Characterization of Polymorphs of a Novel Quinolinone Derivative, TA-270(4-Hydroxy-1-methyl-3-octyloxy-7-sinapinoylamino-2(1H)-quinolinone)

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The polymorphic forms and amorphous form of TA-270(4-hydroxy-1-methyl-3-octyloxy-7-sinapinoylamino-2(1H)-quinolione), a newly developed antiallergenic compound, were characterized by powder X-ray diffractometry, thermal analysis, infraed spectroscopy and solid state ^<13>C-NMR. The intrinsic dissolution rates of polymorphic forms were measured using the rotating disk method at 37℃. The dissolution rates correlated well with the thermodynamic stability of each polymorphic form. These dissolution properties were clearly reflected in the oral bioavailability of TA-270 in rats. The transition behavior for each polymorph and for the amorphous form was studied under the high temperature and humidity conditions. The β- and δ-forms were transformed into the α-form by heating. The amorphous form was also easily crystallized into α-form by heating, however it was relatively stable under humidified conditions. The internal molecular packing of each polymorph was estimated from IR and solid state NMR spectral analysis.
公益社団法人日本薬学会の論文
2001-10-01