In-vitro enhancement of cholesterol dissolution by commonly used drugs

Abstract

Abstract A rotating disc apparatus was used to study the dissolution of cholesterol in sodium cholate solutions and ox bile. Drugs with structures that render them capable of lowering interfacial resistance were tested and shown to increase cholesterol dissolution rates in both systems. In sodium cholate solutions, loperamide (3 times 10−4 M) increased the rate of dissolution by over six times, and a similar effect was observed with amitriptyline (3 times 10−3 M), diphenhydramine (3 times 10−3 M), dicyclomine (3 times 10−3 M) and propantheline (3 times 10−3 M). These drugs are as effective as benzalkonium chloride at these concentrations. Amitriptyline, propantheline, dicyclomine and diphenhydramine also increased cholesterol dissolution rates into ox bile. If these drugs are excreted into human bile in sufficient quantities and in an active form they may be able to enhance the speed of cholesterol gallstone dissolution therapy.