Pharmacokinetics and Bioavailability of Different Formulations of 2',3'-Dideoxyadenosine (NSC-98700) in Beagle Dogs

摘要

The pharmacokinetics of the anti-AIDS drug, 2'-3'-dideoxyadenosine (DDA, NSC-98700), were examined in dogs. No significant toxicity was noted after i.v. or oral doses of DDA. However, adenine caused significant elevations in BUN and creatinine levels when given i.v. and orally. Kidney granulomas with foci of amorphous, basophilic, nonbirefringent material were noted, as well as multifocal intersititial nephritis. The study showed that buffering or enteric-coating of DDA significantly increased bioavailability and prevented acid degradation of DDA to adenine in the stomach acid.