Document 0819
 DOCN  M9650819
 TI    The effect of food on pharmacokinetics of zalcitabine in HIV-positive
       patients.
 DT    9605
 AU    Nazareno LA; Holazo AA; Limjuco R; Passe S; Twardy SK; Min B; Massarella
       JW; Hoffmann-La Roche Inc., Department of Clinical Pharmacology,;
       Nutley, New Jersey 07110, USA.
 SO    Pharm Res. 1995 Oct;12(10):1462-5. Unique Identifier : AIDSLINE
       MED/96117509
 AB    PURPOSE. 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.
 DE    Acquired Immunodeficiency Syndrome/DRUG THERAPY/*METABOLISM  Adult
       Antiviral Agents/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS/  THERAPEUTIC
       USE  AIDS-Related Complex/DRUG THERAPY/*METABOLISM  Biological
       Availability  Female  *Food  Human  HIV Infections/DRUG
       THERAPY/*METABOLISM  Male  Middle Age  Reverse Transcriptase
       Inhibitors/ADMINISTRATION & DOSAGE/  *PHARMACOKINETICS/THERAPEUTIC USE
       Zalcitabine/ADMINISTRATION & DOSAGE/*PHARMACOKINETICS/THERAPEUTIC  USE
       JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).