Oh

Reduced metabolism, increased permeation through Caco-2

Kahns et al. (1993)

Tetragastrin

Peptidases

Acetyl, caproyl, lauroyl esters

Increased stability in excised intestinal and liver homogenates, reduced hepatic extraction in rats

Yodoya et al. (1994)

Leu-enkephalin, DADLE

Peptidases

Coumarinic acid-based cyclic prodrug

Increased stability to Caco-2 peptidases and increased permeation

Gudmundsson et al. (1999a)

Leu-enkephalin, DADLE

Peptidases

Phenylpropionic acid-based cyclic prodrug

Increased stability to Caco-2 peptidases and increased permeation

Gudmundsson et al. (1999b)

Calcitonin

Peptidases

PEGylated

Increased stability in rat nasal mucosal homogenate

Na et al. (2004)

Table 1 (continued). Examples of Prodrugs to Reduce Presystemic Metabolism

Table 1 (continued). Examples of Prodrugs to Reduce Presystemic Metabolism were less effective in improving bioavailability (Hussain et al. 1987). A salicylate ester of naltrexone was also equally effective in increasing naltrexone oral bioavailability in dogs (Hussain and Shefter, 1988).

A much different approach to increasing the oral bioavailability of hydroxy-morphinans, including nalbuphine and naltrexone, involved derivatization at a position distinct from that involved in presystemic metabolism. Boswell and

oh o

H3COCO

oh o

rio.

hn h3ct

Figure 2. Structures of some of the prodrugs discussed as examples.

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