EP1487408A1 - Topical composition based on ion-exchange resins, in particular for treating erythemas - Google Patents

Topical composition based on ion-exchange resins, in particular for treating erythemas

Info

Publication number
EP1487408A1
EP1487408A1 EP03738198A EP03738198A EP1487408A1 EP 1487408 A1 EP1487408 A1 EP 1487408A1 EP 03738198 A EP03738198 A EP 03738198A EP 03738198 A EP03738198 A EP 03738198A EP 1487408 A1 EP1487408 A1 EP 1487408A1
Authority
EP
European Patent Office
Prior art keywords
topical composition
composition according
erythemas
exchange resins
ion
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Withdrawn
Application number
EP03738198A
Other languages
German (de)
French (fr)
Inventor
Jack Auzerie
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ellipse Pharmaceuticals SAS
Original Assignee
Ellipse Pharmaceuticals SAS
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Ellipse Pharmaceuticals SAS filed Critical Ellipse Pharmaceuticals SAS
Publication of EP1487408A1 publication Critical patent/EP1487408A1/en
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • 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
    • A61K31/785—Polymers containing nitrogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention concerns a topical composition in particular for treating erythemas, characterized in that it comprises at least one ion-exchange resin such as colestyramine and at least one substance containing buffer properties.

Description

A AT
COMPOSITION TOPIQUE A BASE OE RESINES ECHANGEUSES D'IONS, NOTAMMENT POUR LE TRAITEMENT DES ERYTHEMESTOPICAL COMPOSITION BASED ON ION-EXCHANGING RESINS, PARTICULARLY FOR THE TREATMENT OF ERYTHEMS
La présente invention concerne une composition topique à base de résines échangeuses d'ions comme la colestyramine, notamment pour le traitement des érythèmes fessiers en pédiatrie.The present invention relates to a topical composition based on ion exchange resins such as colestyramine, in particular for the treatment of diaper rash in pediatrics.
Les diarrhées aiguës qui affectent de nombreux enfants, plus particulièrement les enfants de moins de cinq ans, nécessitent souvent un traitement pour éviter des surinfections et pour soulager les enfants de la douleur et des démangeaisons engendrées.Acute diarrhea, which affects many children, especially children under the age of five, often requires treatment to avoid secondary infections and to relieve children of the pain and itching it causes.
En effet, les épisodes diarrhéiques aigus provoquent des troubles dermatologiques notamment des lésions cutanées difficiles à cicatriser. Un des facteurs qui initie ce type de troubles dermatologiques est la défécation des sels biliaires qui sont ensuite au contact intime avec la peau.In fact, acute diarrheal episodes cause dermatological disorders, especially skin lesions that are difficult to heal. One of the factors that initiates this type of dermatological disorder is the defecation of bile salts which are then in intimate contact with the skin.
Tout d'abord, ces sels biliaires qui sont des acides abaissent le pH cutané et induisent l'érythème.First of all, these bile salts which are acids lower the skin pH and induce erythema.
Ensuite, ces sels biliaires ont des propriétés tensioactives, si bien que la couche de sébum qui est naturellement protectrice, est éliminée.Then, these bile salts have surface-active properties, so that the layer of sebum which is naturally protective, is eliminated.
Afin de lutter contre ces affections, on peut agir :In order to fight against these affections, we can act:
1/ d'une part avec des traitements par voie orale, notamment la prise :1 / on the one hand with oral treatments, in particular taking:
- d'antibiotiques,- antibiotics,
