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The bioavailability of carbamazepine
Proceedings of the Australian Association of Neurologists
|January 1, 1975
Summary
Carbamazepine absorption from tablets is slow and incomplete. A specially prepared solution improved carbamazepine absorption, suggesting tablet formulation limits bioavailability.
Area of Science:
- Pharmacology
- Drug Absorption
- Bioavailability Studies
Background:
- Plasma carbamazepine levels correlated variably with dosage in patients.
- This suggested incomplete and inconsistent absorption from the gastrointestinal tract.
Purpose of the Study:
- To investigate the absorption of carbamazepine from oral tablets.
- To compare the bioavailability of carbamazepine from tablets versus a solution formulation.
Main Methods:
- Pharmacokinetic studies in six healthy volunteers.
- Administration of increasing single oral doses of carbamazepine tablets.
- Administration of carbamazepine in a specially prepared solution to five subjects.
Main Results:
- Tablet formulation resulted in slow and incomplete carbamazepine absorption.
- Carbamazepine solution led to rapid absorption.
- Four subjects absorbed more drug from the solution than from tablets.
Conclusions:
- The pharmaceutical formulation of carbamazepine tablets significantly limits drug bioavailability.
- Increased bioavailability may present challenges if not carefully managed.