Increased Stability in the Gastrointestinal Tract

The Parkinson's-Reversing Breakthrough

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The poor absorption of carbenicillin (Figure 9.14) after oral administration can to a large extent be attributed to fast acid-catalyzed degradation in the gastrointestinal tract. More acid resistant prodrugs such as carindacillin and carfecillin (Figure 9.14) have been shown to significantly increase the bioavailability of cabenicillin.

Gangciclovir

Gangciclovir

Valgangciclovir

GI epithelium

-> Bioavailability <10%

Prodrug conversion to active gangciclovir

Bioavailability about 60%

FIGURE 9.12 Absorption of gangciclovir and valgangciclovir.

Dopamine

Dopamine

FIGURE 9.13 Dopamine and levodopa.

Levodopa

Levodopa

COOH

COOH

Carbenicillin

Carindacillin

Carfecillin

FIGURE 9.14 Carbenicillin, carindacillin, and carfecillin.

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