YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Pharmacokinetics of Omeprazole-Resin by Crossover Design and the Variation of Absorption upon pH Change in the Guts of the Rat and the Rabbit

Omeprazole 수지염의 흰쥐와 토끼에서의 위장관내 산도변화에 따른 흡수변화 및 교차시험법에 의한 약물동태연구

  • Published : 1995.08.01
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Abstract

Pharmacolinetic profiles of omeprazole enteric coated granules including Ramezole$^\circledR$, Losec$^\circledR$, omeprazole-Na and omeprazole-resin salt were studied using the crossover design in rats and rabbits. The absorption variance of the preparations at the altered pH condition of the gastrointestinal tract was also studied. After oral administration of four omeprazole enteric coated pellets (10mg/kg) with and without concomitant administration NaHCO$_{3}$ (5 mg/ml, 60 mM) in the rats, the differences of absorplion rate and extent were evaluated. In the NaHCO$_{3}$, administration group, the T$_{max}$ appeared to be 2~10 times shorter than water administration group, and the $C_{max}$ also increased to about 4 times, and the AUC increased to about 2.5 times. Pharmacokinetic parameters of four omeprazole enteric coated pellets in rats showed no statistical significance (ANOVA, P>0.05) in both groups. In the crossover study, the second dosed drug showed 4~5 times increased bioavailability than first dosed drug, which shows the strong carry-over effect of acid secretion of the first dosed drug. The differences of the pharmacokinetic parameters of the two test formulations (Losec$^\circledR$ and omeprazole-resin) showed no statistical significance.

