EP3484494A1 - A pharmaceutical or food supplement formulation for the treatment of intestinal constipation - Google Patents
A pharmaceutical or food supplement formulation for the treatment of intestinal constipationInfo
- Publication number
- EP3484494A1 EP3484494A1 EP17748660.2A EP17748660A EP3484494A1 EP 3484494 A1 EP3484494 A1 EP 3484494A1 EP 17748660 A EP17748660 A EP 17748660A EP 3484494 A1 EP3484494 A1 EP 3484494A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- extract
- dry extract
- fruit
- buckthorn
- constipation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
- A23L2/52—Adding ingredients
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/72—Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/906—Zingiberaceae (Ginger family)
- A61K36/9068—Zingiber, e.g. garden ginger
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
Definitions
- TITLE A pharmaceutical or food supplement formulation for the treatment of intestinal constipation
- the present invention relates to the sector of the pharmaceutical and food supplement and functional food industry.
- the invention relates to a tamarind-based composition for the regulation of the gastrointestinal motility and the prevention and/ or treatment of the intestinal constipation.
- Constipation is a disorder of the intestinal motor activity, very common particularly among industrialized countries. It is one of the most frequent gastrointestinal disorders and about 13 million Italians, including about 9 million women, suffer from it.
- Constipation is essentially a disorder connected to defecation and consists in the difficulty to evacuate the intestine. Constipation occurs with a considerable reduction of the evacuation frequency and of the feces volume, abdominal pain and swelling, meteorism and difficulty to evacuate.
- Constipation is a symptom rather than a disease and in most cases it is temporary and not severe.
- the most frequent cause of constipation is to attribute to a fiber- deficient diet or to an excessively high fat content.
- a healthy diet with a high content of vegetables, fresh fruit, wholewheat bread and cereals, is fundamental in preventing constipation.
- An abundant liquid intake allows to keep soft feces, facilitating their expulsion and a constant physical activity is just as much important to maintain an adequate intestinal muscle tone.
- laxatives are generally used.
- Laxatives are usually classified in four categories:
- laxatives which increase feces volume, thereby promoting intestinal transit; among these it is possible to mention psyllium seeds, agar-agar, bran, fucus and guar gum;
- Contact laxatives that act by increasing the contractions of the intestinal wall, thereby activating the peristalsis: among these the following can be mentioned: cascara, senna, buckthorn, rhubarb, castor oil, phenolphthalein, bisacodyl and sodium picosulphate.
- Emollient laxatives that act by mixing themselves to the feces, thereby softening and lubricating them; among these it is possible to mention glycerin and liquid paraffin;
- Osmotic laxatives that act retaining and drawing liquids from the intestine, so as to form voluminous and soft feces and to accelerate the transit thereof in the large intestine; among these it is possible to mention lactulose, mannitol, magnesium salts, sorbitol and tamarind.
- laxative categories exhibits drawbacks.
- contact laxatives can cause diarrhea and abdominal cramps and their prolonged use can damage intestinal muscle function with worsening of the constipation.
- Emollient laxatives can interfere with the absorption of liposoluble vitamins and calcium.
- Osmotic laxatives, especially at high doses, can cause abdominal cramps, nausea and vomiting, as well as dehydration and renal problems.
- Bulk-forming laxatives are the relatively most safe but they are not always sufficient to resolve constipation and moreover, if they are taken in excessive doses, can cause meteorism and obstruction of the intestinal tract.
- the Applicant conducted a research project aimed at providing a food supplement composition for the regulation of the gastrointestinal motility, suitable to prevent and/ or treat constipation, without causing undesired side effects.
- Tamarindus indica The research project started from what was already known in the scientific literature about the effects of tamarind (Tamarindus indica). Tamarind is mentioned as delicate laxative in several pharmacopoeias and it is used in various traditional medicines, particular in the African one.
- the part of tamarind which is used is the fruit pulp, which contains high concentrations of malic acid and tartaric acid, as well as potassium bitartrate, reducing sugars, vitamin B and minerals (Havinga et al., 2010).
- Organic acids in particular, have a laxative effect by virtue of osmotic action.
- Tartaric acid has both a direct and an indirect osmotic effect: following its fermentation by the colon microbiota, in fact, short-chain fatty acids (SCFA) are produced, which in turn draw water and increase feces hydration (Spiller et al., 2003).
- SCFA short-chain fatty acids
- Tamarind is considered harmless and no noteworthy side effects are reported in literature except the possibility to cause, like the other osmotic laxatives, some abdominal discomfort.
- the patent application IN 2209/CHE/201 1 describes a laxative comprising various vegetable ingredients, among which there are senna, haritiki (Terminalia chebula), and bahera as active ingredients with laxative action, tamarind to improve aroma and palatability and ginger to facilitate digestion.