- de ferments lactiques, - d'opiacés, notamment le lopéramide, - principes actifs à activité anti-sécrétoire, comme le produit commercial Tiorfan, et- lactic ferments, - opiates, in particular loperamide, - active ingredients with anti-secretory activity, such as the commercial product Tiorfan, and
- d'argiles, commercialisées sous les dénominations Smecta ou Actapulgite.2/ d'autre part avec application d'une crème ou pommade, notamment : - celles connues sous les dénominations commerciales Jonctum, Madécassol, Mytosil,- clays, marketed under the names Smecta or Actapulgite. 2 / on the other hand with the application of a cream or ointment, in particular: - those known under the trade names Jonctum, Madécassol, Mytosil,
- celles incluant des dermocorticoïdes associés ou non à des antibiotiques. De telles préparations sont dites à activité trophique ou protectrice.- those including dermocorticoids associated or not with antibiotics. Such preparations are said to have trophic or protective activity.
Les résultats sont peu satisfaisants car la barrière occlusive créée peut participer à une surinfection de la plaie par apparition d'une flore bactérienne anaérobie.The results are not very satisfactory because the occlusive barrier created can participate in a secondary infection of the wound by the appearance of an anaerobic bacterial flora.
De plus, ces préparations ne neutralisent pas l'acidité des sels biliaires.In addition, these preparations do not neutralize the acidity of bile salts.
Ces traitements connus ne donnent donc pas satisfaction.These known treatments are therefore not satisfactory.
Notamment la colestyramine est une résine basique synthétique échangeuse d'anions qui présente une forte affinité pour les sels biliaires et forment avec eux un complexe insoluble. On sait que 1 gramme de colestyramine peut absorber jusqu'à deux grammes de sels biliaires. C'est une poudre hygroscopique fine de couleur blanche, quasiment insoluble dans l'eau, l'alcool, le chloroforme et l'éther. Dans une solution à 1 %, le pH est compris entre 4 et 6. Un médicament dont la dénomination commerciale est le Questran, est indiqué pour le traitement des hypercholestérolémies.In particular, colestyramine is a basic synthetic anion exchange resin which has a strong affinity for bile salts and forms with them an insoluble complex. We know that 1 gram of colestyramine can absorb up to two grams of bile salts. It is a fine white hygroscopic powder, almost insoluble in water, alcohol, chloroform and ether. In a 1% solution, the pH is between 4 and 6. A drug, the trade name of which is Questran, is indicated for the treatment of high cholesterolemia.
Cette poudre permet d'absorber les sels biliaires présents dans le tractus gastro-intestinal. On peut ainsi prévenir la formation de calculs et diminuer les triglycérides circulants. La présente invention concerne une composition incluant au moins une résine échangeuse d'ions, notamment la colestyramine ainsi qu'un régulateur de pH. En effet, de façon tout à fait pertinente, le régulateur permet d'augmenter le pH pour permettre une absorption optimisée des sels biliaires par les résines échangeuses d'ions.This powder absorbs bile salts present in the gastrointestinal tract. This can prevent stone formation and decrease circulating triglycerides. The present invention relates to a composition including at least one ion exchange resin, in particular colestyramine as well as a pH regulator. Indeed, in a completely relevant way, the regulator makes it possible to increase the pH to allow an optimized absorption of bile salts by ion exchange resins.
C'est ainsi qu'un pH compris entre 4 et 8, de préférence voisin de 6, est adapté. La composition selon la présente invention est maintenant décrite à l'aide d'exemples particuliers non limitatifs.Thus a pH between 4 and 8, preferably close to 6, is adapted. The composition according to the present invention is now described using specific non-limiting examples.
