Bile acid salt binding with colesevelam HCl is not affected by suspension in common beverages.
It has been previously reported that anions in common beverages may bind to bile acid sequestrants (BAS), reducing their capacity for binding bile acid salts. This study examined the ability of the novel BAS colesevelam hydrochloride (HCl), in vitro, to bind bile acid sodium salts following suspension in common beverages. Equilibrium binding was evaluated under conditions of constant time and varying concentrations of bile acid salts in simulated intestinal fluid (SIF). A stock solution of sodium salts of glycochenodeoxycholic acid (GCDC), taurodeoxycholic acid (TDC), and glycocholic acid (GC), was added to each prepared sample of colesevelam HCl. Bile acid salt binding was calculated by high-performance liquid chromatography (HPLC) analysis. Kinetics experiments were conducted using constant initial bile acid salt concentrations and varying binding times. The affinity, capacity, and kinetics of colesevelam HCl binding for GCDC, TDC, and GC were not significantly altered after suspension in water, carbonated water, Coca-Cola, Sprite, grape juice, orange juice, tomato juice, or Gatorade. The amount of bile acid sodium salt bound as a function of time was unchanged by pretreatment with any beverage tested. The in vitro binding characteristics of colesevelam HCl are unchanged by suspension in common beverages.
Hanus
Martin
M
Analytical Research and Development, Genzyme Drug and Biomaterial Research and Development, Waltham, Massachussets 02451, USA.
Zhorov
Eugene
E
D000499:Allylamine / Q000031:analogs & derivatives* / Q000378:metabolism; D000924:Anticholesteremic Agents / Q000378:metabolism*; D001628:Beverages; D000069472:Colesevelam Hydrochloride; D005999:Glycochenodeoxycholic Acid / Q000378:metabolism*; D006000:Glycocholic Acid / Q000378:metabolism*; D007419:Intestinal Secretions / Q000737:chemistry; D013657:Taurodeoxycholic Acid / Q000378:metabolism*
D000924:Anticholesteremic Agents; D000499:Allylamine; D013657:Taurodeoxycholic Acid; D005999:Glycochenodeoxycholic Acid; D006000:Glycocholic Acid; D000069472:Colesevelam Hydrochloride