- US 2012/ 156143 discloses a composition comprising one or more plant-derived cathartics and an effervescent coupling system.
- plant-derived cathartics buckthorn, alder buckthorn and ginger are mentioned.
- An aim of the present invention is to provide a composition for the treatment of constipation, suitable in particular for the treatment of chronic and occasional constipation, for which bulk-forming laxatives do not show good results, based on active ingredients of natural origin and with the mildest possible action and without side effects.
- composition that comprises an active ingredient with a laxative effect of osmotic type, consisting of tamarind extract, a ginger extract (Zingiber officinale Rose.) and a buckthorn (Frangula dodonei) extract, wherein the buckthorn extract is in a weight ratio less than or equal to 0.03 with respect to the tamarind extract.
- the ginger extract contained in the composition according to the invention prevents the above-mentioned possible, albeit limited, side effects of tamarind extract, thanks to its antiemetic, prokinetic and antispasmodic effects, which prevent abdominal discomfort that could be caused by tamarind, essentially consisting in abdominal swelling and flatulence.
- the buckthorn extract is a contact laxative, whose effect is due to the anthraquinone active ingredient glucofranguline A, and it is considered the mildest anthraquinone laxative.
- buckthorn preparations standardized so as to contain 20-30 mg of glucofranguline A are used.
- An optional component of the composition according to the present invention is caraway (Carum carvi) extract which, besides having antispasmodic effects similar to those of ginger extract, useful to prevent the possible abdominal discomfort caused by the tamarind extract, also shows a marked carminative effect and a choleretic and anti-fermentation action, thus selectively inhibiting intestinal pathogenic bacteria and helping rebalance the intestinal microbiota.
- caraway Carum carvi
- the present invention also relates to a pharmaceutical or food supplement formulation suitable for oral administration, for the treatment of constipation, comprising the above-described composition and pharmaceutically or nutritionally acceptable excipients.
- Such formulation comprises one or more dosage units, each of which comprises from 4.0 to 6.0 g of a 1 : 4 dry extract of Tamarindus indica L. fruit, from 0.10 to 0.30 g of a dry extract of Zingiber officinale Roscoe rhizome, from 0.10 to 0.15 g of a dry extract of buckthorn (Frangula dodonei) bark, and pharmaceutically or nutritionally acceptable excipients.
- the above-mentioned dosage unit can further comprise from 0.10 to 0.20 g of dry extract of Carum carvi fruit.
- a dry extract of Zingiber officinale Roscoe rhizome containing 1% total gingerols, a dry extract of buckthorn (Frangula dodonei Ard.) bark containing 7.7%-9.0% glucofranguline A and a dry extract of Carum carvi L. fruit containing 2.5% polyphenols and 0.8% essential oil are used.
- each dosage unit comprises from 7.7 mg to 13.5 mg of glucofranguline A.
- Solid dosage forms for oral administration include for example capsules, tablets, powders, granules and gels.
- the active ingredient can be mixed with at least one inert diluent such as for example sucrose, lactose, starch or maltodextrin.
- these dosage forms also include additional substances different from inert diluents, such as for example sweeteners, such as sorbitol, sucralose and steviol glycosides, flavours and anti-caking agents such as silicon dioxide.
- the pharmaceutical preparations according to the present invention can be produced using conventional pharmaceutical techniques, as they are described in the various pharmacopoeias or in handbooks of the art such as for example "Remington's Pharmaceutical Sciences 15 Handbook", Mack Publishing, New York, 18th Ed., 1990.
- the daily mean dosage of the compounds according to the present invention depends on many factors, such as for example the severity of the constipation and the condition of the patient (age, weight, sex): the dose can usually vary from 2.0 g to 15.0 g, preferably from 2.7 to 1 1.0 g, of composition according to the invention per day, possibly divided in several administrations.
- the present invention relates to a functional food containing the above-described composition.
- this functional food is such that a predetermined portion thereof contains from 4.0 to 6.0 g of a 1 :4 dry extract of Tamarindus indica L. fruit, from 0.10 to 0.30 g of a dry extract of Zingiber officinale Roscoe rhizome and from 0.10 to 0.15 g of a dry extract of buckthorn (Frangula dodonei) bark.
- such portion also contains from 0.10 to 0.20 g of a dry extract of Carum caraway fruit.
- the functional food of interest can be for example a cereal bar, a yogurt or a similar dairy product, a bakery product or a fruit juice.
- Dosage unit of a formulation according to the invention is a formulation according to the invention.
- Dosage unit of a formulation according to the invention is a formulation according to the invention.
