NO761101L - - Google Patents
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- Publication number
- NO761101L NO761101L NO761101A NO761101A NO761101L NO 761101 L NO761101 L NO 761101L NO 761101 A NO761101 A NO 761101A NO 761101 A NO761101 A NO 761101A NO 761101 L NO761101 L NO 761101L
- Authority
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- Norway
- Prior art keywords
- preparation
- preparation according
- carrier component
- colon
- salts
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 claims abstract description 21
- 210000001072 colon Anatomy 0.000 claims abstract description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 239000000126 substance Substances 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 9
- 229920002125 Sokalan® Polymers 0.000 claims description 8
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 230000008961 swelling Effects 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- 239000001913 cellulose Substances 0.000 claims description 6
- 235000010980 cellulose Nutrition 0.000 claims description 6
- 229920002678 cellulose Polymers 0.000 claims description 6
- 239000008187 granular material Substances 0.000 claims description 6
- 239000004584 polyacrylic acid Substances 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 5
- 239000000463 material Substances 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 238000010521 absorption reaction Methods 0.000 claims description 4
- 235000010410 calcium alginate Nutrition 0.000 claims description 4
- 239000000648 calcium alginate Substances 0.000 claims description 4
- 229960002681 calcium alginate Drugs 0.000 claims description 4
- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 claims description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 229920000642 polymer Polymers 0.000 claims description 4
- 244000215068 Acacia senegal Species 0.000 claims description 3
- 229920000084 Gum arabic Polymers 0.000 claims description 3
- 229920000148 Polycarbophil calcium Polymers 0.000 claims description 3
- 235000010489 acacia gum Nutrition 0.000 claims description 3
- 239000000205 acacia gum Substances 0.000 claims description 3
- 229950005134 polycarbophil Drugs 0.000 claims description 3
- 244000106483 Anogeissus latifolia Species 0.000 claims description 2
- 235000011514 Anogeissus latifolia Nutrition 0.000 claims description 2
- 239000001922 Gum ghatti Substances 0.000 claims description 2
- 235000019314 gum ghatti Nutrition 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 2
- 239000006096 absorbing agent Substances 0.000 claims 1
- 239000003960 organic solvent Substances 0.000 claims 1
- 235000002639 sodium chloride Nutrition 0.000 claims 1
- 206010013554 Diverticulum Diseases 0.000 description 9
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 6
- 210000001035 gastrointestinal tract Anatomy 0.000 description 5
- 206010013530 Diverticula Diseases 0.000 description 4
- 208000012258 Diverticular disease Diseases 0.000 description 4
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 4
- 230000000968 intestinal effect Effects 0.000 description 4
- 210000000936 intestine Anatomy 0.000 description 4
- 210000002429 large intestine Anatomy 0.000 description 4
- 210000002784 stomach Anatomy 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 3
- 210000003608 fece Anatomy 0.000 description 3
- -1 fibres Polymers 0.000 description 3
- 210000004051 gastric juice Anatomy 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 230000037023 motor activity Effects 0.000 description 3
- 230000001148 spastic effect Effects 0.000 description 3
- 235000015099 wheat brans Nutrition 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- 206010010774 Constipation Diseases 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 235000010451 Plantago psyllium Nutrition 0.000 description 2
- 244000090599 Plantago psyllium Species 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 208000007784 diverticulitis Diseases 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 230000008092 positive effect Effects 0.000 description 2
- 206010000060 Abdominal distension Diseases 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 229920000569 Gum karaya Polymers 0.000 description 1
- 229920002488 Hemicellulose Polymers 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 230000001142 anti-diarrhea Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000004067 bulking agent Substances 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 235000006694 eating habits Nutrition 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 230000003325 follicular Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 150000002314 glycerols Chemical class 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 230000002048 spasmolytic effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
-
- 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
- A61K31/74—Synthetic polymeric materials
- A61K31/765—Polymers containing oxygen
- A61K31/78—Polymers containing oxygen of acrylic acid or derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Preparat for kolon.Preparation for colon.
Description
Oppfinnelsen vedrører et preparat beregnet forThe invention relates to a preparation intended for
kolon omfattende en komponent av stiv, makromorfologisk struktur, hvilket preparat er beregnet for behandling av kolon irritabile. colon comprising a component of rigid, macromorphological structure, which preparation is intended for the treatment of irritable bowel syndrome.
