Bile salt binding properties of commonly used gastrointestinal drugs: maalox, carafate, and questran.
We have validated a method to measure bile salt binding by Maalox (aluminum hydroxide and magnesium hydroxide), Carafate (sucralfate), and Questran (cholestyramine) in vitro. The method used in this study involves a correction for adherent water volume and thus provides a correct measure of bile salt binding. With this approach, we described the binding properties of Maalox, Carafate, and Questran. The bile salt binding capacities of Carafate and Maalox are limited and do not have physiological or pharmacological significance. On the other hand, we found that Questran has substantial bile salt binding capacity. At the recommended dosage, Questran could deplete the total bile salt pool. We also found that Carafate, although not used as an antacid, has buffering capacity (maintaining a pH of solution in the range 4.2-4.8) which might contribute to its effectiveness as an ulcer treatment drug.
Shiau
Y F
YF
Gastroenterology Section, Veterans Administration Medical Center, Philadelphia, PA.
Schenkein
J P
JP
Liu
H J
HJ
Khouri
M R
MR
Watkins
J B
JB
D000536:Aluminum Hydroxide / Q000032:analysis*; D001647:Bile Acids and Salts / Q000032:analysis*; D002792:Cholestyramine Resin / Q000032:analysis*; D004338:Drug Combinations / Q000032:analysis; D006863:Hydrogen-Ion Concentration; D008274:Magnesium / Q000032:analysis*; D008276:Magnesium Hydroxide / Q000032:analysis*; D013392:Sucralfate / Q000032:analysis*
D001647:Bile Acids and Salts; D004338:Drug Combinations; D002792:Cholestyramine Resin; C013591:aluminum hydroxide, magnesium hydroxide, drug combination; D013392:Sucralfate; D000536:Aluminum Hydroxide; D008274:Magnesium; D008276:Magnesium Hydroxide