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New method for bioavailability assessment of slow-release preparations of theophylline

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Abstract

Variability in an individual's clearance of theophylline is an important consideration when estimating bioavailability. A method is described for compensating for this problem, using the serum concentration of theophylline and urinary excretion data on its major metabolites to make an estimation of the clearance after oral administration using the intravenous dose as reference. The method is particularly useful for assessing the bioavailability of slow-release theophylline preparations.

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References

  1. J. W. Jenne, M. S. Wyze, B. S. Rood, and F. M. MacDonald. Pharmacokinetics of theophylline: Application to adjustment of the clinical dose of aminophylline.Clin. Pharmacol. Ther. 13:349–360 (1972).

    CAS  PubMed  Google Scholar 

  2. E. Ginchansky and M. Weinberger. Relationship of theophylline clearance to oral dosage in children with chronic asthma.J. Pediatr. 91:655–660 (1977).

    Article  CAS  PubMed  Google Scholar 

  3. P. D. Walson, R. C. Strunk, and L. M. Taussig. Intrapatient variability in theophylline kinetics.J. Pediatr. 91:321–324 (1977).

    Article  CAS  PubMed  Google Scholar 

  4. L. Patric, A. Kalisker, and T. D. Bell. Variation in theophylline clearance rate with time in chronic childhood asthma.J. Allergy Clin. Immunol. 59:440–444 (1977).

    Article  Google Scholar 

  5. J. D. Arnold, G. N. Hill, and L. N. Sansom. A comparison of theophylline in asthmatic children in the acute episode and in remission.Eur. J. Clin. Pharmacol. 20: 443–447 (1981).

    Article  CAS  PubMed  Google Scholar 

  6. R. A. Upton, J. F. Thiercelin, T. W. Guentert, S. M. Wallace, J. R. Powell, L. Sansom, and S. Riegelman. Intraindividual variability in theophylline pharmacokinetics: Statistical verification in 39 of 60 healthy young adults.J. Pharmacokin. Biopharm. 10:123–134 (1982).

    Article  CAS  Google Scholar 

  7. P. A. Mitenko and R. I. Ogilvie. Bioavailability and efficacy of a sustained-release theophyl-line tablet.Clin. Pharmacol. Ther. 16:720–726 (1974).

    CAS  PubMed  Google Scholar 

  8. D. L. Spangler, D. D. Kalof, F. L. Bloom, and H. J. Wittig. Theophylline bioavailability following oral administration of six sustained-release preparations.Ann. Allergy 40:6–11 (1978).

    CAS  PubMed  Google Scholar 

  9. M. Weinberger, L. Hendeles, and L. Bighley. The relation of product formulation to absorption of oral theophylline.N. Engl. J. Med. 299:852–857 (1978).

    Article  CAS  PubMed  Google Scholar 

  10. J. H. G. Jonkman, D. D. S. Tang, R. A. Upton, and S. Riegelman. Measurement of excretion characteristics of theophylline and its major metabolites.Eur. J. Clin. Pharmacol. 20:435–441 (1981).

    Article  CAS  PubMed  Google Scholar 

  11. T. J. Haley. Metabolism and pharmacokinetics of theophylline in human neonates, children, and adults.Drug Metab. Rev. 14:295–335 (1983).

    Article  CAS  PubMed  Google Scholar 

  12. T. J. Monks, C. H. Caldwell, and R. L. Smith. Influence of methylxanthine-containing foods on theophylline metabolism and kinetics.Clin. Pharmacol. Ther. 26:514–524 (1979).

    Google Scholar 

  13. K. T. Muir, J. H. G. Jonkman, D. Tang, M. Kunitani, and S. Riegeiman. Simultaneous determination of theophylline and its major metabolites in urine by reversed-phase ion pair high-performance liquid chromatography.J. Chromatogr. 221:85–95 (1980).

    Article  CAS  PubMed  Google Scholar 

  14. D. D. Tang-Liu, R. L. Williams, and S. Riegeiman. Non-linear theophylline elimination.Clin. Pharmacol. Ther. 31:358–369 (1982).

    Article  CAS  PubMed  Google Scholar 

  15. L. Hendeles, M. Weinberger, and L. Bighley. Absolute bioavailability of oral theophylline.Am. J. Hosp. Pharm. 34:525–527 (1977).

    CAS  PubMed  Google Scholar 

  16. J. H. G. Jonkman, W. C. Berg, R. Schoenmaker, R. A. deZeeuw, J. E. Greving, and N. G. M. Orie. Disposition and clinical pharmacokinetics of microcrystalline theophylline.Eur. J. Clin. Pharmacol. 17:379–384 (1980).

    Article  CAS  PubMed  Google Scholar 

  17. R. A. Upton, L. Sansom, T. W. Guentert, J. R. Powell, J. F. Thiercelin, V. P. Shah, P. E. Coates, and S. Riegeiman. Evaluation of the absorption from 15 commercial theophylline products indicating deficiencies in currently applied bioavailability criteria.J. Pharmacokin. Biopharm. 8:229–242 (1980).

    Article  CAS  Google Scholar 

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Author notes

  1. Tetsuro Ohno

    Present address: Department of Pharmacy, St. Marianna University Hospital, 2095 Sugoh, Miyamae-ku, Kawasaki, 213, Kanagawa, Japan

Authors and Affiliations

  1. Department of Clinical Pharmacy, Tokyo College of Pharmacy, 1432-1 Horinouchi, Hachioji, 192-03, Tokyo, Japan

    Yasuji Kasuya, Tetsuro Ohno, Noriyoshi Kubota, Hidenori Takahashi & Hiroki Hirayama

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  1. Yasuji Kasuya
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  2. Tetsuro Ohno
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  3. Noriyoshi Kubota
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  4. Hidenori Takahashi
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  5. Hiroki Hirayama
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Kasuya, Y., Ohno, T., Kubota, N. et al. New method for bioavailability assessment of slow-release preparations of theophylline. Journal of Pharmacokinetics and Biopharmaceutics 13, 571–587 (1985). https://doi.org/10.1007/BF01058902

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  • DOI: https://doi.org/10.1007/BF01058902

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