Hensikten med oppfinnelsen er å tilveiebringe et preparat for kolon for behandling av kolon irritabile, spesielt The purpose of the invention is to provide a preparation for the colon for the treatment of irritable bowel syndrome, in particular
for å behandle eller hindre utviklingen av divertikler i tykktarmen, (dvs. små follikylære rupturer i veggen av tykktarmen. to treat or prevent the development of diverticula in the colon, (ie small follicular ruptures in the wall of the colon.
Divertikler i tykktarmen blir lett irritert, hvor-ved det oppstår diverticulitis, som gir meget smertefulle tilstander som bare i mange tilfeller kan elimineres ved eliminer-ing av den betente del av tykktarmen. Diverticula in the large intestine are easily irritated, whereupon diverticulitis occurs, which causes very painful conditions that can only be eliminated in many cases by eliminating the inflamed part of the large intestine.
Kolon irritabile er en sykdom som er spesiell for den tilfeldige sivilisasjon. En spastisk tilstand med øket motorisk aktivitet i tykktarmen hører til det patologiske bilde. Dette fører til et øket intraluminalt trykk i kolon som fører Irritable colon is a disease that is peculiar to the casual civilization. A spastic condition with increased motor activity in the colon belongs to the pathological picture. This leads to an increased intraluminal pressure in the leading colon
til dannelse av divertikler, såkalte diverticulosis, med mulighet for en etterfølgende infeksjon, såkalt diverticulitis, som nevnt ovenfor. Dannelsen av divertikler er vanlig og er rapportert å opptre til 56% i en befolkning som har en gjennomsnittsalder på 70 år. Symptomene av kolon irritabile varierer, Det mest vanlige er forandringer i avf^ringsstrukturen, idet både obstipasjon og diare kan opptre i kombinasjon med utvidelse og gass-dannelse. Kolon irritabile er den mest vanlige gastroenterolo-giske sykdom. Den er 2 - 5 ganger så vanlig som mavesår blant pasienter pa en indremedisinsk klinikk. to the formation of diverticula, so-called diverticulosis, with the possibility of a subsequent infection, so-called diverticulitis, as mentioned above. The formation of diverticula is common and is reported to occur in 56% of a population whose average age is 70 years. The symptoms of irritable bowel syndrome vary, the most common being changes in the stool structure, as both constipation and diarrhea can occur in combination with distention and gas formation. Irritable bowel syndrome is the most common gastroenterological disease. It is 2 - 5 times as common as stomach ulcers among patients at an internal medicine clinic.
Enskjønt mekanismen av genesen er kompleks og u-kjent til en viss grad er det et vanlig godtatt faktum at den vanligvis mest alminnelige og altså mest viktige faktor for genesen av divertikularsykdommen er næringsmidler som er for fattige i oppfyllende material. Derved blir mengden feces mindre og tiden for å passere gjennom fordøyelseskanalen er lenger, som igjen fører til spastisk tilstand med øket motorisk aktivitet i tykktarmen. Although the mechanism of the genesis is complex and unknown to a certain extent, it is a commonly accepted fact that the usually most common and thus most important factor for the genesis of diverticular disease is food that is too poor in fulfilling material. Thereby, the amount of faeces is reduced and the time to pass through the digestive tract is longer, which in turn leads to a spastic state with increased motor activity in the large intestine.
Behandlingen har tidligere vært å forandre mat-vaner, dvs. å innta næringsmidler som er mere like i oppfyllende material i kombinasjon med terapeutiske stoffer som antidiare-stoffer, spasmolytiske og antikolinergiske stoffer. Behandlings-typen er imidlertid vanskelig å utføre og har vist seg ikke å være effektiv nok. The treatment has previously been to change eating habits, i.e. to consume foods that are more similar in fulfilling material in combination with therapeutic substances such as antidiarrheal substances, spasmolytic and anticholinergic substances. However, this type of treatment is difficult to perform and has not been shown to be effective enough.
I den senere tid har det fremkommet resultater som viser at hvetekli har en positiv effekt på den divertikulære sykdom. Mengden av feces og passeringstiden gjennom fordøyelses-kanalen øker etter en dose på ca. 20 g kli pr, dag. Videre reduseres det intraluminale trykk i kolon. Den positive effekt av kli skyldes sannsynligvis vannbindingsevnen av klifibrene. Denne kapasitet er avhengig av den omgivende pH. Recently, results have emerged showing that wheat bran has a positive effect on diverticular disease. The amount of faeces and the passage time through the digestive tract increase after a dose of approx. 20 g of bran per day. Furthermore, the intraluminal pressure in the colon is reduced. The positive effect of bran is probably due to the water-binding capacity of the bran fibres. This capacity is dependent on the surrounding pH.
