Pharmacokinetics and delivery of the anti-influenza prodrug oseltamivir to the small intestine and colon using site-specific delivery capsules

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...

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Bibliographic Details
Published in:International journal of pharmaceutics 2003-05, Vol.257 (1), p.297-299
Main Authors: Oo, Charles, Snell, Paul, Barrett, Joanne, Dorr, Albert, Liu, Baolian, Wilding, Ian
Format: Article
Language:English
Subjects:
Absorption
Acetamides - pharmacokinetics
Adult
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - pharmacokinetics
Biological and medical sciences
Capsules
Colon - metabolism
Controlled delivery
Cross-Over Studies
Drug Delivery Systems
Gamma scintigraphy
General pharmacology
Humans
Influenza, Human - drug therapy
Intestine, Small - metabolism
Male
Medical sciences
Middle Aged
Oseltamivir
Pharmaceutical technology. Pharmaceutical industry
Pharmacokinetics
Pharmacology. Drug treatments
Prodrug
Prodrugs - pharmacokinetics
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Summary: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.
ISSN:0378-5173
1873-3476
DOI:10.1016/S0378-5173(03)00164-9