Intestinal absorption of dideoxynucleosides: characterization using a multiloop in situ technique.
The intestinal absorption of dideoxynucleosides was studied in rabbits, using a closed-loop mesenteric-sampling in situ technique developed in this laboratory, and the kinetic profiles were characterized. Each of the dideoxynucleosides exhibited different dependence on the intestinal regions studied: 3'-azido-2',3'-dideoxythymidine was best absorbed from the ileum, while 2',3'-dideoxyinosine and 2',3'-dideoxycytidine were preferentially absorbed from the jejunum. The results were validated by the mass-balance approach; the percent of drug retained in the intestinal lumen and that degraded at the intestinal pH, by colonic flora, in the intestinal tissue, and in plasma were assessed.
Mirchandani
H L
HL
Controlled Drug-Delivery Research Center, Rutgers, State University of New Jersey, College of Pharmacy.
Chien
Y W
YW
D000818:Animals; D001711:Biotransformation; D001834:Body Water / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D015224:Dideoxynucleosides / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D008297:Male; D008643:Mesentery / Q000378:metabolism; D011817:Rabbits; D012995:Solubility
D003692:Delayed-Action Preparations; D015224:Dideoxynucleosides