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References

  1. Clin. Pharmacokinet. v.19 no.1 Clinical pharmacokinetics of drugs used in the treatment of gastrointestinal diseases Lauritsen,K.;Laursen,L.S.;Madsen,R.
  2. Med. Res. Reviews v.10 no.1 Omeprazole: The first proton pump inhibitor Lindberg,P.;Wallmark,B.;Mattsson,H.;Rikner,L.;Hoffmann,K.J.
  3. Scand. J. Gastroenterol. v.20 no.suppl. 108 Emerging strategies in ulcer therapy: Pumps and receptors Berglindh,T.;Sachs,G.
  4. Scand. J. Gastroenterol. v.20 no.suppl. 108 Localization of omeprazole and metabolites in the mouse Helander,H.F.;Ramsay,C.H.;Regardh,C.G.
  5. Scand. J. Gastroenterol. v.20 no.suppl. 108 Animal pharmacodynamics of omeprazole-a survey of its pharmacological properties in vivo Larsson,H.;Mattson,H.;Sundell,G.;Carlsson,E.
  6. Drugs v.32 Omeprazole: A preliminary review of its pharmacodynamics and pharmacokinetic properties and therapeutic potential in peptic ulcer disease and Zollinger-Ellison syndrome Stephen-Clissold,S.P.;Campoli-Richards,D.M.
  7. Nature v.290 Substituted benzimidazoles inhibit gastric acid secretion by blocking ($H^+$/$K^+$)ATPase Fellenius,E.;Berglindh,T.;Sachs,G.;Olbe,L.;Elander,B.;Ostrand,S.E.;Wallmark,B.
  8. Scand. J. Gastroenterol. v.20 no.suppl. 108 The mechanism of action of omeprazole-a survey of inhibitory action in vitro Wallmark,B.;Lorentzon,P.;Larsson,H.
  9. Clin. Pharmacokinet. v.20 no.1 Clinical pharmacology of omeprazole Colin,W.H.
  10. TiPS v.14 Reversible inhibitors of the gastric $H^+$/$K^+$-transporting $ATP_{asc}$: A new class of anti-secrstory agent Pope,A.J.;Parsons,M.E.
  11. Eur. J. Clin. Pharmacal. v.26 Oral pharmacokinetics of omeprazole Howden,C.W.;Meredith, P,A,;Forrest,J.A.H.;Reid,J.L.
  12. Clin. Pharmacokinet. v.23 no.6 Pharmacokinetic study of omeprazole in elderly healthy volunteers Landahl,S.;Andersson,T.
  13. Scand. J. Gastroenterol. v.21 no.Suppl. 118 Omeprazole: pharmacokinetics and metabolisms of omeprazole in man Cederberg,C.;Andersson,T.
  14. Therapeutic Drug Monitoring v.12 The pharmacokinetics of omeprazole in humans-a study of single intravenous and oral doses Andersson,T.;Lundborg,P.
  15. Eur. J. Clin. Pharmacol. v.39 Pharmacokinetics of various single intravenous and oral doses of omeprazole Cederberg,C.;Andersson,T.
  16. Scand. J. Gastroenterol. v.20 no.suppl. 108 Development of an oral formulation of omeprazole Pilbrant,A.;Cederberg,C.
  17. U. S. Pat. 2. 611. 730 Medical preparation for reducing the body level of sodium Heming,A.E.
  18. ELSEVIER Manual of microsurgery on the laboratory rat Van dongen,J.J.;Remie,R.;Rensema,J.W.;Van wunnik,G.H.J.
  19. Pharmacokinetics(2nd ed.) Gibaldi,M.;Perrier,D.
  20. Basic clinical phamacokinetics(2nd ed.) Winter,M.E.;Anne,M.;Kimble,K.;Young,L.Y.
  21. Applied pharmaceutics and pharmacokinetics Shargel,L.;Yu,A.B.C.
  22. Manual of pharmacologic calculations with computer programs(2nd ed.) Tallarida,R.J.;Murray,R.B.
  23. J. Chromatogr. v.309 Detrmination of omeprazole and metabolites in plasma and urine by liquid chromatography Lagerstrom,P.O.;Persson,B.A.
  24. J. Chromatogr. v.571 no.1-2 Highperformance liquid chromatographic determination of lansoprazole and its metabolites in human serum and urine Aoki,I.;Okumura,M.;Yashiki,T.
  25. J. Chromatography v.426 Improved procedure for quantitation of omeprazole and metabolites using reverse-phase liquid-performance chromatography Amantea,M.A.;Narang,P.K.
  26. J. Chromatography v.278 Simultaneous HPLC analysis of omeprazole and its sulphone and sulphide metabolites in human plasma and urine Mihaly,G.W.;Prichard,P.J.;Louis,W.J.
  27. J. Pharmaceu. Biomedi. Analysis v.4 no.3 Fully automated gradient elution liquid chromatographic assay of omeprazole and two metabolites Grundevik,I.;Jerndal,G.;Persson,B.A.
  28. Archives Pharmacal Res. v.17 no.6 Determination of omeprazole in rat plasma by HPLC with column switching Shim,S.H.;Bok,S.J.;Kwon,K.I.
  29. Jpn. Pharmacol. Ther. v.21 no.10 胃潰瘍 十二指腸潰瘍에 대한 proton pump inhibitor의 全國共同硏究 三輪 剛;丹羽 寬文;常岡 健二
  30. Scand. J. Gastroenterol. v.21 Inhibition of basal and betazole- and sham-feeding-induced acid secretion by omeprazole in man Lind,T.;Cederberg,C.;Ekenved,G.;Olbe,L.
  31. J. Clin. pharmacol. therapeu. toxicol. v.31 no.2 Comparative bioavailability of two enteric-coated capsules of omeprazole in healthy volunteers Garg,S.K.;Chugh,Y.;Tripathi,S.K.;Kumar,N.;Sharma,P.L.
  32. Gastroenterol. v.88 Omeprazole: A study of its inhibition of gastric pH and oral pharmacokinetics after morning or evening dosage Prichard,P.J.;Yeomans,N.D.;Mihaly,G.W.;Jones,D.B.;Buckle,P.J.;Smallwood,R.A.;Louis,W.J.
  33. Br. J. Clin. Pharmacol. v.29 Pharmacokinetics and bioavailability of omeprazole after single and repeated oral administration in healthy subjects Andersson,T.;Andren,N.;Cederberg,C.;Lagerstrom,P.O.;Lundborg,P.;Skanberg,I.
  34. Drug Invest. v.2 no.4 Pharmacokinetics of omeprazole and metabolites following single intravenous and oral doses of 40 and 80 mg Andersson,T.;Regardh,C.G.
  35. Gut v.29 Effect of single and repeated intravenous doses of omeprazole on pentagastrin stimulated gastric acid secretion and pharmacokinetics in man Jansen,J.B.M.J.;Lundborg,P.;Baak,L.C.;Greve,J.;Ohman,M.;Stover,C.;Rohss,K.;Lambers,C.B.H.W.
  36. Digestion v.44 no.suppl 1 Omeprazole: Pharmacology, pharmacokinetics and interactions Oosterhuis,B.;Jonkman,J.H.G.
  37. Scand. J. Gastroenterol. v.20 no.suppl 108 Pharmacokinetics and metabolism of omeprazole in animals and man-an overview Regardh,C.G.;Gabrielsson,M.;Hoffmann,K.J.;Lofberg,I.;Skanberg,I.
  38. J. Kor. Pharm. Sci. v.23 no.1 Bioeqivalence of entric-coated omeprazole products Kim,C.K.;Jeong,E.J.;Lee,W.K.