Une composition de base selon la présente invention comprend les éléments suivants :A basic composition according to the present invention comprises the following elements:
- 30 % en poids de colestyramine, - 30 % en poids d'hydroxyde d'aluminium,- 30% by weight of colestyramine, - 30% by weight of aluminum hydroxide,
- 30 % en poids hydroxyde de magnésium, et - 10 % d'eau- 30% by weight magnesium hydroxide, and - 10% water
Cette composition conduit à une pâte épaisse.This composition results in a thick paste.
Des essais sont conduits sur des sujets ayant comme affection une dermatite secondaire ;Trials are conducted on subjects with secondary dermatitis as a condition;
- à une gastro-entérite infectieuse,- infectious gastroenteritis,
- au syndrome d'intestin grêle court, et- short small intestine syndrome, and
- à une entérocolite nécrotique néonatale.- neonatal necrotic enterocolitis.
La pâte épaisse à base de colestyramine est appliquée 4 fois par jour sur la zone correspondant sensiblement à la zone couverte par une couche culotte.The thick colestyramine paste is applied 4 times a day to the area corresponding substantially to the area covered by a diaper.
L'observation médicale est conduite à chaque application.The medical observation is conducted for each application.
On note une régression des lésions au bout de 2 à 7 jours.A regression of the lesions is noted after 2 to 7 days.
Ainsi la composition permet un rééquilibrage physiologique local suite à l'apparition de la dermite irritative. Les régulateurs de pH peuvent être choisis aussi parmi : le phosphate monopotassique, le phosphate disodique, l'acétate de sodium, l'acétate d'ammonium, le citrate de sodium, l'acide citrique, le tétraborate de disodium, l'acide borique, les acides aminés comme la lysine, la leucine, l'alanine, le pαrαhydroxybenzoαte de méthyle, le pαrαhydroxybenzoαte de propyle, le benzoαte de sodium.Thus the composition allows a local physiological rebalancing following the appearance of irritant dermatitis. The pH regulators can also be chosen from: monopotassium phosphate, disodium phosphate, sodium acetate, ammonium acetate, sodium citrate, citric acid, disodium tetraborate, boric acid , amino acids like lysine, leucine, alanine, methyl pαrαhydroxybenzoαte, propyl pαrαhydroxybenzoαte, sodium benzoαte.
Plus généralement, on peut retenir les substances douées de propriétés tampon.More generally, substances endowed with buffering properties can be retained.
Des exemples de formulations galéniques sous forme de crèmes ou de talc sont indiquées ci-après.Examples of galenical formulations in the form of creams or talc are given below.
Labraf il : nom commercial de macrogolglycérides oléïquesLabraf il: trade name of oleic macrogolglycerides
Tef ose 63 : nom commercial de PEG-6-32 Stéarate et glycol stéarate. / Crème avec 10 % de colestyramine et du dihydrogénophosphate de sodiumTefose 63: trade name of PEG-6-32 Stearate and glycol stearate. / Cream with 10% colestyramine and sodium dihydrogen phosphate
3/ Talc comprenant 10 % de colestyramine :3 / Talc comprising 10% colestyramine:
On peut envisager différentes formes galéniques :We can consider different dosage forms:
- crème,- cream,
- gels,- gels,
- lotions,- lotions,
- aérosols, - spray-aérosols La composition peut aussi être envisagée en application directement sur des supports externes au contact direct des zones à traiter comme les couches culottes pour les nourrissons, enfants et personnes âgées. - aerosols, - spray-aerosols The composition can also be considered for application directly to external supports in direct contact with the areas to be treated, such as diapers for infants, children and the elderly.

