DESIGN AND CHARACTERIZATION OF SEVELAMER HYDROCHLORIDE: A NOVEL PHOSPHATE-BINDING PHARMACEUTICAL

Sevelamer hydrochloride (polyallylamine crosslinked with epichlorohydrin) is a polymeric hydrogel that has been developed as an oral pharmaceutical to prevent the absorption of dietary phosphate by kidney dialysis patients. It has been found to bind to phosphate in vitro, and to do so more effectively than a wide range of other cationic polymers. It shows a preference for phosphate over other intestinal anions, such as chloride and bicarbonate. The preference for phosphate is believed to be due to its dianion character, and may also involve hydrogen bonding. The absorption of phosphate in vitro is rapid (less than a minute) relative to the time of passage of such a drug through the small intestine (hours). It has also been found to prevent the absorption of dietary phosphate in vivo and in humans, and is presently awaiting FDA approval.