✦ LIBER ✦

Oral and rectal nalbuphine bioavailability: First-pass metabolism in rats and dogs

✍ Scribed by Bruce J. Aungst; Gilbert Lam; Eli Shefter

Publisher: John Wiley and Sons
Year: 1985
Tongue: English
Weight: 370 KB
Volume: 6
Category: Article
ISSN: 0142-2782
DOI: 10.1002/bdd.2510060407

No coin nor oath required. For personal study only.

✦ Synopsis

The disposition of the narcotic antagonist/analgesic nalbuphine after i.v., oral, and rectal dosing was evaluated in rats and dogs. In both species nalbuphine had high systemic clearance and low oral bioavailability as a result of extensive first-pass metabolism. Administration to a closed 2 cm length of rectum in rats resulted in complete bioavailability ; first-pass metabolism was circumvented. However, the extent of first-pass metabolism increased when the dose was not restricted to the lower rectum. Rectal nalbuphine bioavailability in dogs from a solution or three suppository formulations was low and equivalent to oral bioavailability. This was probably because of upward spreading of the dose and subsequent first-pass metabolism. Sodium salicylate, which has been shown to improve rectal absorption of other drugs, did not affect nalbuphine bioavailability rectally.

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