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Drug delivery to the proximal colon
The Journal of Pharmacy and Pharmacology
|December 1, 1985
Summary
Drug delivery systems, including capsules and multiparticulate pellets, travel together through the upper gastrointestinal tract. Pellets disperse in the colon, showing slower transit and significant variability, impacting colon drug delivery.
Area of Science:
- Pharmacokinetics and Drug Delivery
- Gastrointestinal Physiology
Background:
- Understanding gastrointestinal transit is crucial for optimizing oral drug delivery systems.
- Capsules and multiparticulate systems represent common dosage forms with distinct release characteristics.
Purpose of the Study:
- To compare the gastrointestinal transit of a capsule and a multiparticulate pellet system.
- To evaluate the implications of transit patterns for colon-specific drug delivery.
Main Methods:
- Monitoring the transit of radiolabeled capsule and pellet preparations in six healthy volunteers.
- Utilizing scintigraphy to track the movement of both dosage forms through the gastrointestinal tract.
Main Results:
- Both capsule and pellet systems exhibited similar transit times through the stomach and small intestine, reaching the colon at approximately 4 hours post-dose.
- Pellet dispersion occurred within the colon, with slower transit rates compared to the capsule.
- Significant inter-subject variability was observed in large bowel transit times.
Conclusions:
- The dispersion of pellets in the colon suggests potential for localized drug release.
- Variability in colonic transit necessitates careful consideration for colon-targeted drug delivery strategies.
- These findings inform the design of oral drug delivery systems for colonic therapies.