Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1987-12-04
1989-09-12
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424471, 424474, 424475, 424481, 4241951, A61K 4700
Patent
active
048658472
DESCRIPTION:
BRIEF SUMMARY
It is known that duodenal ulcers, ventricular ulcers and other gastric mucosa lesions, which are frequently induced by stress and/or medicaments, can bleed and perforate in a life-threatening manner.
It is also known that various foods, beverages and in particular medicaments irritate the gastric mucosa and in higher concentrations even attack the same, so that this can also lead to ulceration and bleeding. Gastric mucosa-irritating beverages are e.g. alcohol and strongly roasted coffee. The irritation is frequently based on a stimulation of gastric acid secretion. Certain drug or medicament groups, e.g. non-steroidal antirheumatics (NSAID) have a clearly defined side-effect spectrum, particularly undesired gastrointestinal effects (e.g. gastric mucosa lesions, associated with bleeding or perforation). Thus, it has been observed that acetylsalicylic acid can lead to gastrorrhagia, which also applies for other NSAID's, such as e.g. indomethacin (cf. R. Bruhn et al, Fortschritte der Medizin, 100 (36), pp 1661 to 1668 (1982). There is a definite risk linked with therapy with acetylsalicylic acid and other medicaments from the NSAID group, so that before using these medicaments, their therapeutic usefulness must be balanced against the accompanying risk.
It is an object of the present invention to find an agent protecting the gastric mucosa against the development of ulcerations in such a way that gastric mucosa-harming foods, beverages and/or medicaments can be administered or taken without disturbing side-effects extending up to life-threatening bleeding and perforation.
It has been found that this problem can be solved in that isolated chlorogenic acid or its physiologically acceptable derivatives are suitable for protecting the gastric mucosa against foods, beverages and/or medicaments, which are known to damage the gastric and duodenal mucosa or which can stimulate gastric acid secretions. According to the invention the tanning agents or] chlorogenic is are administered before or simultaneously with the intake of said irritating materials.
Within the scope of the invention the term chlorogenic acid is understood to mean the mono- and di-caffeoylquinic acids, as well as mixtures thereof. Particular preference is given to 3-, 4- and 5-caffeoylquinic acids or mixtures thereof and in particular 3-caffeoylquinic acid. The acids can be used as free acid or in the form of their physiologically acceptable derivatives, particularly salts or esters. Alkali metal salts and in particular potassium salts are particularly suitable. These derivatives can be used in place of the free acid, because the acid is liberated therefrom in the strongly acid gastric medium.
Chlorogenic acid is a compound occurring in numerous plants, e.g. in green coffee beans, was isolated by Freudenberg in 1920, its structure was explained and was subsequently also synthesized (cf. Merck Index, tenth edition, No. 2112). It is known from a publication by V. Istudor et al, Farmacia, 29, pp 41 to 48 (1981) that an extract obtainable from Calendulae flores can be used in tea form for treating gastric and gastroduodenal ulcers. It was reported that the extract contains inter alia alantoin, caffeine acid and polyphenol derivatives, including chlorogenic acid. Chlorogenic acid is said to be a choleretic and cholagogue. A synergism is assumed between the different constituents of the tested extract.
It has now been found that as a pure substance chlorogenic acid has an action which protects the gastric mucosa. This is clearly due to the fact that under the action of chlorogenic acid a surface-protecting film is formed, which protects the gastric mucosa. There is a simultaneous reduction in stimulated gastric acid secretion. These effects are possibly based on an adstringent action of chlorogenic acid.
Chlorogenic acid is able to protect the gastric or duodenal mucosa against aggresive or acid secretion-stimulating foods, beverages and medicaments. As has been gastroscopically observed, immediately after contact with the mucosa the agents of the inventi
REFERENCES:
patent: 4003999 (1977-01-01), Lybrand et al.
Code Kaffee-Handelsges. mbH
Horne Leon R.
Page Thurman K.
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