YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Pharmacokinetic Study on DWQ-013, a New Quinolone, in Rats and Mice

신규 퀴놀론계 항생물질 DWQ-013의 흰쥐 및 생쥐에서의 체내동태

  • Published : 1995.06.01
Download PDF
⟨ Previous Next ⟩

Abstract

The phannacokinetics and tissue distribution of DWQ-013, a new quinolone, were examined in rats and mice following a single intravenous and oral administration. DWQ-013 in plasma and urine was determined by both HPLC and microbiological assay. The plasma concentration of the drug declined biexponentially. The terminal half life of the drug was 11.11$\pm$0.14 hour after intravenous dosing. The volume of distribution at terminal elimination phase(Vd$_\beta$) and total clearance of the drug were 1.29$\pm$0.15 l/kg and 0.78$\pm$0.09 l/h/kg. The bioavailability of DWQ-013 after oral administration was 56.0% (HPLC) and 77.2%(bioassay), respectively. Twelve-hour urinary recovery of drug was measured by HPLC and bioassay to 0.035$\pm$0009% and 4.71$\pm$066% after oral dosing, to 0.055$\pm$0.014% and 7.65$\pm$1.53% after intravenous dosing, which may indicate the presence of biologically active metabolites. Binding of the drug to plasma proteins ranged from 97%~99% at various concentrations. The drug was highly distributed in order of liver, kidney and lung after 1.5 hours in mice.

Keywords

References

  1. Antimicrob. Agents. Chemother. v.77 In vitro antibacterial activity of AM-715, a new nalidixic acid analog Ito,A.;Hirai,K.;Inoue,M.;Koga,H.;Suzue,S.;Irikura,T.;Misuhashi,S.
  2. Antimicrob. Agents Chemother. v.25 Ciprofloxacin, a quinolone carboxylic acid compound active against aerobic and anaerobic bacteria Chin,N.;Neu,H.C.
  3. Antimicrob. Agents Chemother. v.25 In vito activity of ciprofloxacin compared with those of other new fluorinated piperazinylsubstiuted quinolone derivates Caekenberghe,D.L.;Pattyn,S.
  4. Drugs v.35 Ciprofloxacin, A review of its antibacterial activity, pharmacokinetic properties and therapeutic use Campoli-Richards,D.M.;Monk,J.P.;Benfield,A.P.P.;Todd.P.A.;Ward.A.
  5. Yakhak Hoeji v.38 In vitro and in vivo antibacterial activities of the new quinolone, DWQ-013 Yu,Y.H.;Park,N.J.;Kim,B.O.;Choi,M.J.;Shim,J.S.;Kang,T.C.;Lee,J.W.;Kim,D.Y.
  6. Yakhak Hoeji v.38 General pharmacology of DWQ-013, a new synthetic quinolone antibiotics(effects on the central nervous system) Lim,S.W.;Kim,Y.M.;Yu,Y.H.;Lee,J.W.
  7. Soft Science Applied Phramacokinetics-Theory and Experiments Hanano,M.;Umemira,K.;Iga,T.
  8. Arzeim. Forch. v.36 Isolation and structural elucidation of urinary metabolites of ciprofloxacin Gau,W.;Kurz,J.;Petersen,U.;Ploschke,J.;Wuensche,C.
  9. Antimicrob. Agents Chemother v.27 Comparison of highpressure liquid chromatography and bioassay for determination of ciprofloxacin in serum and urine Joos,B.;Ledergerber,B.;Flepp,M.;Bettex,J.;Luthy,R.;Siegenthaler,W.
  10. J. Antimicrob. Chemother. v.26 no.SUP.B Quinolone pharmacokinetics and metabolism Loded,H.;Hoffken,G.;Boeckk,M.;Deppermann,N.;Borner,K.;Koeppe,P.
  11. Antimicrob. Agents Chemother. v.27 Pharmacokinetics of ciprofloxacin after oral and parenteral administration Hoffken,G.;Lode,H.;Prinzing,C.;Borner,K.;Koeppe,P.
  12. Antimicrob. Agents Chemther v.30 Absolute oral bioavilability of ciprofloxacin Drusano,G.L.;Standiford,H.C.;Plaisance,U.J.;Forrest,A.;Leslie,J.;Caldwell,J.
  13. Arzneim. Forsch. v.36 Pharmacokinetics of ciprofloxacin, 1st communication Seifert,H.M.;Maruhn,D.;Maul,W.;Forster,D.;Ritter,W.
  14. Antimicrob. Agents Chemother v.26 Pharmacokinetics of intravenouly administered ciprofloxacin Wise,R.;Lockley,R.M.;Webberly,M.;Dent,J.
  15. Clin. Pharmacokinet v.19 Clinical pharmacokinetics of ciprofloxacin Vance-Bryan,K.;Guay,D.R.P.;Rotschafer,J.C.
  16. Metabolism of ciprofloxacin in man In first ciprofloxacin workshop, proceedings Beermann,D.;Scholl,H.;Wingender,W.;Frster,D.;Beubler,E.;Neu,H.(ed.);Weuter,H.(ed.)
  17. Arzneim. Forsch. v.36 Pharmacokinetics of ciprofloxacin, 2nd communication Seifert,H.M.;Maruhn,D.;Scholl,H.