Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Polymer from ethylenic monomers only
Patent
1979-07-18
1980-12-23
Roberts, Elbert L.
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Polymer from ethylenic monomers only
424238, 424 35, 424 37, 2603971, 424240, A01N 4502, A61K 31575, A61K 932, A61K 940
Patent
active
042410479
DESCRIPTION:
BRIEF SUMMARY
The present invention concerns a novel medicinal composition for the treatment of biliary lithiasis.
It is known that biliary lithiasis is characterised by the presence in the bile of calculi formed essentially of cholesterol. Under normal physiological conditions, the water-insoluble cholesterol is solubilized in the bile in the form of a colloidal solution, thanks to the phospholipids and particularly to the biliary salts which permit the formation of micellae. Under pathological conditions, with subjects suffering from lithiasis, the cholesterol-enriched bile is incapable of completely solubilizing the cholesterol. The cholesterol excess precipitates and forms the vesicular calculi.
It is known from the work carried out by Danzinger and collaborators (N. Engl. J. Med. 1972, 286, 1-8) that chenodeoxycholic acid (C.sub.24 H.sub.40 O.sub.4, molecular weight 392.56) is capable of dissolving the vescular calculi when administered by oral route. These results have since been confirmed by numerous references. ##STR1##
It is also known from work carried out by NORTHFIELD and collaborators (Gut. 1975, 16, 1-17) that chenodeoxycholic acid acts essentially by decreasing the biliary secretion of the cholesterol.
This effect could result from a diminution of the hepatic synthesis of the cholesterol (Salen and collaborators, Clin. Res., 1973, 21, 523).
The use of chenodeoxycholic acid for the treatment of biliary lithiasis thus is of a certain degree of interest, but it is not without harmful secondary effects. In particular, there is noted a poor digestive tolerance with fairly frequent attacks of diarrhea, which are sometimes considerable and not well tolerated, a certain hepatic intolerance, with a raising of the transaminases and of the .gamma.-glutamyl transpeptidase. Moreover, the treatment is costly, because of the cost of the product and the amount of the posology.
According to the present invention, there has been found a means of overcoming the aforementioned inconveniences, secondary effects and cost of the treatment, by associating with the chenodeoxycholic acid a compound which is a spasmolytic of the main biliary duct and of the sphincter of Oddi and is choleretic: hymecromone (C.sub.10 H.sub.8 O.sub.3 --molecular weight 176, 173). ##STR2##
Hymecromone, a spasmolytic of the main biliary duct and of the sphincter of Oddi (VAYRE and HUREAU, Med. Cher. Dig. 1974, 3, 293-297) enlarges the diameter of the choledochus, opens the sphincter of Oddi and as a result facilitates the evacuation of the small size biliary calculi in the duodenum.
The choleretic hymechromone (FONTAINE L. and collaborators, Therapie, 1968, 23, 51-62, and U.S. Pat. No. 3,175,943), by increasing the volume of discharged bile, assures the flushing of the biliary duct and renews the contact of the calculi with the bile, and consequently causes a more rapid dissolving of the vesicular calculi.
Moreover, hymecromone is capable of modifying the composition of the bile, by decreasing particularly the concentration of cholesterol, as indicated in the following table, which gives the average of the results obtained in connection with five dogs after oral administration of hymecromone in the dose of 25 mg per kg.
______________________________________ Cholesterol content in the
bile (mg/liter)
______________________________________
Before treatment 420
30 minutes after treatment
102
1 hour after 110
11/2 hours after 132
2 hours after 145
21/2 hours after 170
______________________________________
The similar properties of chenodeoxycholic acid and hymecromone (decrease in the concentration of cholesterol in the bile) and the complementary properties of the hymecromone (spasmolytic and choleretic properties) make it possible, according to the present invention, to improve the effects of the chenodeoxycholic acid during lithiasis. Furthermore, hymecromone has an excellent digestive tolerance. The result of the association is in fact an improvement in the tolerance, a reduction in the cost of treatment and an impro
REFERENCES:
patent: 3175943 (1965-03-01), Molho et al.
patent: 4079133 (1978-03-01), Drees et al.
Northfield et al., "Gut", (1975), vol. 16, pp. 1-17.
Danzinger et al., "New Eng. Jour. Med.", (1972), 286, pp. 1-8.
Therapie (1968) (XXIII), article by Fontaine et al., pp. 52-62.
P. Vayre et al., J. Med. Cher. Dig. (1974), No. 3, pp. 293-297.
Lechevin Jean-Claude
Treilles Jean-Noel
Lipha Lyonnaise Industrielle Pharmaceutique
Roberts Elbert L.
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