The effect of food on pharmacokinetics of zalcitabine in HIV-positive patients.
OBJECTIVE
The purpose of this study was to determine the effect of food on the pharmacokinetics of zalcitabine in HIV-positive patients.


METHODS
Twenty patients received single oral 1.5 mg doses of zalcitabine with and without a standard breakfast in an open-label, randomized crossover study with at least a one week washout period between treatments. Serial blood and urine samples were collected over 24 hours and assayed for zalcitabine by a modified GC/MS method.


RESULTS
Administration with food delayed and prolonged absorption resulting in a decrease of approximately 39% in maximal plasma concentrations compared to dosing under fasting conditions. Comparison of plasma AUC values indicated a small (14%) reduction in bioavailability when given with food. Approximately 59% and 45% of the dose were excreted unchanged in the urine under fasting and fed conditions, respectively.


CONCLUSIONS
The results of this study show that the administration of zalcitabine with food results in a mild reduction in bioavailability. Although these changes are not expected to be of clinical importance, further studies must be conducted for confirmation.
Nazareno
L A
LA
Hoffmann-La Roche Inc., Department of Clinical Pharmacology, Nutley, New Jersey 07110, USA.
Holazo
A A
AA
Limjuco
R
R
Passe
S
S
Twardy
S K
SK
Min
B
B
Massarella
J W
JW
D000386:AIDS-Related Complex / Q000188:drug therapy / Q000378:metabolism*; D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy / Q000378:metabolism*; D000328:Adult; D000998:Antiviral Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001682:Biological Availability; D005260:Female; D005502:Food; D015658:HIV Infections / Q000188:drug therapy / Q000378:metabolism*; D006801:Humans; D008297:Male; D008875:Middle Aged; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D016047:Zalcitabine / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use
D000998:Antiviral Agents; D018894:Reverse Transcriptase Inhibitors; D016047:Zalcitabine