Useful Extend-release Chitosan Tablets with High Antioxidant Activity 英文参考文献.docVIP

Pharmaceutics 2010, 2, 245–257; doi:10.3390/pharmaceutics2020245 OPEN ACCESS pharmaceutics ISSN 1999-4923 /journal/pharmaceutics Article Useful Extend-release Chitosan Tablets with High Antioxidant Activity Taira Yasufuku 1,?, Makoto Anraku 1,?, Yuko Kondo 1, Toshiyuki Hata 1, Junzo Hirose 1, Nobuyuki Kobayashi 2 and Hisao Tomida 1,* 1 Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, 1 Sanzo, Gakuen-cho, Fukuyama 729-0292, Japan 2 Dainichiseika Color Chemicals Mfg. Co., Ltd., 7-6, Nihonbashi Bakuro-cho 1-chome, Chuo-ku, Tokyo, 103-8383, Japan ? These authors contributed equally to this work. * Author to whom correspondence should be addressed; E-Mail: tomida@fupharm.fukuyama-u.ac.jp; Tel.: +81-84-936-2111; Fax: +81-84-936-2024. Received: 6 May 2010; in revised form: 21 May 2010 / Accepted: 26 May 2010 / Published: 27 May 2010 Abstract: The antioxidant properties of different low molecular weight (LMW) chitosans (CS1; 22 kDa, CS2; 38 kDa, CS3; 52 kDa, CS4; 81 kDa) were examined for possible use in extended-release tablets. The criteria used were the ability of the chitosans to reduce Cu2+, and hydroxyl and superoxide radicals and N-centered radicals derived from 1,1-diphenyl-2-picrylhydrazyl, via the use of ESR spectrometry. CS2 showed the highest scavenging activity. CS1 and CS3, however, were much less effective and CS4 was not a viable antioxidant. The results suggest that CS2 could be useful in combating the development of oxidative stress. A series of chitosan tablets were prepared using a spray drying method and evaluated as an extended-release matrix tablet using theophylline (TPH) as a model drug. The release of TPH from the different MW chitosan tablets increased with increasing MW of the chitosan used. CS2, CS3 and CS4 showed a reasonable release activity, but CS1 showed the shortest release activity. Moreover, the CS2-TPH