Gallstones cholate

In the bile cholesterol is kept soluble by fats, phospholipids like lecithin and by bile acids. The important bile acids in human bile are cholic acid, chen-odeoxycholic acid or chenodiol and ursodeoxycholic acid or ursodiol. Bile acids increase bile production. Dehydrocholic acid, a semisynthetic cholate is especially active in this respect. It stimulates the production of bile of low specific gravity and is therefore called a hydrocholeretic drug. Chenodiol and ursodiol but not cholic acid decrease the cholesterol content of bile by reducing cholesterol production and cholesterol secretion. Ursodiol also decreases cholesterol reabsorption. By these actions chenodiol and ursodiol are able to decrease the formation of cholesterolic gallstones and they can promote their dissolution. 

Matsumura et al. (1996) analyzed hypercholeresis in dogs with pigment gallstones after cholate infusion. 

In vitro, a solution of 97% d limonene was found to be 100-fold better at solubilizing cholesterol than sodium cholate. A small trial followed with 15 patients, whereby 20 mL of the d-limonene preparation, was introduced into the gallbladder via a catheter on alternate days for up to 48 days. Treatment was successful in 13 patients with gallstone dissolution sometimes occurring after three infusions. Side effects included vomiting and diarrhea (Igimi et al., 1976). 

Mechanism of cholesterol gallstone dissolution Analysis of the kinetics of cholesterol monohydrate dissolution in tauro-cholate/lecithin solutions by the Mazer, Bendek and Carey model, J.Phys.Chem., 85 127 (1981). 

A commercial emulsifying agent, glyceryl monooctanoate (monooctanoin), has been found to be an excellent solvent for cholesterol [278]. In vitro it dissolved mixed cholesterol gallstones more than twice as fast as did sodium cholate solutions which have been used as infusions for dissolution of retained cholesterol bile duct stones. Monooctanoin has also been tried by T-tube infusion in an attempt to effect direct dissolution of stones. Cholesterol solubility and dissolution kinetics are enhanced (Fig. 4.39). Monooctanoin infusions were well tolerated and some or all stones in 10 out of 12 patients were removed by dissolution by biliary tract infusion of monooctanoin over periods ranging from 4 to 21 days. 

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