Stabilization of AD-1590, a non-steroidal antiinflammatory agent, in suppository bases by .BETA.-cyclodextrin complexation.

TERUTAKA TAKAHASHI, Izumi Kagami, Kenzo KITAMURA, Yutaka Nakanishi, YU IMASATO

Chemical and Pharmaceutical Bulletin · 1986 · 13 citations · 0 references

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Abstract

Stabilization of AD-1590 in an oleaginous suppository by complexation with β-cyclodextrin (β-CvD) was investigated. Suppositories were stored at 37°C and 75% relative humidity. AD-1590 was rapidly decomposed by autoxidation in the case of the suppository containing only AD-1590. On the other hand, no decomposition was observed in the case of the suppository containing AD-1590-β-CyD complex. The stabilizing effect of complexation is considered to be attributable to insolubilization of AD-1590 in the oleaginous base. The release rate was also promoted by complexation. These results indicate that complexation with CyDs is a promising means of improving the bioavailability and the stability of drugs which are very unstable when solubilized in an oleaginous base.