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. 1985 Dec;20(6):589–596. doi: 10.1111/j.1365-2125.1985.tb05116.x

The rise and fall of serum theophylline concentration: a comparison of sustained-release formulations in volunteers with rapid theophylline clearance.

J C Mucklow, S Kuhn
PMCID: PMC1400821  PMID: 4091990

Abstract

The pharmacokinetics of four sustained-release formulations of theophylline have been examined after single doses (Nuelin SA, Phyllocontin, Slo-phyllin and Theo-Dur) and at steady-state (Phyllocontin, Theo-Dur) in six healthy adult volunteers, selected because they all eliminated theophylline rapidly after an intravenous dose of aminophylline. After a single dose of Theo-Dur, the peak concentration of theophylline was smaller and occurred later than after single doses of Nuelin SA, Phyllocontin and Slo-phyllin, suggesting that absorption occurs over a longer period. The systemic availability of theophylline was virtually complete after all four formulations. After repeated 12-hourly dosing to steady-state, and adjustment of dose to achieve trough concentrations of between 5 and 10 mg l-1 (28-55 mumol l-1), theophylline concentration fluctuated to a significantly greater extent within a dose interval when the subjects were taking Phyllocontin than when they were taking Theo-Dur.

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Selected References

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

  1. Dederich R. A., Szefler S. J., Green E. R. Intrasubject variation in sustained-release theophylline absorption. J Allergy Clin Immunol. 1981 Jun;67(6):465–471. doi: 10.1016/0091-6749(81)90100-7. [DOI] [PubMed] [Google Scholar]
  2. Domson J. F., Hein E. W., Sheen A., Sly R. M. Comparison of Theolair SR and Theo-Dur tablets. Ann Allergy. 1979 Oct;43(4):220–222. [PubMed] [Google Scholar]
  3. Ellis E. F., Koysooko R., Levy G. Pharmacokinetics of theophylline in children with asthma. Pediatrics. 1976 Oct;58(4):542–547. [PubMed] [Google Scholar]
  4. Hendeles L., Weinberger M. Theophylline. A "state of the art" review. Pharmacotherapy. 1983 Jan-Feb;3(1):2–44. doi: 10.1002/j.1875-9114.1983.tb04531.x. [DOI] [PubMed] [Google Scholar]
  5. Jenne J. W., Wyze M. S., Rood F. S., MacDonald F. M. Pharmacokinetics of theophylline. Application to adjustment of the clinical dose of aminophylline. Clin Pharmacol Ther. 1972 May-Jun;13(3):349–360. doi: 10.1002/cpt1972133349. [DOI] [PubMed] [Google Scholar]
  6. Jonkman J. H., van der Boon W. J. Nocturnal theophylline plasma concentrations. Lancet. 1983 Jun 4;1(8336):1278–1279. doi: 10.1016/s0140-6736(83)92728-9. [DOI] [PubMed] [Google Scholar]
  7. Kelly H. W., Murphy S. Efficacy of a 12-hour sustained-release preparation in maintaining therapeutic serum theophylline levels in asthmatic children. Pediatrics. 1980 Jul;66(1):97–102. [PubMed] [Google Scholar]
  8. Mitenko P. A., Ogilvie R. I. Pharmacokinetics of intravenous theophylline. Clin Pharmacol Ther. 1973 Jul-Aug;14(4):509–513. doi: 10.1002/cpt1973144part1509. [DOI] [PubMed] [Google Scholar]
  9. Mitenko P. A., Ogilvie R. I. Rational intravenous doses of theophylline. N Engl J Med. 1973 Sep 20;289(12):600–603. doi: 10.1056/NEJM197309202891202. [DOI] [PubMed] [Google Scholar]
  10. Pedersen S. Delay in the absorption rate of theophylline from a sustained release theophylline preparation caused by food. Br J Clin Pharmacol. 1981 Dec;12(6):904–905. doi: 10.1111/j.1365-2125.1981.tb01329.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Scott P. H., Tabachnik E., MacLeod S., Correia J., Newth C., Levison H. Sustained-release theophylline for childhood asthma: evidence for circadian variation of theophylline pharmacokinetics. J Pediatr. 1981 Sep;99(3):476–479. doi: 10.1016/s0022-3476(81)80354-x. [DOI] [PubMed] [Google Scholar]
  12. Simons F. E., Luciuk G. H., Simons K. J. Sustained-release theophylline for treatment of asthma in preschool children. Am J Dis Child. 1982 Sep;136(9):790–793. doi: 10.1001/archpedi.1982.03970450032008. [DOI] [PubMed] [Google Scholar]
  13. Taylor D. R., Duffin D., Kinney C. D., McDevitt D. G. Circadian variation in plasma theophylline concentrations during maintenance therapy with a sustained-release preparation in patients with obstructive airways disease. Br J Clin Pharmacol. 1984 Jul;18(1):27–30. doi: 10.1111/j.1365-2125.1984.tb05017.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Taylor D. R., Duffin D., Kinney C. D., McDevitt D. G. Investigation of diurnal changes in the disposition of theophylline. Br J Clin Pharmacol. 1983 Oct;16(4):413–416. doi: 10.1111/j.1365-2125.1983.tb02186.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Warren J. Theophylline concentrations and posture. Lancet. 1983 Oct 8;2(8354):850–850. doi: 10.1016/s0140-6736(83)90764-x. [DOI] [PubMed] [Google Scholar]
  16. Weinberger M., Hendeles L., Bighley L. The relation of product formulation to absorption of oral theophylline. N Engl J Med. 1978 Oct 19;299(16):852–857. doi: 10.1056/NEJM197810192991603. [DOI] [PubMed] [Google Scholar]
  17. Weinberger M., Hendeles L. Current concepts. Slow-release theophylline rationale and basis for product selection. N Engl J Med. 1983 Mar 31;308(13):760–764. doi: 10.1056/NEJM198303313081306. [DOI] [PubMed] [Google Scholar]
  18. Weinberger M., Hendeles L., Wong L. Relationship of formulation and dosing interval to fluctuation of serum theophylline concentration in children with chronic asthma. J Pediatr. 1981 Jul;99(1):145–152. doi: 10.1016/s0022-3476(81)80982-1. [DOI] [PubMed] [Google Scholar]

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