Summary
The absorption of a theophylline solution containing 80–120 mg doses delivered to different sites in the gastro-intestinal tract has been determined in 3 male volunteers using a remote controlled drug release system (HF-capsule). There was no difference between the stomach, ileum and the colon in the amount of theophylline absorbed (AUC). The T1/2abs of theophylline absorbed via the colon was prolonged when compared with that entering via the upper gastro-intestinal tract. The results provide a rational basis for the further development of theophylline formulations and are indispensable for planned development and to account for variation in the bioavailability of retarded release drug preparations.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Hirtz J (1984) The absorption window: Fact or fiction? Pharmacy Internat 5 (7): pp 175–178
Schuster O, Hugemann B, Graul EH, Loew D (1984) Absorptionslokalisation von Furosemid durch Verwendung einer ferngesteuerten Arzneimittelkapsel unter Röntgen- und CT-Kontrolle. In: Graul EH, Loew D (eds) Pathophysiologie und Therapie des gestörten Natrium- und Wasserhaushaltes, (Workshop Diuretika '84, Bad Nauheim April 1984), Medicef 1984, pp 128–137
Caldwell J, Staib AH, Cotgreave IA, Siebert-Weigel M (1986) Intraindividual comparison of theophylline pharmacokinetics in human volunteers after intravenous infusion with ethylenediamine or sodium glycinate. Br J Clin Pharmacol 22: (in press)
Jusko WJ, Polisczcuk A (1976) High-pressure liquid chromatographic and spectrophotometric assays for theophylline in biological fluids. Am J Hosp Pharm 33: 1193–1196
Wagner JG (1975) Fundamentals of clinical pharmacokinetics. Drug Intelligence Publications, Hamilton, Illinois
Betzien G, Kaufmann B, Schneider B, Ritschel WA (1985) KINPAK — a new program package for standardized evaluation of kinetic parameters. Arzneimittelforsch 35 [I] 1: 14–20
Hendeles L, Weinberger M, Johnson G (1980) Theophylline. In: Evans WE, Schentag JJ, Jusko WI (eds) Applied pharmacokinetics. Principles of therapeutic drug monitoring. Applied therapeutics, Inc. San Francisco 1980, chapter 6: pp 95–138
Frömming KH, Schwabe L, Staib AH, Rietbrock N, Lassmann A, Molz KH, Schuppan D, Siebert-Weigel M, Voegele D (1983) Untersuchungen zur Liberation, Absorption und Elimination von Theophyllin bei rasch und verzögert freisetzenden oralen Arzneiformen. Arzneimittelforsch 33 [I] 3: 446–452
Schuppan D, Molz KH, Staib AH, Rietbrock N (1981) Bioavailability of theophylline from a sustained-release aminophylline formulation (Euphyllin retard tablets)-plasma levels after single and multiple oral doses. Int J Clin Pharmacol Ther Tox 19 [5]: 223–227
Bolme P, Edlund PO, Eriksson M, Paalzow L, Winbladh B (1979) Pharmacokinetics of theophylline in young children with asthma: Comparison of rectal enema and suppositories. Eur J Clin Pharmacol 16: 133–139
De Leede LGJ, De Boer AG, Van Vuelzen SL, Breimer DD (1982) Zero-order rectal delivery of theophylline in man with an osmotic system. J Pharmacokinet Biopharm 10 [5]: 525–537
Graul EH, Loew D, Schuster O (1985) Voraussetzung für die Entwicklung einer sinnvollen Retard- und Diuretikakombination — Untersuchungen von Furosemid in verschiedenen Darmabschnitten. Therapiewoche 35: 4277–4291
Schuster O, Haertel M, Hugemann B, Gikalov I, Schiemann O, Fenner H (1985) Untersuchungen zur klinischen Pharmakokinetik von Allopurinol, I. Mitt.: Allopurinol — Absorptionsorte und Dosisproportionalität der Allopurinol/Oxipurinol-Bioverfügbarkeit. Arzneimittelforsch 35 [I] 4: 760–765
Staib AH, Loew D, Harder S, Graul EH, Pfab R, Hugemann B (1985) Theophylline absorption at different gastrointestinal sites in the man: Studies employing a remote control liberation system (HF-capsule). Arch Pharmacol 330 [suppl] R 15 (abstr 66)
Hugemann B, Schuster O (1982) Vorrichtung zur Freisetzung von Substanzen an definierten Orten des Verdauungstraktes. Patentschrift DE 2928477 C3 (A 61 K 9/00)
Riegelman S, Collier P (1980) The application of statistical moment theory to the evaluation of in vivo dissolution time and absorption time. J Pharmacokinet Biopharm 8 [5]: 509–534
Author information
Authors and Affiliations
Additional information
in technical collaboration with B. Hugemann, Frankfurt/Main
Rights and permissions
About this article
Cite this article
Staib, A.H., Loew, D., Harder, S. et al. Measurement of theophylline absorption from different regions of the gastro-intestinal tract using a remote controlled durg delivery device. Eur J Clin Pharmacol 30, 691–697 (1986). https://doi.org/10.1007/BF00608217
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00608217