Ulempen ved kli er imidlertid vanskeligheter i å administrere den store mengde kli som er nødvendig for å oppnå en effektiv behandling. Dette skyldes det faktum at kli er vanskelig å håndtere og små mengder herav er ikke effektiv nok til å endre den spastiske tilstand som er tilstede i kolon ved kolon irritabile. Mengden av nødvendig kli er også funnet å være irriterende å svelge, avhengig av en følelse av opphopning av maven den den umiddelbare svelging av den administrerte kli-mengde. However, the disadvantage of bran is difficulty in administering the large amount of bran required to achieve an effective treatment. This is due to the fact that bran is difficult to handle and small amounts of it are not effective enough to change the spastic condition present in the colon in irritable bowel syndrome. The amount of bran required is also found to be irritating to swallow, depending on a feeling of engorgement of the stomach on the immediate swallowing of the administered amount of bran.
Pasienten finner samme problemer også i å benytte andre typer av oppfyllingsdannende stoffer som sterhulia gummi, psyllium-frø og cellulosederivater. The patient also finds the same problems in using other types of fillers such as sterhulia gum, psyllium seeds and cellulose derivatives.
Det idielle middel for å behandle divertikulær-sykdom skulle således være et stoff som ikke absorberes eller nedbrytes i fordøyelseskanalen og som absorberer vann og sveller til et vesentlig større volum i tarmen, spesielt i tykktarmen enn i maven. Videre bør et slikt stoff være i en form så det lett administreres uten å føre til ubehag. The ideal agent for treating diverticular disease should thus be a substance which is not absorbed or broken down in the digestive tract and which absorbs water and swells to a significantly larger volume in the intestine, especially in the large intestine than in the stomach. Furthermore, such a substance should be in a form so that it is easily administered without causing discomfort.
Prepar-atet ifølge oppfinnelsen oppfyller overraskende disse krav og preparatet erkarakterisert vedat stoffet ved siden av nevnte komponent omfatter en forbindelse som har en vannabsorberingsevne under svelling ved pH over 4, idet svellemidlet er valgt blant karboksylpolymere. Ifølge en foretrukken utførelse av oppfinnelsen er midletkarakterisert vedat svelle-forbindelsen sveller ved pH over 5. The preparation according to the invention surprisingly fulfills these requirements and the preparation is characterized in that the substance next to said component comprises a compound which has a water absorption capacity during swelling at a pH above 4, the swelling agent being chosen from among carboxyl polymers. According to a preferred embodiment of the invention, the agent is characterized in that the swelling compound swells at a pH above 5.
I henhold til en annen foretrukket utførelsesform av oppfinnelsen er midletkarakterisert vedat bærekomponenten er et fibrøst cellulosematerial. According to another preferred embodiment of the invention, the agent is characterized in that the carrier component is a fibrous cellulose material.
Ifølge et ytterligere trekk ved oppfinnelsen er midletkarakterisert vedat det består av kli .og polyakrylsyre. According to a further feature of the invention, the agent is characterized by the fact that it consists of bran and polyacrylic acid.
Ifølge en ytterligere foretrukket utførelsesformAccording to a further preferred embodiment
av oppfinnelsen er midletkarakterisert vedat det videre omfatter et bindemiddel og et lipofilt stoff. of the invention, the agent is characterized in that it further comprises a binder and a lipophilic substance.
Oppfinnelsen vedrører også en fremgangsmåte for fremstilling av midlet ifølge oppfinnelsen. Midlet ifølge oppfinnelsen omfatter således en bærende vannabsorberende svellende komponent som er inert overfor prosesser i fordøyelses-kanalen og en forbindelse som sveller ubetydelig i mavens sure pH, men øker betraktelig i volum når det når tarmen. Forholdet mellom komponentene kan variere, men ligger fortrinnsvis i om-rådet på 98 : 2 til 20 : 80. Ved å binde disse sammen idet det benyttes et egnet bindemiddel oppnås lett håndterlig og lett administrerbar form. The invention also relates to a method for producing the agent according to the invention. The agent according to the invention thus comprises a carrying water-absorbing swelling component which is inert to processes in the digestive tract and a compound which swells insignificantly in the acidic pH of the stomach, but increases considerably in volume when it reaches the intestine. The ratio between the components can vary, but is preferably in the range of 98:2 to 20:80. By binding these together using a suitable binder, an easily manageable and easily administrable form is achieved.
