NO873920L - APPLICATION OF TARGETS AND / OR CHLOROGENIC ACID AND NUTRITIONAL, USEFUL AND / OR MEDICINES WITH DETERGENT AND / OR CHLOROGENIC ACID ADDED. - Google Patents
APPLICATION OF TARGETS AND / OR CHLOROGENIC ACID AND NUTRITIONAL, USEFUL AND / OR MEDICINES WITH DETERGENT AND / OR CHLOROGENIC ACID ADDED.Info
- Publication number
- NO873920L NO873920L NO873920A NO873920A NO873920L NO 873920 L NO873920 L NO 873920L NO 873920 A NO873920 A NO 873920A NO 873920 A NO873920 A NO 873920A NO 873920 L NO873920 L NO 873920L
- Authority
- NO
- Norway
- Prior art keywords
- chlorogenic acid
- gastric
- acid
- nutritional
- gastric mucosa
- Prior art date
Links
- CWVRJTMFETXNAD-JUHZACGLSA-N chlorogenic acid Chemical compound O[C@@H]1[C@H](O)C[C@@](O)(C(O)=O)C[C@H]1OC(=O)\C=C\C1=CC=C(O)C(O)=C1 CWVRJTMFETXNAD-JUHZACGLSA-N 0.000 title claims description 29
- PZIRUHCJZBGLDY-UHFFFAOYSA-N Caffeoylquinic acid Natural products CC(CCC(=O)C(C)C1C(=O)CC2C3CC(O)C4CC(O)CCC4(C)C3CCC12C)C(=O)O PZIRUHCJZBGLDY-UHFFFAOYSA-N 0.000 title claims description 28
- CWVRJTMFETXNAD-FWCWNIRPSA-N 3-O-Caffeoylquinic acid Natural products O[C@H]1[C@@H](O)C[C@@](O)(C(O)=O)C[C@H]1OC(=O)\C=C\C1=CC=C(O)C(O)=C1 CWVRJTMFETXNAD-FWCWNIRPSA-N 0.000 title claims description 27
- CWVRJTMFETXNAD-KLZCAUPSSA-N Neochlorogenin-saeure Natural products O[C@H]1C[C@@](O)(C[C@@H](OC(=O)C=Cc2ccc(O)c(O)c2)[C@@H]1O)C(=O)O CWVRJTMFETXNAD-KLZCAUPSSA-N 0.000 title claims description 27
- 235000001368 chlorogenic acid Nutrition 0.000 title claims description 27
- 229940074393 chlorogenic acid Drugs 0.000 title claims description 27
- FFQSDFBBSXGVKF-KHSQJDLVSA-N chlorogenic acid Natural products O[C@@H]1C[C@](O)(C[C@@H](CC(=O)C=Cc2ccc(O)c(O)c2)[C@@H]1O)C(=O)O FFQSDFBBSXGVKF-KHSQJDLVSA-N 0.000 title claims description 27
- BMRSEYFENKXDIS-KLZCAUPSSA-N cis-3-O-p-coumaroylquinic acid Natural products O[C@H]1C[C@@](O)(C[C@@H](OC(=O)C=Cc2ccc(O)cc2)[C@@H]1O)C(=O)O BMRSEYFENKXDIS-KLZCAUPSSA-N 0.000 title claims description 27
- 239000003814 drug Substances 0.000 title claims description 9
- 235000016709 nutrition Nutrition 0.000 title claims description 7
- 239000003599 detergent Substances 0.000 title 1
- 210000001156 gastric mucosa Anatomy 0.000 claims description 16
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 230000027119 gastric acid secretion Effects 0.000 claims description 10
- 210000002784 stomach Anatomy 0.000 claims description 9
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 6
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 6
- 230000002378 acidificating effect Effects 0.000 claims description 3
- 239000000654 additive Substances 0.000 claims description 3
- 239000003435 antirheumatic agent Substances 0.000 claims description 3
- 239000011248 coating agent Substances 0.000 claims description 3
- 238000000576 coating method Methods 0.000 claims description 3
- 230000002496 gastric effect Effects 0.000 claims description 3
- 229940126601 medicinal product Drugs 0.000 claims description 3
- 230000000996 additive effect Effects 0.000 claims description 2
- 230000003637 steroidlike Effects 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims 3
- 241001122767 Theaceae Species 0.000 claims 1
- 210000004211 gastric acid Anatomy 0.000 claims 1
- 240000007154 Coffea arabica Species 0.000 description 15
- 239000002253 acid Substances 0.000 description 10
- 230000000694 effects Effects 0.000 description 10
- 230000000740 bleeding effect Effects 0.000 description 8
- 208000032843 Hemorrhage Diseases 0.000 description 7
- 210000004051 gastric juice Anatomy 0.000 description 7
