Polysaccharides as potential antioxidative compounds for extended-release matrix tablets.
The objective of this study was to identify polysaccharides with antioxidant properties for use as potential antioxidative compounds for extended-release matrix tablets. The antioxidant properties of five different polysaccharides, high molecular weight alginate (H-ALG), low molecular weight alginate (L-ALG), high molecular weight chitosan (H-chitosan), low molecular weight chitosan (L-chitosan), and pectic acid (PA) were examined using N-centered radicals from 1,1'-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and reducing power, based on their ability to reduce Cu(2+). L-chitosan and PA had acceptable scavenging abilities and were good radical scavengers, with good reducing power, but the H-chitosan and alginate derivatives were much less effective. The results suggest that L-chitosan and PA could be useful in combating oxidative stress. A PA and L-chitosan interpolymer complex (IPC) tablet was prepared and evaluated as an extended-release tablet matrix using theophylline (TPH) as a model drug. The release of TPH from the matrix tablet (TPH/PA/L-chitosan=200 mg:150 mg:50 mg) was slower than that from PA only (TPH/PA/chitosans=200 mg:200 mg:0 mg) or L-chitosan only (TPH/PA/L-chitosan=200 mg:0 mg:200 mg) tablet. Turbidity measurements also indicated the optimum complexation ratio for IPC between PA/L-chitosan to be 1/3, indicating an acceptable relationship between the turbidity of the complex and the release ratio of TPH. These results suggest that an L-chitosan/PA complex would be potentially useful in an extended-release IPC tablet with high antioxidant activity.
Tomida
Hisao
H
Faculty of Pharmacy and Pharmaceutical Sciences, Department of Physical Pharmaceutics, Fukuyama University, 1 Sanzo, Gakuen-cho, Fukuyama 729-0292, Japan. tomida@fupharm.fukuyama-u.ac.jp
Yasufuku
Taira
T
Fujii
Takeshi
T
Kondo
Yuko
Y
Kai
Toshiya
T
Anraku
Makoto
M
D000166:Acridines / Q000737:chemistry; D052160:Benzothiazoles / Q000737:chemistry; D001713:Biphenyl Compounds / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D016166:Free Radical Scavengers / Q000737:chemistry*; D009391:Nephelometry and Turbidimetry; D010084:Oxidation-Reduction; D010618:Phenanthrolines / Q000737:chemistry; D010851:Picrates / Q000737:chemistry; D011134:Polysaccharides / Q000737:chemistry*; D013451:Sulfonic Acids / Q000737:chemistry; D013607:Tablets; D013806:Theophylline / Q000378:metabolism
D000166:Acridines; D052160:Benzothiazoles; D001713:Biphenyl Compounds; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016166:Free Radical Scavengers; D010618:Phenanthrolines; D010851:Picrates; D011134:Polysaccharides; D013451:Sulfonic Acids; D013607:Tablets; C529854:tetrapyridoacridine; C002502:2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid; D013806:Theophylline; C004931:1,1-diphenyl-2-picrylhydrazyl