- dry extracts mentioned in the examples above are more precisely the following: dry extract of Zingiber officinale Roscoe rhizome containing 1% total gingerols, dry extract of buckthorn (Frangula dodonei Ard.) bark containing 7.7%-9.0% glucofranguline A and dry extract of Carum carvi L. fruit containing 2.5% polyphenols and 0.8% essential oil.
- Examples 1 and 2 were realized in form of powder sachets, possibly bipartite, intended to be dissolved in water for oral administration.
- composition according to example 2 was tested in patients affected by chronic constipation, selected on the basis of the diagnostic criteria set in the Consensus Conference on the Diagnostic Criteria of Functional Disorders of the Intestine (called Rome III), namely on the basis of the presence of at least two of the following characteristics: straining during defecation, hard stools or fecalomas, sensation of incomplete evacuation, sensation of anorectal obstruction/blockage, need to perform manual maneuvers for evacuation, fewer than three defecations per week. This in the absence of a diagnosis of irritable bowel syndrome.
- 1 1 patients were selected on the basis of the above-mentioned criteria and such patients were divided into two groups A and B, composed of 8 and 3 patients respectively, on the basis of how severe was the constipation, which was more severe in group A.
- the composition according to the present invention proves to be effective in opposing constipation already at a dose corresponding to half the dosage unit of the example 2. Moreover, the composition proves to be very well tolerated, since it did not provoke abdominal pain except in a very mild form in only two patients from group A and did not provoke diarrhea episodes. In addition, it was not observed any abdominal swelling. Finally, patients evaluated pleasant the taste of the composition according to the present invention.
- the buckthorn extract is comprised in the tested composition in such an amount to have around 10- 12 mg glucofranguline A in each dosage unit, a dose which corresponds to around half the minimum dose of glucofranguline A used to achieve a laxative effect (monographs about buckthorn suggest typical glucofranguline A intake equal to 20 mg or 30 mg). This suggests a synergic effect of the buckthorn extract with the tamarind extract in causing a significant laxative effect of the present composition even if the amount of buckthorn extract would not by itself be sufficient to perform any therapeutically useful activity.
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- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Botany (AREA)
- Medicinal Chemistry (AREA)
- Mycology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biotechnology (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Alternative & Traditional Medicine (AREA)
- Food Science & Technology (AREA)
- Nutrition Science (AREA)
- Polymers & Plastics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Abstract
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT102016000075072A IT201600075072A1 (en) | 2016-07-18 | 2016-07-18 | Pharmaceutical or dietary supplement composition for the treatment of intestinal constipation |
PCT/EP2017/068056 WO2018015353A1 (en) | 2016-07-18 | 2017-07-17 | A pharmaceutical or food supplement formulation for the treatment of intestinal constipation |
Publications (1)
Publication Number | Publication Date |
---|---|
EP3484494A1 true EP3484494A1 (en) | 2019-05-22 |
Family
ID=57610110
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP17748660.2A Withdrawn EP3484494A1 (en) | 2016-07-18 | 2017-07-17 | A pharmaceutical or food supplement formulation for the treatment of intestinal constipation |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP3484494A1 (en) |
IT (1) | IT201600075072A1 (en) |
WO (1) | WO2018015353A1 (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IT202000005101A1 (en) * | 2020-03-10 | 2021-09-10 | Modesto Giberti | FOOD PREPARATION BASED ON GINGER |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2006514962A (en) * | 2003-01-30 | 2006-05-18 | カウンシル・オブ・サイエンティフィック・アンド・インダストリアル・リサーチ | Bioavailability to enhance the activity of caraway extract and its fractions |
US8545902B2 (en) * | 2010-12-15 | 2013-10-01 | Nicholas Lion | Dosage forms of plant-derived cathartics |
-
2016
- 2016-07-18 IT IT102016000075072A patent/IT201600075072A1/en unknown
-
2017
- 2017-07-17 EP EP17748660.2A patent/EP3484494A1/en not_active Withdrawn
- 2017-07-17 WO PCT/EP2017/068056 patent/WO2018015353A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO2018015353A1 (en) | 2018-01-25 |
IT201600075072A1 (en) | 2018-01-18 |
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Ipc: A61K 36/9068 20060101AFI20200518BHEP Ipc: A23L 33/105 20160101ALI20200518BHEP Ipc: A61K 36/23 20060101ALI20200518BHEP Ipc: A23L 2/52 20060101ALI20200518BHEP Ipc: A61K 36/48 20060101ALI20200518BHEP Ipc: A61P 1/10 20060101ALI20200518BHEP Ipc: A61K 36/72 20060101ALI20200518BHEP |
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