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KMID : 0043319900130020147
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Archives of Pharmacal Research
1990 Volume.13 No. 2 p.147 ~ p.150
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Pharmacokinetics of Methotrexate after Intramuscular Injection of Methotrexate-Polylysine Conjugate in Rabbits
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Yoon EJ
Lee MG/Lee HJ/Park MK/Kim CK
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Abstract
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Methotrexate (MTX)-poly-L-lysine (PLL) conjugate was relatively stable in phosphate buffer of pH 7.4 and in plasma. However, liver homogenate accelerated the release of MTX from the conjugate. Pharmacokinetics and tissue distribution of MTX were compared after intramuscular injection of MTX (treatment I) and MTX-PLL conjugate (treatment II), 10mg/kg as free MTX to rabbits. The peak concentrations of MTX in treatment II were significantly lower than those in treatment I. The amount of MTX excreted in 24-hr urine was significantly reduced in treatment II and it suggested that MTX be more metabolized in treatment II than in treatment I. The amounts of MTX remaining in each organ after 24-hr of intramuscular injection were not significantly different in both treatments.
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