Den daglige dose, som er effektiv i behandling av divertikular sykdom, er 2 - 10 g, som er betraktelig lavere enn det som er nødvendig ved å benytte vanlige svellemidler. The daily dose, which is effective in the treatment of diverticular disease, is 2 - 10 g, which is considerably lower than that required by using common bulking agents.
Bærekomponenten har en stiv, makromorfologisk struktur og virker ved siden av sin egen vannabsorberende evne, som en bærer for den annen forbindelse. Prinsippielt kan alle forbindelser som tilfredsstiller dette krav benyttes som en bærekomponent. Fortrinnsvis benyttes polysakkarider av typen cellulose og hemicellulose, som kli av forskjellige korntyper, andre typer av cellulose, fibre, mikrokrystallinsk cellulose ("Avicel")>psyllium-frø eller deler herav. The carrier component has a rigid, macromorphological structure and, in addition to its own water-absorbing capacity, acts as a carrier for the other compound. In principle, all compounds that satisfy this requirement can be used as a carrier component. Polysaccharides of the type cellulose and hemicellulose are preferably used, such as bran of various grain types, other types of cellulose, fibres, microcrystalline cellulose ("Avicel") > psyllium seeds or parts thereof.
Den annen komponent av kolon-preparatet er av den type at det lett absorberer vann og sveller til et visst volum. Dette finner sted i en viss grad under sure betingelser (pH 3)5men dets egenskap øker ved økende pH (3 _ 10) i den vandige opp-løsning. Ved pH som er tilstede i tarmkanalen har volumet øket betraktelig (-2 - 20 ganger) sammenlignet til i maven. Disse forbindelser er fortrinnsvis polymere som har fri karboksygrupper, som polyakrylsyre (Garbopol-typen), karboksypolysakkarider, som Karaja gummi (sterculia gummi), gum ghatti (India gummi), gummi arabicum eller salter herav, som polykarbofil, natriumkarboksy- The second component of the colon preparation is of the type that easily absorbs water and swells to a certain volume. This takes place to a certain extent under acidic conditions (pH 3)5, but its property increases with increasing pH (3 - 10) in the aqueous solution. At the pH present in the intestinal tract, the volume has increased considerably (-2 - 20 times) compared to the stomach. These compounds are preferably polymers having free carboxyl groups, such as polyacrylic acid (Garbopol type), carboxypolysaccharides, such as Karaja gum (sterculia gum), gum ghatti (India gum), gum arabic or salts thereof, such as polycarbophil, sodium carboxy-
metylcellulose, kalsiumalginat.methylcellulose, calcium alginate.
Bindemidlet kan være det vanlige stoff som benyttes som granuleringsmidler ved fremstilling av tabletter og granuler, som polyvinylpyrrolidon, polyvinylacetat, etylcellulose og poly-akrylater• The binder can be the usual substance used as granulating agents in the production of tablets and granules, such as polyvinylpyrrolidone, polyvinyl acetate, ethyl cellulose and polyacrylates•
Disse anvendes fortrinnsvis i kombinasjon med et lyofilt stoff som cetanol, voks, fettsyreestere, glycerolestere et c. These are preferably used in combination with a lyophilic substance such as cetanol, wax, fatty acid esters, glycerol esters et c.
Ytterligere lipofile stoffer kan benyttes for be-legg av den faste sammensetning for å muliggjøre administrering av preparatet når det er tilstede i granulær form. Additional lipophilic substances can be used for coating the solid composition to enable administration of the preparation when it is present in granular form.
Granulene som dannes kan administreres som sådanne eller suspendert i en oppløsning som et slim eller suspensjon. De kan også presses til tabletter. The granules formed can be administered as such or suspended in a solution as a slime or suspension. They can also be pressed into tablets.
Oppfinnelsen skal forklares nærmere ved hjelp av noen eksempler. The invention will be explained in more detail with the help of some examples.