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 150000007513 acids Chemical class 0.000 description 5
- 239000013543 active substance Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 206010061164 Gastric mucosal lesion Diseases 0.000 description 3
- 208000025865 Ulcer Diseases 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 239000000284 extract Substances 0.000 description 3
- 230000001681 protective effect Effects 0.000 description 3
- CWVRJTMFETXNAD-GMZLATJGSA-N 5-Caffeoyl quinic acid Natural products O[C@H]1C[C@](O)(C[C@H](OC(=O)C=Cc2ccc(O)c(O)c2)[C@@H]1O)C(=O)O CWVRJTMFETXNAD-GMZLATJGSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical class NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 208000034158 bleeding Diseases 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000000523 sample Substances 0.000 description 2
- 230000028327 secretion Effects 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- QAIPRVGONGVQAS-DUXPYHPUSA-N trans-caffeic acid Chemical class OC(=O)\C=C\C1=CC=C(O)C(O)=C1 QAIPRVGONGVQAS-DUXPYHPUSA-N 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- ACEAELOMUCBPJP-UHFFFAOYSA-N (E)-3,4,5-trihydroxycinnamic acid Chemical class OC(=O)C=CC1=CC(O)=C(O)C(O)=C1 ACEAELOMUCBPJP-UHFFFAOYSA-N 0.000 description 1
- GYFFKZTYYAFCTR-JUHZACGLSA-N 4-O-trans-caffeoylquinic acid Chemical compound O[C@@H]1C[C@](O)(C(O)=O)C[C@@H](O)[C@H]1OC(=O)\C=C\C1=CC=C(O)C(O)=C1 GYFFKZTYYAFCTR-JUHZACGLSA-N 0.000 description 1
- DSHJQVWTBAAJDN-SMKXDYDZSA-N 4-caffeoylquinic acid Natural products CO[C@@]1(C[C@@H](O)[C@H](OC(=O)C=Cc2ccc(O)c(O)c2)[C@H](O)C1)C(=O)O DSHJQVWTBAAJDN-SMKXDYDZSA-N 0.000 description 1
- LTSOENFXCPOCHG-GQCTYLIASA-N 4-chloro-6-[[(e)-3-oxobut-1-enyl]amino]-1-n-prop-2-enylbenzene-1,3-disulfonamide Chemical compound CC(=O)\C=C\NC1=CC(Cl)=C(S(N)(=O)=O)C=C1S(=O)(=O)NCC=C LTSOENFXCPOCHG-GQCTYLIASA-N 0.000 description 1
- GYFFKZTYYAFCTR-UHFFFAOYSA-N 5-O-(6'-O-galloyl)-beta-D-glucopyranosylgentisic acid Natural products OC1CC(O)(C(O)=O)CC(O)C1OC(=O)C=CC1=CC=C(O)C(O)=C1 GYFFKZTYYAFCTR-UHFFFAOYSA-N 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- GYFFKZTYYAFCTR-ZNEHSRBWSA-N Cryptochlorogensaeure Natural products O[C@@H]1C[C@@](O)(C[C@@H](O)[C@@H]1OC(=O)C=Cc2ccc(O)c(O)c2)C(=O)O GYFFKZTYYAFCTR-ZNEHSRBWSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010017788 Gastric haemorrhage Diseases 0.000 description 1
- 241000533293 Sesbania emerus Species 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- 230000009858 acid secretion Effects 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 230000003356 anti-rheumatic effect Effects 0.000 description 1
- 235000004883 caffeic acid Nutrition 0.000 description 1
- 229940074360 caffeic acid Drugs 0.000 description 1
- 239000008845 cholagoga Substances 0.000 description 1
- 229940124571 cholagogue Drugs 0.000 description 1
- 239000000731 choleretic agent Substances 0.000 description 1
- 230000001989 choleretic effect Effects 0.000 description 1
- QAIPRVGONGVQAS-UHFFFAOYSA-N cis-caffeic acid Chemical class OC(=O)C=CC1=CC=C(O)C(O)=C1 QAIPRVGONGVQAS-UHFFFAOYSA-N 0.000 description 1
- 238000012505 colouration Methods 0.000 description 1
- GYFFKZTYYAFCTR-LMRQPLJMSA-N cryptochlorogenic acid Natural products O[C@H]1C[C@@](O)(C[C@H](O)[C@H]1OC(=O)C=Cc2ccc(O)c(O)c2)C(=O)O GYFFKZTYYAFCTR-LMRQPLJMSA-N 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 208000000718 duodenal ulcer Diseases 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- 239000000446 fuel Substances 0.000 description 1
