YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Interaction between Omeprazole and $\gamma$-Cyclodextrin

오메프라졸과 $\gamma$-시클로덱스티린과의 복합체 형성 및 제제학적 특성

  • Published : 1995.04.01
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Abstract

The interaction of omeprazole(OMP) with $\gamma$-cyclodextrin($\gamma$-CyD) was investigated by solubility study and the complexation was confirmed by means of UV/VIS spectrophotometer, circular dichroism, differential scanning calorimeter, and $^{1}$H nuclear magnetic resonance spectra. The stability, dissolution rate, and partition coefficient of the complex were measured. The results present that the benzimidazole moiety and a part of pyridine ring containing sulfur atom of OMP might be included into the cavity of $\gamma$-CyD and the formation type of inclusion complex appeared to be B$_{s}$. The stoichiometric ratio of OMP to $\gamma$-CyD in the complex was found to be 1:1 and the stability constant of the complex found to be 97.1 M$^{-1}$. And the dissolution rate of OMP was markedly increased by inclusion complex formation with $\gamma$-CyD, and so it was above 90% in 5 min. from solid complex. Oil to water partition coefficient of OMP-$\gamma$-CyD complex was 60, which is significantly higher than that of OMP itself, 36.4. The degradation rate constant of OMP were greater than OMP-$\gamma$-CyD complex in aqueous solutions of various pHs, and the half lives of OMP and OMP-$\gamma$-CyD at pH 9 were 279.2 and 509.9 days, respectively, showing that the complex was more stable than OMP, therefore it was thought that OMP was stabilized by inclusion formation with $\gamma$-CyD.

Keywords

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