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Absorption characteristics of selected slow-release formulations of theophylline

Absorption characteristics of selected slow-release formulations of theophylline
Formulation Time to peak serum concentration* Comments
Extended-release 12-hour tablet[1,2] 3 to 7 hours after morning dose when given every 12 hours
  • Preferred formulation given most consistent absorption
  • Complete absorption occurs in the presence or absence of food
  • Scored tablets can be split without affecting absorption characteristics
Extended-release 24-hour tablet[3,4] 8 to 12 hours when given every 24 hours
  • Twice daily administration may be used to minimize fluctuations in serum concentration
  • More complete absorption occurs when taken with food or within 1 to 2 hours of mealtime
  • Scored tablets can be split without affecting absorption characteristics

Extended-release 24-hour capsule[5,6]

(United States brand name: Theo-24)
Variable and difficult to predict; it depends on both administration time and fasting status
  • Other slow-release formulations are preferred due to erratic absorption
  • Incomplete absorption occurs when taken after an overnight fast; pH-dependent dissolution causes much more rapid and complete absorption when taken after food or in the evening (ie, dose-dumping)
Absorption characteristics (ie, rate and extent) are product-specific; refer to locally approved prescribing information for dosing and monitoring recommendations. These formulations may also be called sustained-release in some countries.
* The times to peak serum concentration selected for this table represent the time a peak is generally observed at the dosing interval most commonly used for the product and at steady-state (ie, after approximately three days of consistent administration).
References:
  1. Theophylline extended-release tablets. US Food and Drug Administration (FDA) approved product information. Revised October 2021. US National Library of Medicine. (Available online at https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=77e849b8-900b-4f0d-ac5c-1391abcd5721 (Accessed February 7, 2023)).
  2. Theophylline anhydrous sustained-release tablets. Health Canada approved product monograph. Revised January 13, 2022. Health Canada. (Available online at https://pdf.hres.ca/dpd_pm/00064324.PDF (Accessed February 7, 2023)).
  3. Theophylline (anhydrous) extended-release tablets. US Food & Drug Administration (FDA) approved product information. Revised November 2021. US National Library of Medicine. (Available online at https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=038c2b07-8028-4dc4-847c-adafe1b0e81a (Accessed February 7, 2023)).
  4. Theophylline sustained-release tablets. Health Canada approved product monograph. Revised September, 28, 2021. Health Canada. (Available online at https://pdf.hres.ca/dpd_pm/00063080.PDF (Accessed February 7, 2023)).
  5. Weinberger, M, Hendeles, L. Theophylline in asthma. N Engl J Med 1996; 334:1380.
  6. Theo-24. US Food & Drug Administration (FDA) approved product information. Revised August 2017. US National Library of Medicine. (Available online at https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7a108fa0-c230-475f-be93-6f864b98a410 (Accessed February 7, 2023)).

Adapted from: Weinberger, M, Hendeles, L. Theophylline in asthma. N Engl J Med 1996; 334:1380.

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