Physicochemical properties and dissolution improvements of 9,10-anthraquinone-2-carboxylic acid and 2-phenyl-4-quinolone

• Main Authors: Tsai, Shang-Yuan, 蔡尚元
• Other Authors: Shan-Yang Lin
• Format: Others
• Language: zh-TW
• Published: 1996
• Online Access: http://ndltd.ncl.edu.tw/handle/22625165088364159839

博士 === 中國醫藥學院 === 藥物化學研究所 === 84 === 　　9,10-Anthraquinone-2-carboxylic acid ( AQCA ) is a　quinone derivative and 2-phenyl-4-quinolone ( PQO ) is a　quinolone deri-vative. AQCA was found to posses antiallergic　activity; PQO was shown to demonstrate anticancer and　antiarrhythmic effects. In this study, the physicochemical properties of AQCA and PQO were investigated. Their solid dispersions or ground mixtures were prepared and in-vitro dissolution tests were carried out to investigate the improvement on dissolution. 　　By using FT-IR, differential　scanning calorimetry and pow-der X-ray diffractometry, AQCA was　found to appear as crystal Form I and methanolic solvate. PQO　found to appear as crystal Form I and II. Both compounds are　insoluble in water. 　　The solid dispersions of AQCA showed　amorphous and in-creased dissolution rate when the content of povidone over 70％. The ground mixture of AQCA showed amorphous and enhanced dissolution rate when the content of gelatin over 80%. The stabi-lity study indicated the ground mixture with gelatin was better. 　　The solid dispersions of PQO in polyethylene glycol 10,000 or povidone K-90 showed the dissolution rate of PQO in povidone K-90 was much higher than that in polyethylene glycol 10,000.