En egnet metode for å bestemme vannabsorberings-kapasiteten av preparatene ifølge oppfinnelsen er følgende: 0,5 g av.preparatet bringes i kontakt med 40 ml av mave- eller tarmsaft i 24 timer. Deretter sentrifugeres blandingen ved 4000'omdreininger pr. minutt i 5 minutter og sentrifugatet fjernes. Mengden som blir tilbake tilsvarer vannabsorberings-kapasiteten av preparatet. A suitable method for determining the water absorption capacity of the preparations according to the invention is the following: 0.5 g of the preparation is brought into contact with 40 ml of gastric or intestinal juice for 24 hours. The mixture is then centrifuged at 4,000 rpm. minute for 5 minutes and the centrifuge is removed. The amount that remains corresponds to the water absorption capacity of the preparation.
Eksempel 1.Example 1.
50 g hvetekli og 20 g "Carbopol" 934 blandes og tilsettes 7 g "Vinnapas" B 100 (polyvinylacetat) og 18 g glyce-rylmonostearat oppløst i metylenklorid/isopropanolblanding (9+1)-Granulene tørkes og males gjennom en sikt 2,4 mm. 50 g of wheat bran and 20 g of "Carbopol" 934 are mixed and 7 g of "Vinnapas" B 100 (polyvinyl acetate) and 18 g of glyceryl monostearate dissolved in a methylene chloride/isopropanol mixture (9+1) are added. The granules are dried and ground through a sieve 2.4 etc.
0,5 g absorberer 2,7 g H20 i mavesaft.0.5 g absorbs 2.7 g H20 in gastric juice.
0,5 g absorberer 18 g H20 i tarmsaft.0.5 g absorbs 18 g H20 in intestinal juice.
Eksempel 2.Example 2.
50 g hvetekli blandes med 20 g kalsiumalginat og 13,4 g "Kollidon" K 90 (polyvinylpyrrolidon) oppløst i isopropanol tilsettes. Granulene tørkes og males gjennom en sikt 2,4 mm. 50 g of wheat bran is mixed with 20 g of calcium alginate and 13.4 g of "Kollidon" K 90 (polyvinylpyrrolidone) dissolved in isopropanol is added. The granules are dried and ground through a 2.4 mm sieve.
0,5 g absorberer 2 g H20 i mavesaft.0.5 g absorbs 2 g H20 in gastric juice.
0,5 g absorberer 8 g H20 i tarmsaft.0.5 g absorbs 8 g H20 in intestinal juice.
Eksempel 3-Example 3-
50 g "Avicel" (mikrokrystallinsk cellulose) blandes med 2 g "Carbopol" 934 og tilsettes 4,2 g "Kollidon" K 90 opp- løst i en blanding av metylenklorid og isopropanol (9+1). Granulene tørkes og presses til tabletter på en Diaf eksenter-presse. 50 g of "Avicel" (microcrystalline cellulose) is mixed with 2 g of "Carbopol" 934 and 4.2 g of "Kollidon" K 90 dissolved in a mixture of methylene chloride and isopropanol (9+1) is added. The granules are dried and pressed into tablets on a Diaf eccentric press.
1 tablett (= 0,5 g) absorberer 1,5 g mavesaft.1 tablet (= 0.5 g) absorbs 1.5 g of gastric juice.
1 tablett (= 0,5 g) absorberer 4,5 g tarmsaft. 1 tablet (= 0.5 g) absorbs 4.5 g of intestinal juice.
Preparatene ifølge oppfinnelsen kan også benyttes ved andre abnorme tilstander i tarmen som obstipasjon, idet feces får en mere normal konsistens og normalt volum, hvilket forbedrer tarmens motoriske aktivitet. The preparations according to the invention can also be used for other abnormal conditions in the intestine such as constipation, as faeces acquire a more normal consistency and normal volume, which improves the motor activity of the intestine.
