Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-01-18
1998-12-08
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
A61K 3156
Patent
active
058469648
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/01187 filed Jul. 19, 1994, published as WO95/03056 Feb. 2, 1995.
FIELD OF THE INVENTION
The present invention relates to a hepatitis C virus proliferation inhibitor containing bile acid as the active principle.
BACKGROUND ART
Hepatitis, which is neither hepatitis A nor hepatitis B, forms 95 to 100% of post-transfusion hepatitis and 40 to 50% of sporadic hepatitis and easily becomes chronic, further changing at high rates to cancer of liver via chronic hepatitis or hepatic cirrhosis. Recently, hepatitis C virus (hereinafter referred to as HCV) was identified, and it has been demonstrated that most of hepatitis previously known as non-hepatitis A or non-hepatitis B are caused by this hepatitis C virus.
Although interferon has been known as an agent having inhibitory effect on the proliferation of hepatitis C virus, it is pointed out that there are problems such as its low rate in the effectiveness as little as 30 to 40%, the 60 to 70% recrudescence after discontinuance of the dosage thereof, the appearance of influenza-like symptoms, such as pyrexia, headache and vomiting, and of diverse side effects such as leukopenia, at the high rates.
Bile acid is a drug being publicly known as a choleretic, liver function improving agent, etc. As examples of the inhibitory effect of bile acid on the proliferation of virus, the anti-viral activities against herpes virus, human immunodeficiency virus, influenza virus, parainfluenza virus, etc., have been known (see Japanese Patent Laid-opened Nos. Sho 59-167517 Gazette, Sho 63-301823 Gazette, Hei 2-167235 Gazette, Hei 4-500514 Gazette and Hei 4-500670 Gazette). However, it has not been known that bile acid has an inhibitory effect on the proliferation of hepatitis C virus. Although a suppository preparation comprising an ursodeoxycholic acid salt and interferon is disclosed in Japanese Patent Laid-opened No. Sho 62-77333 Gazette, the bile acid is used just as an absorption promoting agent in the dosage of interferon into colon or rectum, and therefore, the disclosure does not suggest at all that bile acid has an inhibitory effect on the proliferation of hepatitis C virus.
It is an object of the present invention to provide a novel and highly effective hepatitis C virus proliferation inhibitor which gives no adverse reaction.
DISCLOSURE OF THE INVENTION
As a consequence of enthusiastic investigation made by the inventors of the present invention on hepatitis C and hepatitis C virus, such inventors found that bile acid can show an inhibitory effect on the proliferation of hepatitis C virus and have subsequently accomplished the present invention. Namely, the present invention is directed to a hepatitis C virus proliferation inhibitor comprising bile acid or the physiologically acceptable salts thereof as the active principle.
As bile acid to be used in the present invention, free bile acid, such as ursodeoxycholic acid and chenodeoxycholic acid, or conjugated bile acid such as tauroursodeoxycholic acid can be exemplified. As the physiologically acceptable salt of bile acid, an alkali metal salt thereof such as the sodium salt can be exemplified. These salts can be prepared according to any of the methods for manufacturing bile acid widely known in the art.
As the administration route for the hepatitis C virus proliferation inhibitor according to the present invention, oral administration with any of tablets, capsules, granules, powders, medicated syrup, etc. or parenteral administration with injections,. suppositories, etc. can be exemplified. These pharmaceutical preparations can be prepared by combining with additives, such as fillers, binders, disintegrators, lubricants, stabilizers and correctives, and according to any of the methods widely known in the art. The dose range of the inhibitory agent for an adult per day, though subject to symptoms and ages of the patients as well as other factors, is normally from 800 to 3,000 mg, preferably from 1,200 to 1,800 mg, and more preferably from 1,400 to 1,600 mg, for oral administr
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Henley III Raymond
Tokyo Tanabe Company Limited
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