Prolonged release of drug from triacetyl-β-CyD complex for oral and rectal administration

Abstract

Triacetyl-β-cyclodextrin (TA-β-CyD), a hydrophobic cyclodextrin derivative, that is insoluble in water, was used to form a complex with flufenamic acid (FA). FA-TA-β-CyD complex formation was demonstrated by differential scanning calorimetry and powder X-ray diffractometry. The release rate of FA from the FA-TA-β-CyD complexes in phosphate buffer pH 6.8 was significantly retarded compared to that of FA from the FA and glucose mixture. When the FA-TA-β-CyD complexes were administered directly into the intraduodenal lumen, the plasma concentration of FA remained at a plateau level (10-18 μg/ml) for 6–8 h. An increased mean residence time of FA following FA-TA-β-CyD complexes administration was observed. These results indicate that TA-β-CyD may serve as a hydrophobic carrier in prolonged-release preparations of FA.