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KMID : 0369819970270040253
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Jorunal of Korean Pharmaceutical Sciences
1997 Volume.27 No. 4 p.253 ~ p.263
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Complexation of Omeprazole with Meglumine and its Stability
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이계주/Rhee GY
김성욱/도기찬/박종범/황성주/Kim SW/Do KC/Park CB/Hwang SJ
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Abstract
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To investigate the interaction of omeprazole (OMP) and meglumine (MEG), a complex was prepared by freeze-drying method in ammoniacal aqueous medium at room temperature and subjected to IR, DSC, and 1H NMR analysis. In addition, the stability of the complex was tested by accelerated stability analysis, and the dissolution rate of both powder and enteric coated was determined pellet by paddle method. The results are as follows; i) IR, DSC, and 1H NMR studies indicate the formation of inclusion complex between OMP and MEG probably by electrostatic forces as [OMP][MEGH]+ form in a stoichiometric ratio (1:1) of OMP : MEG. ii) The dissolution rate of enteric coated OMP-MEG complex pellet in simulated enteric fluid was 90.6% in 10 minutes, which may satisfy the requirement for the regulation of dissolution. iii) OMP-MEG complex were decomposed according to pseudo 1st order kinetics: while the decomposition of OMP showed a rate constant (k25?C) of 5.13×10?4?day?1, a half-life(t1/2) of 1,350 days, a shelf-life(T_{90%}) 205 days and an activation energy of 23.53 kcal/mole. OMP-MEG complex inhibited a rate (k25) of 2.92×10?4?day?1, a half-life(t1/2) of 2,373 days, a shelf-life (T_{90%}) of 306 days and an activation energy of 20.18 kcal/mole. iv) OMP was stabilized markedly by the formation of OMP-MEG complex between OMP and MEG, and the humidity increased the stability of OMP-MEG complex by decreasing the decomposition rate(k50?C) from 1.27×10?2?day?1 at 31% R.H. to 2.54×10?2?day?1 at 90% R.H.
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KEYWORD
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Omeprazole, Omeprazole-Meglumine complex, Stability, Dissolution rate, Decomposition rate constant
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