${\beta}$-씨클로덱스트린 포접화합물로부터 펜티아작의 용출

Studies on Dissolution of Fentiazac from ${\beta}-Cyclodextrin$ Inclusion Complex

To increase the solubility of fentiazac which is used widely as a non-steroidal antiinflammatory drug, its inclusion complex and suppositories were prepared and studied. Inclusion complexes of fentiazac with ${\beta}-cyclodertin$ $({\beta}-CyD)$ were prepared by four diffrent methods; coprecipitation method, kneading method, solvent evaporation method, freeze drying method. Suppositories of $fentiazac/{\beta}-CyD$ with PEG 1500 and Witepsol H-15 were prepared by solvent evaporation method and freeze drying method. Inclusion complex formation of fentiazac with ${\beta}-CyD$ was ascertained by powder X-ray diffractometry, differential scanning calorimetry and IR spectroscopy. The dissolution rate of fentiazac from the inclusion complex increased in distilled water and KP 2nd disintegration test fluids (pH 6.8) but extemly decreased in KP 1st disintegration test fluid (pH 1.2). Inclusion complexes prepared by freeze drying method and solvent evaporation method were similar. Freeze drying method seemed to be suitable for preparation of complex with most higher dissolution rate but coprecipitation method seemed not to be suitable. The dissolution rate of fentiazac increased markedly by ${\beta}-CyD$ complexation. The release rates of suppositories increased in the following order. Complex prepared by freeze dying method in PEG 1500 > complex prepared by solvent evaporation method in PEG 1500 > fentiazac in PEG 1500 > complex prepared by freeze dying method in Witepsol H-15 > complex prepared by solvent evaporation method in Witepsol H-15 > fentiazac in Witepsol H-15.