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Experiences with the rectal use of trimethoprim
J Sallai1, A Vernyik, G Regdon
1Department of Pharmacodynamics, Albert Szent-Györgyi Medical University, Hungary.
The Journal of Pharmacy and Pharmacology
|May 1, 1997
Summary
Rectal trimethoprim absorption was evaluated using various suppository bases. Optimal formulations demonstrated high bioavailability, exceeding oral administration in some cases, suggesting suitability for clinical trials.
Area of Science:
- Pharmacology
- Drug Delivery Systems
Background:
- Rectal administration offers an alternative route for drug delivery.
- Trimethoprim is an antibiotic commonly administered orally.
Purpose of the Study:
- To investigate the feasibility and efficacy of rectal trimethoprim delivery.
- To identify optimal suppository bases for trimethoprim rectal absorption.
Main Methods:
- In vitro drug liberation studies using 24 different suppository bases.
- In vivo pharmacokinetic studies in anesthetized rats.
- Spectrophotometric and bioassay methods for drug quantification.
- Comparison of rectal versus oral administration bioavailability.
Main Results:
- Lipohydrophilic Witepsol W 35 with polysorbates yielded the highest bioavailability (63.8%).
- Hydrophilic Macrogol 1540 also showed good absorption (52.9%).
- Rectal absorption exceeded oral administration (38.8%) with certain formulations.
Conclusions:
- Trimethoprim is well-absorbed rectally when formulated appropriately.
- Selected rectal formulations show promising bioavailability for clinical investigation.
- Rectal trimethoprim suppositories are suitable for further pharmacological studies.