Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/60—Salicylic acid; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23F—COFFEE; TEA; THEIR SUBSTITUTES; MANUFACTURE, PREPARATION, OR INFUSION THEREOF
  • A23F5/00—Coffee; Coffee substitutes; Preparations thereof
  • A23F5/10—Treating roasted coffee; Preparations produced thereby
  • A23F5/14—Treating roasted coffee; Preparations produced thereby using additives, e.g. milk, sugar; Coating, e.g. for preserving
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
  • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
  • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
  • C07H13/08—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings

Definitions

• Tannin or catechin-based tannin agents and / or isolated chlorogenic acid or their physiologically compatible deriv tives have the effect, when used before or during the absorption of foodstuffs, stimulants and / or medicines which activ the secretion of gastric acid and / or irritate or attack the gastric mucous membrane, of reducing the secretion of gastric ac and / or of protecting the gastric mucous membrane.
• Tannins based on tannin or catechin and / or isolated chlorogenic acid or their physiologically tolerable derivatives lead, when used, before or at the same time as the administration of food, food and / or / which stimulates gastric acid secretion and / or irritates or attacks the gastric mucosa. or medicines to reduce gastric acid secretion and / or to protect the gastric mucosa.
• tannins and / or chlorogenic acid as well as food, luxury foods and / or medicinal products with added tannins and / or chlorogenic acid
• duodenal ulcer, ventricular ulcer and other gastric mucosal lesions which are often stress and / or medication-induced, can bleed or perforate in a life-threatening manner.
• Non-steroidal anti-inflammatory drugs NSAIDs
• NSAIDs Non-steroidal anti-inflammatory drugs
• acetylsalicylic acid can lead to gastric bleeding; the same applies to the other NSAIDs, e.g. Indomethacin (see R. Bruhn et al., Progress in Medicine 100 (36), 1661 to 168 (1982)).
• Therapy with acetylsalicylic acid and other drugs from the NSAID group carries a defined risk, so that before using these drugs, their therapeutic benefits must be weighed against the accompanying risk.
• the invention is therefore based on the object of finding a means by which the gastric mucosa can be protected against the development of ulcerations in such a way that food, luxury foods and / or medications that damage the gastric mucosa can be administered without disturbing side effects up to life-threatening bleeding and perforations.
• tannins based on tannins or catechins or agents based on isolated chlorogenic acid or their physiologically tolerable derivatives are suitable for protecting the gastric mucosa against food, luxury foods and / or drugs who are known to damage the gastric and duodenal mucosa or to stimulate gastric acid secretion.
• the tannins or the chlorogenic acid are applied before or simultaneously with the administration of the agents mentioned.
• chlorogenic acid means the mono- and dicaffeoylquinic acids and mixtures thereof.
• the 3-, 4- and 5-caffeoylquinic acids or their mixture, in particular the 3-caffeoylquinic acid, are particularly preferred.
• the acids can be used as free acid or in the form of their physiologically compatible derivatives, in particular salts or esters.
• the alkali salts, especially the potassium salts, are particularly suitable.
• the derivatives mentioned can be used instead of the free acid, since the acid is released from them in the strongly acidic gastric environment.
• Chlorogenic acid is a compound found in numerous plants, for example in green coffee beans, which was isolated by Freudenberg in 1920, the structure of which has been elucidated, and which was later also synthesized (see Merck Index, 10th edition, No. 2112). From a publication by V. Istudor et al., Farmacia 29, 41 to 48 (1981) it is known that a from Calendulae
• Flores available extract can be used as stomach tea for the treatment of gastric and duodenal ulcers. It is reported that the extract includes Contains alantoin, caffeinic acid and polyphenol derivatives, including chlorogenic acid. Chlorogenic acid is said to be a choleretic and cholagogue. A synergism between the different components of the examined extract is suspected.
• chlorogenic acid as a pure substance has a protective effect on the gastric mucosa. This is apparently due to the fact that under the action of chlorogenic acid a superficial protective film is formed which protects the gastric mucosa. At the same time, the stimulated gastric acid secretion decreases. These effects may be due to an astringent or tanning effect of chlorogenic acid, similar to that of tanning agents.
• the hydrolyzable ester-like tannins and / or their derivatives are particularly preferred as tanning agents.
• These tannins are esters of sugars, especially glucose, with various hydroxybenzoic acids, especially 3, 4, 5-trihydroxybenzoic acid (gallic acid).
• the non-ester-like, condensed tannins which are primarily compounds from the group of catechins, such as those found in tea, can also be used.
• the various tannins are commercially available; as a rule, these are mixtures of compounds which are obtained from natural raw materials.