Claims

REVENDICATIONS
1. Composition topique notamment pour le traitement des érythèmes, caractérisée en ce qu'elle inclut au moins de la colestyramine comme résine échangeuse d'ions et au moins une substance douée de propriétés tampon. 1. Topical composition in particular for the treatment of erythemas, characterized in that it includes at least colestyramine as an ion exchange resin and at least one substance endowed with buffering properties.
2. Composition topique selon la revendication 1, caractérisée en ce que la substance douée de propriété tampon est choisie parmi le phosphate monopotassique, le phosphate disodique, l'acétate de sodium, l'acétate d'ammonium, le citrate de sodium, l'acide citrique, le tétraborate de disodium, l'acide borique, les acides aminés comme la lysine, la leucine, l'alanine, le parahydroxybenzoate de méthyle, le parahydroxybenzoate de propyle, le benzoate de sodium.2. Topical composition according to claim 1, characterized in that the substance endowed with buffering property is chosen from monopotassium phosphate, disodium phosphate, sodium acetate, ammonium acetate, sodium citrate, citric acid, disodium tetraborate, boric acid, amino acids such as lysine, leucine, alanine, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium benzoate.
3. Composition topique selon la revendication 1 ou 2, caractérisée en ce qu'elle comprend un régulateur de pH permettant de conférer à ladite composition un pH compris entre 4 et 8, pour permettre une absorption optimisée des sels biliaires par les résines échangeuses d'ions.3. Topical composition according to claim 1 or 2, characterized in that it comprises a pH regulator making it possible to give said composition a pH of between 4 and 8, to allow optimized absorption of bile salts by the exchange resins of ions.
4. Composition topique selon la revendication 3, caractérisée en ce que le régulateur de pH permet de conférer à ladite composition un pH voisin de 6,0.4. Topical composition according to claim 3, characterized in that the pH regulator makes it possible to confer on said composition a pH close to 6.0.
5. Composition topique selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle est présentée sous l'une des différentes formes galéniques, crème, gels, lotions, aérosols ou spray- aérosols.5. Topical composition according to any one of the preceding claims, characterized in that it is presented in one of the different dosage forms, cream, gels, lotions, aerosols or spray-aerosols.
6. Composition topique selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle est appliquée directement sur des supports externes au contact direct des zones à traiter. 6. Topical composition according to any one of the preceding claims, characterized in that it is applied directly to external supports in direct contact with the areas to be treated.
EP03738198A 2002-03-26 2003-03-26 Topical composition based on ion-exchange resins, in particular for treating erythemas Withdrawn EP1487408A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0203729 2002-03-26
FR0203729A FR2837710B1 (en) 2002-03-26 2002-03-26 TOPICAL COMPOSITION BASED ON ION-EXCHANGE RESINS, IN PARTICULAR FOR THE TREATMENT OF ERYTHEMES
PCT/FR2003/000948 WO2003080025A1 (en) 2002-03-26 2003-03-26 Topical composition based on ion-exchange resins, in particular for treating erythemas

Publications (1)

Publication Number Publication Date
EP1487408A1 true EP1487408A1 (en) 2004-12-22

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ID=27839185

Family Applications (1)

Application Number Title Priority Date Filing Date
EP03738198A Withdrawn EP1487408A1 (en) 2002-03-26 2003-03-26 Topical composition based on ion-exchange resins, in particular for treating erythemas

Country Status (6)

Country Link
US (1) US20050220755A1 (en)
EP (1) EP1487408A1 (en)
AU (1) AU2003244715A1 (en)
CA (1) CA2480007A1 (en)
FR (1) FR2837710B1 (en)
WO (1) WO2003080025A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2947276B1 (en) * 2009-06-24 2012-10-26 Seppic Sa COSMETIC COMPOSITION BASED ON ION EXCHANGE RESINS LOADED WITH LIPOAMINOACIDES
DE102022103062A1 (en) * 2022-02-09 2023-08-10 Dietrich Seidel Products for bacterial toxin binding and elimination in the treatment of wounds and inflammatory skin lesions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2919230A (en) * 1953-10-29 1959-12-29 Rohm & Haas Hydrophilic base therapeutic compositions comprising cation-exchange resin
US4851392A (en) * 1985-02-05 1989-07-25 Warner-Lambert Company Ingestible aggregate and delivery system prepared therefrom
ATE180968T1 (en) * 1991-12-20 1999-06-15 Hoechst Ag POLYASPARTAMIDE DERIVATIVES AS ADSORPTION AGENTS FOR BALE ACIDS, POLYASPARTAMIDE DERIVATIVES LOADED WITH BALE ACIDS AND METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
JP2003517441A (en) * 1998-09-25 2003-05-27 アルコン ラボラトリーズ， インコーポレイテッド Sustained-release and comfortable composition for eye disease and method for treating eye disease
BR0014117A (en) * 1999-09-21 2002-05-14 Alcon Lab Inc Use of fatty acid / amino acid soaps to increase the antimicrobial effectiveness of topical pharmaceutical compositions

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
None *
See also references of WO03080025A1 *

Also Published As

Publication number Publication date
FR2837710B1 (en) 2005-07-08
WO2003080025A1 (en) 2003-10-02
US20050220755A1 (en) 2005-10-06
CA2480007A1 (en) 2003-10-02
AU2003244715A1 (en) 2003-10-08
FR2837710A1 (en) 2003-10-03

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