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2001). The double prodrug ximelagatran was developed to try to improve the oral absorption of melagatran. Ximelagatran has an ethyl ester group in place of the carboxylic acid and an Nhydroxyamidine group in place of the amidine. 2. 5. 2. This is also illustrated in Scheme 6. , 2001; Gustafsson, 2003). , 2001). Poly- or zwitterionic compounds present a challenge. Like the example of melagantran discussed above in relation to the changes in the pKa value of a benzamidine group, other poly-charged molecules are difficult to absorb from the GIT unless the molecule, by chance or design, is a substrate for carrier-mediated transport.

Pro-drugs as Novel Drug Delivery Systems. Washington DC. ACS Symposium Series #14, American Chemical Society; 1975 Horspool KR, Lipinski CA. Enabling Strategies: Advancing New Drug Delivery Concepts to Gain the Lead. Drug Deliv Tech 2003; 3:34–46 Im WB, Sih JC, Blakeman DP, and McGarth JP. Omeprazole, a Specific Inhibitor of Gastric (H+–K+)–ATPase, is a H+–Activated Oxidizing Agent of Sulfhydryl Groups. J Biol Chem 1985; 260:4591–4597 Johnson P. Pro-drugs and First-Pass Effects. Chem Ind 1980; June 7:443–447 Jusko WJ.

1961). A more recent example is famciclovir (6), a deoxydiacetate prodrug of penciclovir (5). In this case, not only were two primary hydroxl groups acetylated but additional lipophilicity was gained by removal of the 6-oxy functional group. Bioconversion of 5 required two deacetylation steps and an oxidation event (probably xanthine oxidase). , 1998). In rats the oral bioavailability of penciclovir was only 1–2%. When 6-deoxy penciclovir was dosed, the bioavailability of penciclovir was increased to 9%.

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