Article

Effects of oxethazaine and gamma-cyclodextrin complex formation on intestinal contractions

Author : Yutaka Inoue, Rina Suzuki, Misa Horage, Mio Togano, Hajime Moteki, Mitsutoshi Kimura, Masahiko Ogihara, Shigeru Ando, Junko Kikuchi, Isamu Murata, Ikuo Kanamoto

The aims of this study were to prepare ground mixtures (GMs) and a coprecipitate (CP) of oxethazaine (OXZ) and γ-cyclodextrin (γCD) and to assess the physicochemical properties of those inclusion complexes. of OXZ and γCD. Assessment of the physical properties of complexes in a solid state and in solution suggested that inclusion complexes were formed in a GM and the CP when the molar ratio of OXZ/γCD was 1/2. The formation of OXZ/γCD=1/2 inclusion complexes resulted in increased solubility, and small amounts of those complexes were found to promptly inhibit ileal contractions. In addition, the CP was the only preparation that significantly inhibited the contraction of smooth muscle in response to Ba2+ and acetylcholine (ACh). Thus, a CP of OXZ/γCD would be highly useful in treating intestinal spasms as an inhibitor of the contraction of smooth muscle in the ileum.


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