Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai
Patent
1985-12-10
1990-06-05
Evans, J. E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C-o-group doai
514 25, 514511, A61K 3305, A61K 3123, A61K 31225, A61K 31335
Patent
active
049314750
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a cholagogue and/or a gallstone solubilizer comprising a borneol compound as the active component thereof.
BACKGROUND ART
Unexpectedly, there are a wide variety of bile duct and gallbladder diseases which include cholangitis, cholecystitis, biliary dys-kinesia (bile filling up the gall bladder, discharge function disorder), cholelithiasis, etc., and these diseases not infrequently develop into chronic diseases. Operations encounter difficulties and do not always afford good results.
Accordingly, it is important to use cholagogues and like agents for causing bile to normally flow into the duodenum via the bile duct without stagnation, for preventing formation of gallstones and for dissolving gallstones for treatment.
We have carried out research on the medicinal efficacy of components of a Japanese traditional drug, "Kiogan", and found that (+)-borneol has a totally unexpected, strong and sustained activity to promote the flow of bile and to dissolve gallstones and further that other borneols also have similar activity. Thus, the present invention has been accomplished.
DISCLOSURE OF THE INVENTION
Borneols are generally in the form of white crystalline powder or blocks and have unique fragrance. The pharmacological activities of borneols are not known except that naturally occurring (+)-borneol is empirically known to have pharmacological activities such as analgesic, anti-inflammatory, sedative and anti-palpitation effects and central depressant activity because it has fragrance and has long been used in the oriental medicine under the name of "Ryuno".
With attention directed to the cholagogic activity and gallstone dissolving activity of borneol compounds which activities have not been heretofore known, the present invention provides a novel cholagogic and gallstone solubilizing agent which contains a borneol compound as its active component.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 is a graph showing variations in the amount of secreted bile with time when (+)-borneol was administered to rats intraduodenally or orally;
FIG. 2 is a graph showing variations in the amount of secreted bile with time when (-)-borneol, (.+-.)-borneol, acetic acid ester of borneol, acetic acid ester of isoborneol or isoborneol was intraduodenally given to rats;
FIG. 3 is a graph showing variations in the amount of secreted bile with time when bornyl glucoside was intraduodenally administered to rats;
FIG. 4 is a graph showing variations in the amount of secreted bile with time when bornyl succinate was orally administered to rats; and
FIG. 5 to FIG. 11 are graphs showing variations in the weight of solids, content of phospholipids, content of cholesterol, amounts of bile acids and total amount of bile acids in the secreted bile with the lapse of time when (+)-borneol or sodium dehydrocholate was intraduodenally administered to rats.
BEST MODE OF CARRYING OUT THE INVENTION
According to the present invention, the borneol compounds include the following.
a. Borneols such as (+)-borneol, (-)-borneol, (.+-.)-borneol, (+)-isoborneol, (-)-isoborneol and (.+-.)-isoborneol.
(+)-, (-)- and (.+-.)-borneols are represented by the following structural formula and have a melting point of 204.degree. to 208.degree. C. ##STR1##
(+)-, (-)- and (.+-.)-isoborneols are represented by the following structural formula and have a melting point of 212.degree. to 214.degree. C. ##STR2##
b. Esters of borneols with fatty acids (R--COOH wherein R is alkyl having 1 to 9 carbon atoms). The esterification reaction is represented by the following equation. ##STR3##
The following alkyl-containing acids are examples of useful fatty acids.
Acetic acid (CH.sub.3 --)
Propionic acid (CH.sub.3 --CH.sub.2 --)
n-Butyric acid (CH.sub.3 --(CH.sub.2).sub.2 --)
Isovaleric acid ##STR4## n-Caproic acid (CH.sub.3 (CH.sub.2).sub.4 --) n-Enanthylic acid (CH.sub.3 (CH.sub.2).sub.5 --)
c. Esters of borneols with dicarboxylic acid (HOOC-(CH.sub.2).sub.n -- COOH where n is 2, 3 or 4).
Examples of useful dicarboxylic aci
REFERENCES:
patent: 2657166 (1953-10-01), Stonecipher
patent: 2666728 (1954-01-01), Smith
patent: 3181151 (1965-05-01), Nordmann
patent: 4242360 (1980-12-01), Pailer et al.
patent: 4767783 (1988-08-01), Hara et al.
Chemical Abstracts, Apr. 26, 1982, vol. 96, No. 17, p. 87, 96: 135798u.
The Merck Index, ninth edition (1976), pp. 173 and 174.
Evans J. E.
Hiya Pharmaceutical Co., Ltd.
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