- 229960000905 indomethacin Drugs 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 230000001151 other effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 150000008442 polyphenolic compounds Chemical class 0.000 description 1
- 235000013824 polyphenols Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
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- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000036269 ulceration Effects 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Description
Det er kjent at ulcera duodeni, ulcera ventriculi og andre mageslimhinnelesJoner, som ofte er stress- og/eller medika-mentinduserte, kan føre til livstruende blødninger eller perforeringer. It is known that ulcera duodeni, ulcera ventriculi and other gastric mucosal lesions, which are often stress- and/or medication-induced, can lead to life-threatening bleeding or perforations.
Videre er det kjent at forskjellige nærings-, nytelses- og spesielt legemidler irriterer mageslimhinnen og i høyere konsentrasjoner også angriper denne, slik at det også her kan komme til sårdannelse og blødninger. Nytelsesmidler som irriterer megeslimhinnen er eksempelvis alkohol og sterkt brent kaffe. Irritasjonen beror ofte på en stimulering av magesyresekresjonen. Bestemte legemiddelgrupper, f.eks. ikke-steroidale antireumatika (NSAID) oppviser et definert bivirkningsspektrum, hvorav uønskede gastrointestinale effekter (f.eks. mageslimhinnelesJoner, som kan føre til blødning, hhv. perforering) står i forgrunnen. Følgelig er det observert at acetylsalisylsyre kan føre til mageblød-ninger; det samme gjelder også for de øvrige NSAID, som f.eks. indometacin (se R. Brunn et al., Fortschritte der Medizin 100 (36), 16561 til 168 (1982)). Behandling med acetylsyre og andre legemidler fra gruppen av NSAID er belastet med en definert risiko, slik at før anvendelse av disse medikamentene må deres terapeutiske nytte avveies mot den ledsagende risiko. Furthermore, it is known that various nutritional, recreational and especially pharmaceuticals irritate the gastric mucosa and in higher concentrations also attack it, so that ulcers and bleeding can also occur here. Alcohol and strong coffee are examples of substances that irritate the stomach lining. The irritation is often due to a stimulation of gastric acid secretion. Certain drug groups, e.g. non-steroidal antirheumatic drugs (NSAIDs) exhibit a defined spectrum of side effects, of which undesirable gastrointestinal effects (e.g. gastric mucosal lesions, which can lead to bleeding or perforation) are in the foreground. Consequently, it has been observed that acetylsalicylic acid can lead to stomach bleeding; the same also applies to the other NSAIDs, such as e.g. indomethacin (see R. Brunn et al., Fortschritte der Medizin 100 (36), 16561 to 168 (1982)). Treatment with acetyl acid and other drugs from the group of NSAIDs is burdened with a defined risk, so that before using these drugs, their therapeutic benefit must be weighed against the accompanying risk.
Formålet med foreliggende oppfinnelse er følgelig å tilveie-bringe et middel hvorved mageslimhinnen kan beskyttes mot utvikling av sårdannelse på en slik måte at nærings-, nytelses- og/eller legemidler som er skaldelige for mageslimhinnen kan administreres uten forstyrrende bivirkninger og livstruende blødninger og perforeringer. The purpose of the present invention is therefore to provide a means by which the gastric mucosa can be protected against the development of ulceration in such a way that nutritional, recreational and/or pharmaceuticals which are harmful to the gastric mucosa can be administered without disturbing side effects and life-threatening bleeding and perforations.
