Properties of an Oral Preparation Containing a Chitosan Salt

Abstract

The 2-(4-chlorophenoxy)-2-methylpropionic acid (CMP) salt of chitosan (CS), CS-CMP, and that of a CS derivative (CP), were prepared and their ability to adsorb bile acids investigated. CS-CMP and CP-CMP rapidly adsorbed taurocholate (TCA) and glycocholate (GCA) when these bile acids were present together in the medium, with simultaneous release of CMP. A secondary bile acid, taurodeoxycholate, was preferentially adsorbed over TCA and GCA. Alginate gel beads containing CS-CMP did not differ from CS-CMP alone in their manner of bile acids take up. Furthermore, oral administration of CS-CMP to rats resulted in decreased serum cholesterol and triacylglycerol levels for two weeks. Therefore, CS-CMP, as well as a vehiclecontaining CS-CMP, might be a useful agent with which to treat hyperlipidemia

Keywords

• Chitosan
• 2-(4-Chlorophenoxy)-2-methylpropionic acid
• Bile acid adsorption
• Drug release
• Hyperlipidemia