STUDIES ON DISTRIBUTION OF DIANHYDROGALACTITOL INTO CENTRAL NERVOUS-SYSTEM OF RAT

  • 1 January 1978
    • journal article
    • research article
    • Vol. 62  (3) , 409-412
Abstract
The distribution of dianhydrogalactitol-C14 (DAG-C14) [an agent which is currently being evaluated for treatment of cancer of the CNS] which was administered to rats as an i.v. bolus injection was studied in plasma and brain tissue. Analysis of samples was carried out by a high-pressure liquid chromatography method which specifically responds to the parent drug. Samples were monitored by both UV and liquid scintillation spectrometry. Plasma level measurements indicate that intact DAG has a relatively short half-life in plasma (t1/2 [half-time] = 43.7 min, and brain (t1/2 = 50.3 min). These findings differ significantly from those studies which have measured total radioactivity when monitoring DAG levels, and should be considered in the design of DAG dose regimens. Data from both brain and plasma were consistent with a classic 2-compartment open model.