Det er funnet at denne oppgaven lar seg løse ved at isolert klorogensyre eller dens fysiologisk tålbare derivater anvendes for reduksjon av magesyresekresjonen og/eller for beskyttelse -av mageslimhinnen. Spesielt tjener de nevnte midlene til beskyttelse av mageslimhinnen overfor nærings-, nytelses- og/eller legemidler som er kjent for å skade mageslimhinnen, hhv. å kunne stimulere magesyresekresjonen. Ifølge oppfinnelsen anvendes klorogensyren før eller samtidig med de nevnte midlene. It has been found that this task can be solved by using isolated chlorogenic acid or its physiologically tolerable derivatives to reduce gastric acid secretion and/or to protect the gastric mucosa. In particular, the aforementioned agents serve to protect the gastric mucosa against food, recreational and/or medicinal products which are known to damage the gastric mucosa, respectively. to be able to stimulate gastric acid secretion. According to the invention, the chlorogenic acid is used before or at the same time as the agents mentioned.
Innenfor rammen av oppfinnelsen forstås under 4ilorogensyre mono- og dikaffeoylkinasyrene samt deres blandinger. Spesielt foretrukne er 3-, 4- og 5-kaffeoylkinasyren, hhv. deres blandinger. Syrene kan anvendes som frie syrer eller i form av fysiologisk tålbare derivater, spesielt salter eller estere. De nevnte derivatene kan finne anvendelse istedenfor de frie syrene, i det syrene settes fri fra disse i sterkt surt magemiljø. Within the scope of the invention, 4ilorogenic acid is understood to mean the mono- and dicaffeoylquinic acids and their mixtures. Particularly preferred are 3-, 4- and 5-caffeoylquinic acid, respectively their mixtures. The acids can be used as free acids or in the form of physiologically tolerable derivatives, especially salts or esters. The aforementioned derivatives can be used instead of the free acids, as the acids are set free from these in a strongly acidic stomach environment.
Klorogensyre er en forbindelse som forekommer i tallrike planter, eksempelvis i grønne kaffebønner, og som ble isolert i 1920 av Freudenberg, forbindelsens struktur er oppklart og den er senere også syntetisert (se Merck Index, 10. opplag, nr. 2112). Fra en publikasjon av V. Istudor et al., Farmacia 29, 41 til 48 (1981) er det kjent at ekstrakt som kan oppnås fra Calendulae flores kan finne anvendelse som magete for behandling av mage- og tolvfIngertarmssår. Det rapporteres at ekstraktet bl.a. inneholder alantoin, kaffeinsyre og polyfenolderivater, derunder klorogensyre. Om klorogensyren sies det at den er et koleretikum eller kolagogum. Det formodes en synergisme mellom de forskjellige bestanddelene av det undersøkte ekstraktet. Chlorogenic acid is a compound that occurs in numerous plants, for example in green coffee beans, and which was isolated in 1920 by Freudenberg, the compound's structure was clarified and it 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 extract obtainable from Calendulae flores can find application as a stomachic for the treatment of gastric and duodenal ulcers. It is reported that the extract i.a. contains allantoin, caffeic acid and polyphenol derivatives, including chlorogenic acid. Chlorogenic acid is said to be a choleretic or cholagogue. A synergism between the different components of the investigated extract is presumed.
I monografien "Kaffee" av Hans Gerhard Maier, Berlin og Hamburg 1981, side 80, angis under avsnittet: Oversikt over tidligere undersøkelser viser at klorogensyre bevirker en sekresjonsøkning i magen. In the monograph "Kaffee" by Hans Gerhard Maier, Berlin and Hamburg 1981, page 80, it is stated under the section: Overview of previous research shows that chlorogenic acid causes an increase in secretion in the stomach.
