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Pharmacokinetics of a new oral formulation of amoxicillin

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Summary

The bioavailability of the recently developed 1 g dispersible tablet form of amoxicillin (B) and the 1 g dispersible tablet in suspension form (C) were compared to that of the 1 g standard reference formulation (A). Twelve healthy volunteers were involved in this single-dose, open, randomized, three-way cross-over study. The mean peak serum levels were 14.1±4.1 μg/ml after A, 15.1 ±3.1 μg/ml after B and 15.1±5.4 μg/ml after C. The area under the drug concentration versus time curves were 47.6±12.0 μg.h/ml after A, 52.8±10.2 μg.h/ml after B and 51.1±13.8 μg.h/ml after C. On the basis of these two pharmacokinetic parameters, the three formulations were found to be bioequivalent. In addition, the predicted serum concentrations during multiple dosing (3 times a day), derived from the corresponding mean concentrations after a single 1 g dose of C showed that 8 hourly administration would yield therapeutic serum concentrations for infections such as uncomplicated community-acquired pneumonia due to susceptible or less susceptible strains in otherwise healthy subjects.

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References

  1. Macfarlane J.T. (1987): Treatment of lower respiratory infections. Lancet, II, 1446–1449.

    Article  Google Scholar 

  2. Appelbaum P.C. (1992): Antimicrobial resistance inStreptococcus pneumoniae: an overview. Clin. Infect. Dis., 15, 77–83.

    PubMed  CAS  Google Scholar 

  3. Doern G.V. (1994): Emergence of antimicrobial resistance withStreptococcus pneumoniae, Haemophilus influenzae andNeisseria species. 34th Interscience Conference on Antimicrobial Agent and Chemotherapy. Orlando. S91(C), 288.

  4. Klugman K.P. (1994): Management of antibiotic-resistant pneumococcal infections. J. Antimicrob. Chemother., 33, 191–193.

    Article  Google Scholar 

  5. Gibaldi M., Perrier D. (Eds) (1982): Pharmacokinetics. New York: Marcel Dekker, 451–457.

    Google Scholar 

  6. Westlake W.J. (1976): Symmetrical confidence intervals for bioequivalence trials. Biometrics, 32, 741–744.

    Article  PubMed  CAS  Google Scholar 

  7. Schuirmann D.J. (1987): A comparison of the two one-sided tests procedure and the power approach for assessing the equivalence of average bioavailability. J. Pharm. Biopharm., 15, 657–680.

    Article  CAS  Google Scholar 

  8. Steinijans V.W., Hauschke D., Jonkman J.H.G. (1992): Controversies in bioequivalence studies. Clin. Pharmacokinet., 22, 247–253.

    Article  PubMed  CAS  Google Scholar 

  9. Spyker D.A., Rugloski R.J., Vann R.L., O’Brien W.M. (1977): Pharmacokinetics of amoxicillin: dose dependence after intravenous, oral, and intramuscular administration. Antimicrob. Agents Chemother., 11, 132–141.

    PubMed  CAS  Google Scholar 

  10. Bodey G.P., Nance J. (1972): Amoxicillin: in vitro and pharmacological studies. Antimicrob. Agents Chemother., 1, 358–362.

    PubMed  CAS  Google Scholar 

  11. Duval J., Soussy C.J. (1973): Activité antibactérienne et pharmacocinétique de l’amoxicilline. Comparaison avec l’ampicilline. Med. Malad. Infect., 12, 525–531.

    Article  Google Scholar 

  12. Croydon E.A.P., Sutherland R. (1970): α-Amino-p-hydroxybenzylpenicillin (BRL 2333), a new semisynthetic penicillin: absorption and excretion in man. Antimicrob. Agents Chemother., 4, 427–430.

    Google Scholar 

  13. Sutherland R., Croydon E.A.P., Rolinson G.N. (1972): Amoxicillin: a new semisynthetic penicillin. BMJ, 3, 13–16.

    Article  PubMed  CAS  Google Scholar 

  14. Hespe W., Verschoor J.S.C., Olthoff M. (1987): Bioavailability of new formulations of amoxicillin in relation to its absorption kinetics. Arzneimittelforschung., 37, 372–375.

    PubMed  CAS  Google Scholar 

  15. Comité de l’antibiogramme de la société française de microbiologie (1994), Path. Biol., 42, 8, I–VIII.

    Google Scholar 

  16. Welling P.B., Huang H., Koch P.A., Craig W.A., Madsen P.O. (1977): Bioavailability of ampicillin and amoxicillin in fasted and non fasted subjects. J. Pharm. Sci., 66, 549–552.

    Article  PubMed  CAS  Google Scholar 

  17. Westphal J.F., Deslandes A., Brogard J.M., Carbon C. (1991): Reappraisal of amoxicillin absorption kinetics. J. Antimicrob. Chemother., 27, 647–654.

