PHARMACOKINETICS OF N-(4-HYDROXYPHENYL)-ALL-TRANS-RETINAMIDE IN RATS

  • 1 January 1980
    • journal article
    • research article
    • Vol. 8  (3) , 168-172
Abstract
The concentration of N-(4-hydroxyphenyl)-all-trans-retinamide (HPR [an antineoplastic drug]) was determined in plasma and a variety of tissues from rats after an i.v. dose (5 mg/kg). The plasma concentration-time curve could be accurately described by a triexponential equation. The apparent volume of distribution of HPR was approximately 10-12 l/kg; the terminal half-life was 12 h. Metabolites of HPR were more abundant than intact drug in most tissues 24 h after the i.v. dose. A 5 day excretion study with radiolabeled HPR revealed that less than 2% of a single i.v. dose (5 mg/kg) is excreted as unmetabolized HPR in urine and feces; most of the radioactivity is eliminated in the feces. HPR was incompletely absorbed after an oral dose (10 mg/kg).

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