Det er imidlertid nå overraskende funnet at klorogensyre som rent stoff oppviser en beskyttende virkning på mageslimhinnen. Dette skyldes åpenbart at det under innvirkning av klorogensyre dannes en beskyttelsesfirlm på overflaten som beskytter mageslimhinnen. Samtidig avtar den stimulerte magesyresekresjonen. Muligens skyldes disse virkningene en astringerende,hhv. garvende, virkning av klorogensyre, tilsvarende som for garvestoffene. However, it has now surprisingly been found that chlorogenic acid as a pure substance exhibits a protective effect on the gastric mucosa. This is obviously due to the fact that, under the influence of chlorogenic acid, a protective film is formed on the surface which protects the stomach lining. At the same time, the stimulated gastric acid secretion decreases. Possibly these effects are due to an astringent, or tanning, effect of chlorogenic acid, similar to that of the tanning substances.
Klorogensyre er følgelig i stand til å beskytte mageslimhinnen mot aggresive, hhv. syresekresjonsstimulerende nærings-, nytelses- og legemidler. Som det kunne observeres gastroskopisk danner midlene ifølge oppfinnelsen umiddelbart etter kontakt med slimhinnen en hvit- og nettaktig besjiktning som virker som en beskyttelsesfilm. Ved tilførsel av 10% alkohol som irritasjonsmiddel viser det seg i området som er beskyttet på denne måten ingen forandring, mens den ubehandlede mageslimhinnen oppviser en patologisk rødfarging. Liknende forsøk med acetylsalisylsyre gir også en virksom beskyttelse av mageslimhinnen ved samtidig forhindring av de fryktede blødningene som ellers ofte opptrer ved tilførsel av acetylsalisylsyre og de øvrige NSAID alene. Chlorogenic acid is therefore able to protect the gastric mucosa against aggressive, resp. acid secretion-stimulating nutritional, recreational and medicinal products. As could be observed gastroscopically, the agents according to the invention form immediately after contact with the mucous membrane a white and net-like coating which acts as a protective film. When 10% alcohol is applied as an irritant, the area protected in this way shows no change, while the untreated gastric mucosa shows a pathological red colouration. Similar trials with acetylsalicylic acid also provide effective protection of the gastric mucosa by simultaneously preventing the dreaded bleeding that otherwise often occurs when acetylsalicylic acid and the other NSAIDs are administered alone.
For anvendelse ifølge oppfinnelsen prepareres garvestoffene, hhv. klorogensyren, fortrinnsvis på en slik måte at en frigivelse først foregår i magen. Dette kan foregå på i og for seg kjent måte, ved at man ved fremstillingen av tab-letter anvender en besjiktning som først løses opp i surt magemiljø. Administreringen av midlet kan enten foregå før eller fortrinnsvis samtidig med administreringen det midlet mot hvilket mageslimhinnen skal beskyttes. Hva angår nærings- eller nytelsesmidler dreier det seg om midler som i utgangspunktet praktisk talt ikke inneholder klorogensyre, hhv. bare en liten mengde av dette, men som ved tilsats ifølge oppfinnelsen kan overføres til en magevennligere form. For use according to the invention, the tanning substances are prepared, respectively the chlorogenic acid, preferably in such a way that a release first takes place in the stomach. This can take place in a manner known in and of itself, by using a coating which is first dissolved in an acidic stomach environment during the production of tablets. The administration of the agent can either take place before or preferably at the same time as the administration of the agent against which the gastric mucosa is to be protected. With regard to nutritional or recreational products, these are products which basically practically do not contain chlorogenic acid, or only a small amount of this, but which by addition according to the invention can be transferred to a more stomach-friendly form.
Spesiell betydning har oppfinnelsen i forbindelse med legemiddel-virkestoffer som skader mageslimhinnen i en lsik grad at sår eller blødninger kan oppstå. Et spesielt problem utgjør i denne forbindelse acetylsalisylsyre og de øvrige NSAID, som av mange pasienter må inntas regelmessig som analetikum, hhv. antireumatikum, og som da kan føre tild e omtalte bivirkningene i magekanalen. Ved anvendelse av et kombinasjonspreparat av acetylsalisylsyre eller de andre NSAID med garvestoffer og/eller klorogensyre i en admini-streringsform som setter de virksomme stoffene fri i magesaften kan mageslimhinnen virksomt beskyttes med: det resul-tatet at ingen mageslimhinnelesjoner hhv. blødninger lenger observeres. The invention has special significance in connection with pharmaceutical active substances which damage the gastric mucosa to such an extent that ulcers or bleeding can occur. A particular problem in this connection is acetylsalicylic acid and the other NSAIDs, which many patients must take regularly as analgesia, or antirheumatic, and which can then lead to the mentioned side effects in the stomach tract. When using a combination preparation of acetylsalicylic acid or the other NSAIDs with tanning agents and/or chlorogenic acid in an administration form that releases the active substances into the gastric juice, the gastric mucosa can be effectively protected with: the result that no gastric mucosal lesions or bleeding longer is observed.