    Article  PubMed  CAS  Google Scholar 

  18. Sjövall J. (1979): Dose dependence in human absorption of aminopenicillins. Infection, 7, S458-S462.

    Article  PubMed  Google Scholar 

  19. Sjövall J., Alvan G., Westerlund D. (1985): Dose-dependant absorption of amoxicillin and bacampicillin. Clin. Pharmacol. Ther., 38, 241–250.

    PubMed  Google Scholar 

  20. Sjövall J., Alvan G., Akerlund J.E. et al. (1992): Dose-dependant absorption of amoxicillin in patients with an ileostomy. Eur. J. Clin. Pharmacol., 43, 277–281.

    Article  PubMed  Google Scholar 

  21. Paintaud G., Alvan G., Dahl M.L., Grahnen A., Sjövall J., Svensson J.O. (1992): Nonlinearity of amoxicillin absorption kinetics in human. Eur. J. Clin. Pharmacol., 43, 283–288.

    Article  PubMed  CAS  Google Scholar 

  22. Vogelman B., Craig W.A. (1986): Kinetics of antimicrobial activity. J. Pediatr., 108, 835–840.

    Article  PubMed  CAS  Google Scholar 

  23. Vogelman B., Gudmundsson S., Legett J., Turnidge J., Ebert S., Craig W.A. (1988): Correlation of antimicrobial pharmacokinetic parameters with therapeutic efficacy in an animal model. J. Infect. Dis., 158, 831–847.

    PubMed  CAS  Google Scholar 

  24. Legett J., Fantin B., Ebert S. et al. (1989): Comparative antibiotic dose-effect relations at several dosing intervals in murine pneumonitis and thigh-infection models. J. Infect. Dis., 159, 281–292.

    Google Scholar 

  25. Drusano G.L. (1988): Role of pharmacokinetics in the outcome of infections. Antimicrob. Agents Chemother., 32, 289–297.

    PubMed  CAS  Google Scholar 

  26. Bundtzen R.W., Gerber A.U., Cohn D.L., Craig W.A. (1981): Postantibiotic suppression of bacterial growth. Rev. Infect. Dis., 3, 28–37.

    PubMed  CAS  Google Scholar 

  27. Bennett S., Vogelman B., Craig W.A. (1985): Postantibiotic effects. J. Antimicrob. Chemother., 15, S37-S46.

    Google Scholar 

  28. Vogelman B., Gudmundsson S., Turnidge J., Legett J., Craig W.A. (1988): In vivo postantibiotic effect in a thigh infection in neutropenic mice. J. Infect. Dis., 157, 287–298.

    PubMed  CAS  Google Scholar 

  29. Leng B.M., Lacut J.Y., Aubertin J.M. (1976): Pharmacokinetics of amoxycillin according to administration schedule. J. Int. Med. Res., 4, 449–453.

    PubMed  CAS  Google Scholar 

  30. Neu H.C. (1981): Current practices in antimicrobial dosing. Rev. Infect. Dis., 3, 12–18.

    PubMed  CAS  Google Scholar 

  31. Kunin C.M. (1981): Dosage schedules of antimicrobial agents: a historical review. Rev. Infect. Dis., 3, 4–11.

    PubMed  CAS  Google Scholar 

  32. Bakker-Woundenberg I.A.J.M., Van der Berg J.C., Fontijne P., Michel M.F. (1984): Efficacy of continuous versus intermittent administration of penicillin G inStreptococcus pneumoniae pneumonia in normal and immunodeficient rats. Eur. J. Clin. Microbiol., 3, 131–135.

    Article  Google Scholar 

  33. Norbring F. (1981): Current practice in penicillin dosing. J. Antimicrob. Chemother., 8, S1-S6.

    Article  Google Scholar 

  34. Moreno F., Crisp C., Jorgensen J.H., Patterson J.E. (1994): The clinical and molecular epidemiology of bacteriamia due toStreptococcus pneumoniae isolates not susceptible to penicillin at a University Hospital. 34th Interscience Conference on Antimicrobial Agent and Chemotherapy. Orlando., S41, C10.

  35. Bedos J.P., Vallée E., Moine P., Chastang CI. (1994): A two years’ survey ofStreptococcus pneumoniae (Sp) isolates in Bichat-Claude Bernard Hospital, Paris, France: epidemiology data, risk factors of infection by penicillin nonsensitive strains. 34th Interscience Conference on Antimicrobial Agent and Chemotherapy. Orlando., S41, C12.

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Authors and Affiliations

  1. Département de pharmacologie clinique, hôpital Bichat Claude Bernard, Paris, France

    M-H. Prevot & B. Rouveix

  2. Laboratoire de Microbiologie, l’Université Louis Pasteur, Strasbourg, France

    F. Jehl

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  1. M-H. Prevot
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  2. F. Jehl
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  3. B. Rouveix
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Prevot, MH., Jehl, F. & Rouveix, B. Pharmacokinetics of a new oral formulation of amoxicillin. European Journal of Drug Metabolism and Pharmacokinetics 22, 47–52 (1997). https://doi.org/10.1007/BF03189784

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  • DOI: https://doi.org/10.1007/BF03189784

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