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  • Title: Antitumor activity of prolonged-release derivative of cytosine arabinoside, cytosine arabinoside-agarose conjugate.
    Author: Hashida M, Kojima T, Muranishi S, Sezaki H.
    Journal: Gan; 1978 Dec; 69(6):839-43. PubMed ID: 750275.
    Abstract:
    A prolonged-release derivative of cytosine arabinoside (Ara-C), cytosine arabinoside-agarose bead conjugate (Ara-C-AB), was synthesized and its pharmaceutical and pharmacological characteristics were examined. Ara-C was released successively for considerably long period from Ara-C-AB in vitro. Following intraperitoneal injection of 3H-Ara-C-AB, radioactivity could be detected in plasma and urine of BDF1 mouse for four days, while 3H-Ara-C administered as a free form was excreted completely in the first 24 hr. Increase in lifespan of L1210 leukemia-bearing mice was demonstrated after intraperitoneal injection of Ara-C-AB with both the dosage schedules of three days before and one day after inoculation of L1210 cells at the dose of 30 mg equivalent Ara-C/kg.
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