Ved en spesielt gunstig administreingsform, f.eks. i form av en kjerne/skall-tablett med det virksomme stoffet som kjerne og klorogensyren i det ytre skallet, frigis først klorogensyren og deretter det virksomme stoffet. In the case of a particularly favorable form of administration, e.g. in the form of a core/shell tablet with the active substance as the core and the chlorogenic acid in the outer shell, the chlorogenic acid is released first and then the active substance.
I for høy dosering kan klorogensyren ha uønskede bivirkninger, spesielt fremkalle fordøyelsesforstyrrelser med brekninger og betennelsesti 1 stander. Det er følgelig nødvendig å velge doseringen så lav at slike symptomer ikke opptrer. Tilsatsen ifølge oppfinnelsen fører til den ønskede virkningen uten at slike uønskede bivirkninger opptrer. In too high a dosage, the chlorogenic acid can have unwanted side effects, in particular causing digestive disorders with vomiting and inflammatory conditions. It is therefore necessary to choose the dosage so low that such symptoms do not occur. The additive according to the invention leads to the desired effect without such unwanted side effects occurring.
De etterfølgende sammenligningseksemplene skal tjene til en ytterligere beskrivelse av oppfinnelsen, i disse ble kaffe anvendt som en modell for nytelsesmiddel som stimulerer magesyresekresjonen og irriterer mageslimhinnen. Kaffeprøve nr. 1 oppviste bare det tilstedeværende restinnholdet av klorogensyre som finnes i brent kaffe etter brenningen, mens de øvrige kaffesortene ifølge oppfinnelsen fikk en tilsats av klorogensyre. The subsequent comparative examples shall serve for a further description of the invention, in which coffee was used as a model for a stimulant that stimulates gastric acid secretion and irritates the gastric mucosa. Coffee sample No. 1 only showed the present residual content of chlorogenic acid which is found in roasted coffee after roasting, while the other types of coffee according to the invention had an addition of chlorogenic acid.
Fysiologiske forsøkPhysiological experiments
I en forsøksrekke ble innvirkningen av kaffeprøvene 1 til 5 på den menneskelige magesyresekresjonen undersøkt. Prøvene adskilte seg fra hverandre bare i klorogensyreinnhold som angitt i tabell 1. Hver forsøksperson fikk ca. 250 ml av de forskjellige kaffesortene randomisert i dobbeltblind-"crossover"-anordning. Forsøkspersonene var sunne personer av hannkjønn og hunkjønn i alder mellom 19 og 35 år. Etter en 12 timers fasteperiode hie det om morgenen lagt inn ennaso-gastrlsonde hos forøkspersonene, ved hjelp av denne ble det først tatt ut magesaft kvantitativt ved tidspunktet tø. I de følgende 60 minuttene tq_^q hie det for bestemmelse av den basale syresekresjonen tatt ut nydannet magesaft med intervaller på 15 minutter. På 5 forskjellige undersøkelses-dager, som lå minst 2 dager fra hverandre, fikk forsøks-personene 250 ml av kaffeprøvene 1 til 5. Før forsøks-personene inntok de forskjelige kaffeprøvene i løpet av 10 minutter foregikk først tilbakeføringen av den ved tidspunkt 0 uttatte magesaften. I det 10. og 30. minuttet etter begynnelsen av kaffedrikkingen ble det ved hjelp av sonden tatt ut 5 ml magesaft. Mellom det 30. og 150. minuttet ble det så Igjen med intervaller på 15 minutter foretatt en kvantitativ uttakning av magesaften. I disse prøvene ble den titrerbare syren bestemt ved 0,ln NaOH, i tabell 2 er de fundne verdiene angitt i ml NaOH. Volumene av den uttatte magesaften er angitt i tabell 2 i ml. In a series of experiments, the effect of coffee samples 1 to 5 on human gastric acid secretion was investigated. The samples differed from each other only in chlorogenic acid content as indicated in Table 1. Each subject received approx. 