLeod C., Ruedy J. Pharmacokinetics of amoxicillin. Clin Pharmacol Ther. 1974 Dec;16(6):1045–1051. doi: 10.1002/cpt19741661045. [DOI] [PubMed] [Google Scholar]

Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES