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KMID : 0369820000300020113
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Jorunal of Korean Pharmaceutical Sciences
2000 Volume.30 No. 2 p.113 ~ p.118
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Pharmacokinetics of Antiviral Pyrimidine Analogs in Rats
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한규원/Han KW
정낙신/김길수/Jeong LS/Kim KS
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Abstract
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In order to assay the efficacy of newly synthesized antiviral compounds, pyrimidine analogs, pharmacokinetics of those were established as compared with already marketed zidovudine. Zidovudine (15, 20, 25 and 35 mg/kg), LJ142 (18.52 mg/kg) and LJ143 (15, 18.52 and 30 mg/kg) were administered orally and intravenously in rats, blood samples were collected post-injection(i.e., for 360 min) at appropriate time intervals. Those were analyzed by HPLC with UV detection at 265 nm. Pharmacokinetic parameters (Cmax,T1/2,MRT,AUC,AUMC,VdSS,Clt) were calculated. AUCs of zidovudine and LJ143 following I.V. dosing of 15∼25mg/kgand15∼18.18mg/kg were dose-independent. However, AUCs of zidovudine and LJ43 following I.V. dosing of 25∼35mg/kgand18.18∼30mg/kg were dose-dependent. The relative bioavailability of zidovudine, LJ142 and LJ143 following oral administration were 61.94, 46.44 and 78.24%, respectively.
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KEYWORD
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Antiviral drugs, Zidovudine, Pharmacokinetics, Dose dependency, Bioavailability
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