Useful Extend-release Chitosan Tablets with High Antioxidant Activity

Pharmaceutics

Taira Yasufuku¹  Makoto Anraku¹  Yuko Kondo¹  Toshiyuki Hata¹  Junzo Hirose¹  Nobuyuki Kobayashi² 

[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

关键词: chitosan;    antioxidant;    molecular weight;    matrix tablet;    extend-release;    radicals;   

DOI  :  10.3390/pharmaceutics2020245

来源: mdpi

【 摘 要 】

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 tablet showed the highest scavenging activity of the three chitosan tablets (CS2-CS4) using 2,2’-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radicals. These results suggest that a CS2-TPH tablet could be potentially useful in an extended-release matrix tablet with a high antioxidant activity.

【 授权许可】

CC BY   
© 2010 by the authors; licensee MDPI, Basel, Switzerland.