Pharmacokinetics and delivery of the anti-influenza prodrug oseltamivir to the small intestine and colon using site-specific delivery capsules.
Int J Pharm
; 257(1-2): 297-9, 2003 May 12.
Article
in En
| MEDLINE
| ID: mdl-12711184
ABSTRACT
This study investigated the site-specific absorption of oseltamivir using targeted delivery and gamma scintigraphy. On four separate occasions, nine healthy male subjects each received a single 150 mg of oseltamivir administered via the Enterion capsule to the stomach, proximal small bowel, distal small bowel and the ascending colon. Pharmacokinetic parameters of oseltamivir and its carboxylate metabolite show that absorption was similar in the proximal and distal small bowel compared to stomach delivery, but reduced from the ascending colon, demonstrating that absorption-rate limited disposition occurred only for the ascending colon. The metabolite-to-parent ratios were minimally reduced. The results support the feasibility of modified-release formulation development whilst confirming the high and consistent oral bioavailability of oseltamivir.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Prodrugs
/
Drug Delivery Systems
/
Colon
/
Influenza, Human
/
Intestine, Small
/
Acetamides
Type of study:
Clinical_trials
Limits:
Adult
/
Humans
/
Male
/
Middle aged
Language:
En
Journal:
Int J Pharm
Year:
2003
Document type:
Article
Affiliation country:
United States