Terfenadine-β-Cyclodextrin Inclusion Complex with Antihistaminic Activity Enhancement = 항히스타민 효과를 증진시킨 테르페나딘-베타-사이클로덱스트린 포접화합물

다국어 초록 (Multilingual Abstract)

Terfenadine, an antihistaminic drug, has relatively low bioavailability after oral administration due to its limited solubility in water. To enhance the antihistaminic activity of terfenadine, the lerfenadine-β-cyclodextrin (1:2) inclusion complex was prepared by the neutralization method. The solubility and dissolution of the inclustion complex were were carried out, and its antihistaminic activity was then evaluated and compared with terfenadine powder by the passive subcutaneous was higher at lower pH, while its formation ratio was 1:2 irrespective of pH. For terfenadine, it improved the solubility 200 times and the dissoluction rate 5 times. It gave a low histamine level at 30 min. followed by a sustained low level until 60 min, while terfenadine powder gave a low histamine level at 60 min , suggesting that it had faster and more effective antihistaminic activity than terfenadine powder in rats due to fast dissolution and absorption of terfenadine.