Delivery of 2',3'-dideoxyinosine via intratracheal instillation (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

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Delivery of 2',3'-dideoxyinosine via intratracheal instillation (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 36:A2408 1995. Unique Identifier : AIDSLINE ICDB/95610182
Gao X; Wientjes MG; Jurcisek JA; Au JL; College of Pharmacy, Ohio State Univ., Columbus, OH 43210

Abstract: We have shown that the low and variable oral bioavailability (average of 17%, range of 8-23%) of the anti-AIDS drug, 2',3'-dideoxyinosine (ddI), in rats is primarily due to its first-pass elimination in gastric acid and by intestinal flora. This study evaluated whether the intratracheal administration route provides an improved systemic bioavailability. A ddI dose (40 mg/kg in 200 ul) was instilled into the trachea in female Fisher rats and an intravenous tracer dose (9 ug/kg) of 3H-ddI was administered concomitantly to determine the drug clearance. ddI was rapidly absorbed from the lungs; the peak concentration, 17.1 +/- 6.6 ug/ml (mean +/- SD), was reached at 3.4 +/- 2.5 min. The ddI clearance was 74.0 +/- 12.6 ml/min/kg, and the intratracheal bioavailability was 62.8 +/- 6.1% (range 55.0-73.4%). The instillation of a dye solution intratracheally showed that a fraction of the dose spilled over to the gastrointestinal tract, which may have caused the less-than-complete bioavailability. These data indicate a higher and less variable bioavailability of ddI by the intratracheal than by the oral route, which may be further enhanced by using appropriate formulations that localize the entire dose in the lung.
Keywords: Animal Biological Availability Didanosine/*ADMINISTRATION & DOSAGE/PHARMACOKINETICS Female Rats Rats, Inbred F344 Trachea ABSTRACTKWDanimalbiologicalavailabilitydidanosine/KWDadministration&dosage/pharmacokineticsfemaleratsrats,inbredf344tracheaabstract
951030
M95A0970

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