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Ion Exchange Resins in Drug Delivery
Published in Arup K. SenGupta, Ion Exchange and Solvent Extraction, 2007
Sunil K. Bajpai, Manjula Bajpai, Sutanjay Saxena
In addition to the utility of ion exchange resins as excipients, these materials are explored for their therapeutic potential as well. Cholestyramine was the first polymeric resin-based drug approved for the treatment of high cholesterol. The cationic resin in this case serves as a sequestrant to bind bile acids in the gastrointestinal tract. The binding and effective removal of bile acids forces the liver to consume cholesterol and synthesize more bile acids. This leads to an indirect reduction in cholesterol level. The advantage of this therapy is that it does not use conventional drugs and hence shows fewer side effects as compared with conventional therapies. However, a drawback of this therapy is the higher dose requirement for the first-generation resins (4 tablespoons to be administered via fruit juice). Subsequent generation therapies have utilized molecular modeling strategies to impart specificity to the resin, thereby decreasing the dose to capsule size (e.g., Welchol® developed by Genzyme). Specificity for these resins has been achieved by the use of polymers that bind not only via electrostatic interaction but also by other forces such as hydrophobic interactions. Ion exchange resins have also been used for hemoperfusion and management of drug overdoses (poisoning). At present, cholestipol (anion exchange resin) is used in the treatment of type II hyperlipoproteinemia and familial hyperlipoproteinemia in children and young adults.81 The resin is mixed with fluids and administered as slurry.
Process optimization in ginseng fermentation by Monascus ruber and study on bile acid-binding ability of fermentation products in vitro
Published in Preparative Biochemistry & Biotechnology, 2021
Chongyan Zhao, Fang Yang, Feng Lin, Qingsong Qu, Zhixun Li, Xing Liu, Lu Han, Xinyuan Shi
The binding rate of 50 mg of cholestyramine to ST and SC was 87.31 and 77.76%, which were higher than our sample. As the amount of fermentation product increases, the bile salt binding rate increases accordingly (Figure 6). When PM is 150 mg, its binding rate to ST and SC reaches 68% and 71%, respectively, which is equivalent to the binding rate of cholestyramine. The cholestyramine contains a large number of amino groups, which can bind to the carboxyl groups in the bile acid molecule, thereby binding a large amount of bile acid molecules.[40] But cholestyramine is believed to have some adverse side effects, such as constipation, nausea, indigestion, etc., which affect its application. Therefore, ginseng fermented through M. ruber not only was more effective in lipid-lowering activity, but also was safer for our body.