Claims (1)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE7504049A SE7504049L (en) | 1975-04-09 | 1975-04-09 | COLON PREPARATION |
Publications (1)
Publication Number | Publication Date |
---|---|
NO761101L true NO761101L (en) | 1976-10-12 |
Family
ID=20324216
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO761101A NO761101L (en) | 1975-04-09 | 1976-03-30 |
Country Status (12)
Country | Link |
---|---|
BE (1) | BE840552A (en) |
DE (1) | DE2614296A1 (en) |
DK (1) | DK153376A (en) |
FI (1) | FI56772C (en) |
FR (1) | FR2306710A1 (en) |
GB (1) | GB1538123A (en) |
IE (1) | IE42793B1 (en) |
LU (1) | LU74732A1 (en) |
NL (1) | NL7603600A (en) |
NO (1) | NO761101L (en) |
NZ (1) | NZ180552A (en) |
SE (1) | SE7504049L (en) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS52139715A (en) * | 1976-05-14 | 1977-11-21 | Nippon Kayaku Co Ltd | Coated granules of alkali polyacrylate |
FR2471186A1 (en) * | 1979-12-10 | 1981-06-19 | Roussel Uclaf | NEW COLIC DELITESCENCE TABLETS AND THEIR PREPARATION PROCESS |
US4444761A (en) * | 1981-05-04 | 1984-04-24 | Syntex (U.S.A.) Inc. | Cellulose/carboxymethyl cellulose mixtures useful for controlling fecal output, and methods employing them |
US4522804A (en) * | 1983-01-03 | 1985-06-11 | Verex Laboratories, Inc. | Constant release rate solid oral dosage formulations of propranolol |
US4461759A (en) * | 1983-01-03 | 1984-07-24 | Verex Laboratories, Inc. | Constant release rate solid oral dosage formulations of veropamil |
US4521401A (en) * | 1983-01-03 | 1985-06-04 | Verex Laboratories, Inc. | Constant release rate solid oral dosage formulations of quinidine |
EP0273209B1 (en) * | 1986-12-30 | 1992-01-15 | American Cyanamid Company | Composition of matter containing polycarbophil |
GB8817015D0 (en) * | 1988-07-16 | 1988-08-17 | Reckitt & Colmann Prod Ltd | Method of treatment |
AU627775B2 (en) * | 1988-09-20 | 1992-09-03 | Glaxo Group Limited | Pharmaceutical compositions |
DE527942T1 (en) * | 1990-05-04 | 1994-03-03 | Perio Prod Ltd | DISPENSING SYSTEM IN COLON. |
IL98087A (en) * | 1990-05-04 | 1996-11-14 | Perio Prod Ltd | Colonic drug delivery system |
DE9212938U1 (en) * | 1992-09-25 | 1992-11-26 | Boehringer Ingelheim Gmbh, 6507 Ingelheim | Calcium polycarbophil preparation for taking high doses of active ingredients |
US5840332A (en) * | 1996-01-18 | 1998-11-24 | Perio Products Ltd. | Gastrointestinal drug delivery system |
KR20200003827A (en) | 2017-04-14 | 2020-01-10 | 젤레시스 엘엘씨 | Compositions and Methods for Treating or Preventing Intestinal Permeability-Related Disorders |
-
1975
- 1975-04-09 SE SE7504049A patent/SE7504049L/en unknown
-
1976
- 1976-03-30 NO NO761101A patent/NO761101L/no unknown
- 1976-03-31 DK DK153376A patent/DK153376A/en not_active IP Right Cessation
- 1976-04-02 DE DE19762614296 patent/DE2614296A1/en not_active Withdrawn
- 1976-04-06 NL NL7603600A patent/NL7603600A/en not_active Application Discontinuation
- 1976-04-07 FI FI760948A patent/FI56772C/en not_active IP Right Cessation
- 1976-04-08 FR FR7610342A patent/FR2306710A1/en active Granted
- 1976-04-08 GB GB14390/76A patent/GB1538123A/en not_active Expired
- 1976-04-08 NZ NZ180552A patent/NZ180552A/en unknown
- 1976-04-09 BE BE165981A patent/BE840552A/en unknown
- 1976-04-09 LU LU74732A patent/LU74732A1/xx unknown
- 1976-04-09 IE IE749/76A patent/IE42793B1/en unknown
Also Published As
Publication number | Publication date |
---|---|
DE2614296A1 (en) | 1976-10-21 |
NL7603600A (en) | 1976-10-12 |
FR2306710B1 (en) | 1979-07-13 |
NZ180552A (en) | 1978-07-28 |
FR2306710A1 (en) | 1976-11-05 |
GB1538123A (en) | 1979-01-10 |
FI760948A (en) | 1976-10-10 |
DK153376A (en) | 1976-10-10 |
FI56772B (en) | 1979-12-31 |
IE42793B1 (en) | 1980-10-22 |
FI56772C (en) | 1980-04-10 |
BE840552A (en) | 1976-10-11 |
LU74732A1 (en) | 1977-02-04 |
SE7504049L (en) | 1976-10-10 |
IE42793L (en) | 1976-10-09 |
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