title: The effect of food on pharmacokinetics of zalcitabine in HIV-positive patients.
abstract: 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.
authors.affiliation: Hoffmann-La Roche Inc., Department of Clinical Pharmacology, Nutley, New Jersey 07110, USA.
authors.forename: L A
authors.initials: LA
authors.lastname: Nazareno
authors.forename: A A
authors.initials: AA
authors.lastname: Holazo
authors.forename: R
authors.initials: R
authors.lastname: Limjuco
authors.forename: S
authors.initials: S
authors.lastname: Passe
authors.forename: S K
authors.initials: SK
authors.lastname: Twardy
authors.forename: B
authors.initials: B
authors.lastname: Min
authors.forename: J W
authors.initials: JW
authors.lastname: Massarella
mesh_terms: 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
chemical_list: D000998:Antiviral Agents; D018894:Reverse Transcriptase Inhibitors; D016047:Zalcitabine