BIOAVAILABILITY OF SODIUM CYANATE IN PATIENTS WITH SICKLE-CELL DISEASE AND LACK OF INHIBITION INVITRO OF GLOBIN-SYNTHESIS AT INVIVO CONCENTRATIONS OF CYANATE

  • 1 January 1975
    • journal article
    • research article
    • Vol. 195  (2) , 333-339
Abstract
The bioavailability in blood of sodium cyanate administered orally in gelatin capsules, in gelatin capsules plus antacid, in enteric-coated capsules and in cocoa butter suppositories administered rectally to patients with sickle cell disease was studied. Maximal blood concentrations of cyanate did not exceed 0.4 mM. Sodium cyanate taken orally in gelatin capsules yielded the highest blood concentrations of the drug, but the peak concentrations and curve areas were not necessarily dose-related. The duration of the drug in the circulation was about 210 min. Administration of sodium cyanate in the gelatin capsules, taken with an antacid, improved the dose-response relationship within a given patient. Enteric-coated capsules and suppositories showed variable and low bioavailability profiles, respectively. Variability in bioavailability between patients with a given dosage form requires further study. Since the concentration of cyanate attainable in vivo does not inhibit synthesis of either the .alpha.- or .BETA.-chain of hemoglobin in vitro, previous reports on the inhibitory effects of 10 to 100 mM cyanate on globin synthesis in vitro do not appear to be relevant.