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Development of New Omeprazole-Ion Exchange Resin Complex

Omeprazole(OMZ)-cholestyramine(CHL) and various OMZ-Dowex resin complexes were prepared by reaction between OMZ and activated resins in O.lN NaOH solution. And their physical properties were tested by means of infrared(IR), differential scaning caloimeter(DSC), X-ray diffraction. Chemical stability of OMZ-CHL was increased markedly compared with OMZ and the decomposition of OMZ-CHL followed the pseudo first-order kinetics and the rate constants were 2.743 X 10-4/day at 20oC, 7.83 X 10-3/day under 80% RH and 1.68 X 10-2/day 1 under UV radiation, respectively. On the other hand, the rate constants of OMZ were 2.996 X 10-4/day at 20oC, 1.17 X 10-2/day under 85% RH, and 4.07 X 10-2/day under UV radiation, respectively. The rates of dissolution of OMZ-CHL bulk and OMZ-CHL tablet were 100% and more than 85% in 15 minutes, respectively, which ere increased than OMZ base and OMZ-tablet. In the acute toxicological test, the value of oral LD50(mouse) was 4.608g/kg. OMZ-CHL was pelletized using lactose, polyethyleneglycol(PEG), D-sorbitol, Avicel PH 101, sodium laurylsulfate and polyvinylpyrrolidone(PVP) K-30, and enteric coated with HPMCP, Myvacet, acetone, ethanol and cetanol, of which dissolution rate was found to be more than 85% in 10 minutes. From the above results, it was found that OMZ-CHL is a useful means for development of new oral dosage forms of OMZ.