250 ml of the different types of coffee randomized in a double-blind "crossover" arrangement. The subjects were healthy male and female subjects aged between 19 and 35 years. After a 12-hour fasting period, a naso-gastric tube was inserted in the subjects in the morning, with the help of which gastric juice was first extracted quantitatively at the time of thawing. In the following 60 minutes, for the determination of the basal acid secretion, freshly formed gastric juice was taken at intervals of 15 minutes. On 5 different examination days, which were at least 2 days apart, the subjects received 250 ml of coffee samples 1 to 5. Before the subjects consumed the various coffee samples within 10 minutes, the return of the gastric juice taken at time 0 first took place . In the 10th and 30th minutes after the start of coffee drinking, 5 ml of gastric juice was taken out using the probe. Between the 30th and 150th minute, a quantitative extraction of the gastric juice was then again carried out at intervals of 15 minutes. In these samples, the titratable acid was determined with 0.ln NaOH, in table 2 the values found are given in ml NaOH. The volumes of the withdrawn gastric juice are given in table 2 in ml.
For den sammenlignende vurderingen av resultatene ble perioden t(jQ_150 anvendt, i det det er kjent at de første 60 minuttene etter næringsinntak er overlagret med forskjellige andre effekter. De fundne verdiene ble oppnådd ved intra-individuell vurdering, hvorved spredningen for middelverdien kan beregnes ved hjelp av følgende ligning: For the comparative assessment of the results, the period t(jQ_150) was used, as it is known that the first 60 minutes after food intake are superimposed with various other effects. The values found were obtained by intra-individual assessment, whereby the spread for the mean value can be calculated by using the following equation:
Kaffeprøvene nr. 1 til 5 oppviste en identisk brenningsgrad, men inneholdt økende mengde klorogensyre. Som de oppnådde resultatene i tabell 2 viser fører kaffe 1 til til den høyeste syrestimuleringen, med økende klorogensyreinnhold avtar magesyresekresjonen signifikant. Også volumsekresjonen avtar i rekkefølgen for kaffesortene 1 til 5. Innvirkningen av klorogensyre på reduseringen av den ved kaffe-brennstoffer stimulerte menneskelige magesyresekresjonen er åpenbar. Coffee samples no. 1 to 5 showed an identical degree of roasting, but contained an increasing amount of chlorogenic acid. As the obtained results in table 2 show, coffee 1 leads to the highest acid stimulation, with increasing chlorogenic acid content, gastric acid secretion decreases significantly. Also, the volume secretion decreases in the order for coffee varieties 1 to 5. The effect of chlorogenic acid on the reduction of the coffee fuel-stimulated human gastric acid secretion is obvious.
Claims (8)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19863603576 DE3603576A1 (en) | 1986-02-06 | 1986-02-06 | USE OF TANNING SUBSTANCES AND / OR CHLOROIC ACID AND FOOD, ENJOYMENT AND / OR MEDICINAL PRODUCTS WITH ADDITIVES OF TANNING AGENT AND / OR CHLOROGENIC ACID |
| PCT/EP1987/000052 WO1987004619A1 (en) | 1986-02-06 | 1987-02-03 | Use of tannin agents and/or chlorogenic acid, foodstuffs, stimulants and/or medicines with the addition of tannin agents and/or chlorogenic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO873920D0 NO873920D0 (en) | 1987-09-18 |
| NO873920L true NO873920L (en) | 1987-09-18 |
Family
ID=25840729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO873920A NO873920L (en) | 1986-02-06 | 1987-09-18 | APPLICATION OF TARGETS AND / OR CHLOROGENIC ACID AND NUTRITIONAL, USEFUL AND / OR MEDICINES WITH DETERGENT AND / OR CHLOROGENIC ACID ADDED. |
Country Status (1)
| Country | Link |
|---|---|
| NO (1) | NO873920L (en) |
-
1987
- 1987-09-18 NO NO873920A patent/NO873920L/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO873920D0 (en) | 1987-09-18 |
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