• the tannins are known to have an astringent and hemostatic effect. They are used externally as hemostatic agents and for the treatment of local burns (sunburn). It is also known to use tannins Treatment of diarrhea, ie to use catarrhal diseases of the intestinal tract. For this purpose, tannins for complexes with protein (tannin albumin) are used in order to ensure that the tannin is only released in the intestine, that is, it is not yet effective in the stomach.
• tannins for complexes with protein tannins for complexes with protein (tannin albumin) are used in order to ensure that the tannin is only released in the intestine, that is, it is not yet effective in the stomach.
• tannins or chlorogenic acid are able to protect the gastric or duodenal mucosa from aggressive foodstuffs, foods and medicines which stimulate acid secretion.
• the agents according to the invention form a whitish, net-like coating immediately after contact with the mucous membrane, which acts like a protective film.
• 10% alcohol is applied as an irritant, there is no change in the area protected in this way, while the untreated gastric mucosa shows pathological reddening.
• the tannins or the chlorogenic acid are preferably prepared in such a way that they are released only in the stomach. This can be done in a manner known per se by using a coating in the manufacture of tablets which only dissolves in the acidic gastric environment.
• the agents can be administered either before or preferably at the same time as the agents against which the gastric mucosa is to be protected. As far as it concerns foodstuffs or stimulants, it concerns those which contain practically no tannins or chlorogenic acid or an insufficient amount thereof, but which are converted into a more stomach-friendly form by the addition according to the invention can be.
• the invention is of particular importance in connection with active pharmaceutical ingredients which damage the gastric mucosa in such a way that ulcers or bleeding can occur.
• a particular problem in this regard is acetylsalicylic acid and the other NSAIDs, which many patients take regularly as an analgesic or anti-rheumatic and can then lead to the side effects described in the gastrointestinal tract.
• acetylsalicylic acid or the other NSAID with tannins and / or chlorogenic acid in a dosage form that releases the active substances in the gastric juice, the gastric mucosa can be effectively protected, with the result that gastric mucosal lesions or bleeding are no longer observed.
• the combination preparations according to the invention are preferably administered to fasting patients in order to prevent the added tannins from being rendered ineffective by reaction with proteins from the diet.
• a particularly favorable dosage form e.g. in the form of a core / shell tablet with the active substance as the core and the protective substances (tannins and / or chlorogenic acid) in the outer shell
• first the tannin or chlorogenic acid and then the active substance are released.
• the test subjects received 250 ml of coffee samples 1 to 5.
• the gastric juice extracted at time 0 was returned.
• 5 ml gastric juice were siphoned off.
• the gastric juice was then quantitatively removed at intervals of 15 minutes.
• the titratable acid determined with 0.1N NaOH, in Table 2 the values found are given in ml NaOH.
• the volume of gastric juice extracted is given in Table 2 in ml.
• the period t 60-150 was used for the comparative evaluation of the results, since it is known that the first 60 minutes after eating are overlaid by various other effects.
• Coffee samples Nos. 1 to 5 had an identical degree of roasting, but contained increasing amounts of chlorogenic acid. As the results shown in Table 2 show, coffee 1 leads to the highest acid stimulation, with increasing chlorogenic acid content the gastric acid secretion decreases significantly. Volume secretion also decreases in the order of coffee types 1 to 5. The influence of chlorogenic acid on the reduction of human gastric acid secretion stimulated by coffee roasting agents is obvious.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Medicinal Chemistry (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Pharmacology & Pharmacy (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Biotechnology (AREA)
• Molecular Biology (AREA)
• Genetics & Genomics (AREA)
• Biochemistry (AREA)
• Food Science & Technology (AREA)
• Polymers & Plastics (AREA)
• Emergency Medicine (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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• 1986
  • 1986-02-06 DE DE19863603576 patent/DE3603576A1/de not_active Withdrawn
• 1987
  • 1987-02-03 US US07/123,854 patent/US4865847A/en not_active Expired - Lifetime
  • 1987-02-03 JP JP62501519A patent/JPS63502349A/ja active Pending
  • 1987-02-03 EP EP87901423A patent/EP0258339A1/de not_active Withdrawn
  • 1987-02-03 WO PCT/EP1987/000052 patent/WO1987004619A1/de not_active Application Discontinuation
  • 1987-10-05 FI FI874361A patent/FI874361A/fi not_active IP Right Cessation
  • 1987-10-06 DK DK524087A patent/DK524087A/da not_active Application Discontinuation

Non-Patent Citations (1)

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