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Nalbuphine prodrugs

Han, R.-Y. Fang, J.-Y. Sung, K.C. Hu, O.Y.P. Mucoadhesive buccal disks for novel nalbuphine prodrug controlled delivery Effect of formulation variables on drug release and mucoadhesive performance. Int. J. Pharm. 1999, 177 (2), 201-209. [Pg.570]

Figure 1.18. (a) In vitro release of / -nitroaniline (circles) from a poly(carbophenoxyvaleric acid) matrix, as well as the fractional degradation of the matrix (triangles) (data from ref 237). (b) Relationship between the release rate and the aqueous solubility of various nalbuphine prodrugs (data from ref (238))... [Pg.27]

The narcotic agonist/antagonist nalbuphine (8.88) is poorly bioavailable in humans (ca. 10%), mostly due to extensive first-pass metabolism. Two prodrugs were examined, namely the acetylsalicylate (8.89) and the anthran-ilate (8.90) [125]. The hydrolysis of these compounds in rat plasma was fast (tU2 values of some minutes and 1 - 2 h, respectively), while it was slow in dog plasma (lW2 ca. 3 h and 15 h, respectively) and in human plasma (t1/2 ca. 7-10 h and 50-60 h, respectively). Hydrolysis in dog tissue homogenates was also markedly slower than in rat. The dog was, thus, considered to be a fair animal model, and it is of interest that, in this species, the oral bioavailability of 8.88, 8.89, and 8.90 were ca. 6, 20, and 50%, respectively. [Pg.483]

B. J. Aungst, M. J. Myers, E. Shefter, E. G. Shami, Prodrugs for Improved Oral Nalbuphine Bioavailabihty Inter-Species Differences in the Disposition of Nalbuphine and Its Acetylsalicylate and Anthranilate Esters , Int. J. Pharm. 1987, 38, 199 - 209. [Pg.543]

Buccal delivery of opioid analgesics and antagonists can improve bioavailability relative to the oral route. Esterification of the 3-pheno-lic hydroxyl group in opioid analgesics such as nalbuphine, naloxone, naltrexone, oxymorphone, butorphanol, and levallorphan improved bioavailability and eliminated the bitter taste. The prodrug of morphine,... [Pg.94]

For drugs that have poor oral bioavailability, rectal administration of prodrugs can increase their absorption. For example, nalbuphine is an analgesic with potency approximately 0.5-0.9 that of morphine. It is used for the relief of moderate to severe pain from a variety of causes, e.g., surgery, trauma, cancer, kidney, or biliary colic pain. Oral bioavailability of nalbuphine was poor, e.g., around 6% in experimental dogs. Rectal administration of nalbuphine-3-acetylsalicylate in the same animals enhanced the bioavailability 4- to 5-fold to around 28%. In addition, the plasma half-life of nalbuphine after rectal administration of the prodrug was prolonged. [Pg.310]


See other pages where Nalbuphine prodrugs is mentioned: [Pg.502]    [Pg.27]    [Pg.37]    [Pg.502]    [Pg.27]    [Pg.37]    [Pg.230]    [Pg.234]    [Pg.267]    [Pg.267]   
See also in sourсe #XX -- [ Pg.2 , Pg.502 ]

See also in sourсe #XX -- [ Pg.502 ]




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