FR2708853A1 - Acetylsalicylic acid composition with improved bioavailability and process for producing it - Google Patents
Acetylsalicylic acid composition with improved bioavailability and process for producing it Download PDFInfo
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- FR2708853A1 FR2708853A1 FR9308013A FR9308013A FR2708853A1 FR 2708853 A1 FR2708853 A1 FR 2708853A1 FR 9308013 A FR9308013 A FR 9308013A FR 9308013 A FR9308013 A FR 9308013A FR 2708853 A1 FR2708853 A1 FR 2708853A1
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- acetylsalicylic acid
- aspirin
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- composition according
- surfactant
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- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
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- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
L'invention concerne une composition à base d'acide acétylsalicylique à biodisponibilité améliorée. Elle comporte: - des particules d'acide acétylsalicylique, ayant notamment des tailles passant au tamis 160 ou 180 microns, enrobées par un agent tensioactif, tel que le dioctylsulfosuccinate de sodium; - une poudre contenant de l'acide citrique anhydre dans une proportion double de la quantité d'acide acétylsalicylique; - une poudre alcaline contenant du bicarbonate de sodium dans une proportion triple de la dose d'aspirine.The invention relates to a composition based on acetylsalicylic acid with improved bioavailability. It comprises: particles of acetylsalicylic acid, in particular having sizes passing through a 160 or 180 micron sieve, coated with a surfactant, such as sodium dioctylsulfosuccinate; - a powder containing anhydrous citric acid in a double proportion of the amount of acetylsalicylic acid; - an alkaline powder containing sodium bicarbonate in a triple proportion of the dose of aspirin.
Description
COMPOSITION A BASE D'ACIDE ACETYLSALICYLIQUE ABIODISPONIBILITE AMELIOREE ET PROCEDE POUR LA PRODUIRE
L'invention concerne une composition ou formule galénique à base d'acide acétylsalicylique (aspirine), pour usage en présentation effervescente extemporanée à pH tamponné, notamment à des valeurs de 5 à 6. Elle contient des particules d'aspirine, ayant des tailles passant au tamis 160 ou 180, caractérisées par un enrobage tensioactif au dioctylsulfosuccinate de sodium. Cet enrobage permet une dispersion et solubilisation de l'aspirine en vue d'améliorer sa biodisponibilité sanguine.
L'invention concerne aussi un procédé pour la fabrication de cette composition. Il comporte notamment les étapes suivantes:
1) l'aspirine broyée ou "micronisée", notamment en particules ayant des tailles passant au tamis 160 ou 180, est mouillée, en atmosphère d'humidité contrôlée, par une solution alcoolique contenant l'agent tensioactif, le dioctylsulfosuccinate de sodium (D.O.S.S.), dans une proportion de 0,1 à 1, par exemple de l'ordre de 0,5 de D.O.S.S. pour cent en poids d'aspirine ; 2) séchage de la préparation par flux d'air sec pulsé ou à l'étuve 40[deg]C, notamment pendant 6 heures ; 3) incorporation des grains d'aspirine enrobés par le tensioactif (D.O.S.S.) dans une poudre contenant de l'acide citrique anhydre dans une proportion double de la dose d'aspirine.
4) optionnellement, incorporation du mélange acide obtenu à une poudre alcaline contenant du bicarbonate de sodium en une dose triple de la dose d'aspirine.
La poudre composée ainsi obtenue à l'issue de l'étape 4) est stable. Versée dans l'eau pour absorption orale, cette poudre composée détermine la dispersion de l'aspirine enrobée dans cette solution effervescente tamponnée par le citrate trisodique reconstitué (pH entre 5 et 6) entraînant la solubilisation des grains d'aspirine avec, pour résultat, une amélioration de la biodisponibilité de cette aspirine.
L'invention concerne aussi des compositions pouvant se présenter sous des emballages divers, plus particulièrement une composition telle qu'obtenue à l'issue de l'étape 3), d'une part, et dans un emballage différent, la poudre alcaline définie dans l'étape 4), d'autre part. Les contenus des deux emballages peuvent alors être mélangés de façon extemporanée ou versés dans l'eau pour l'absorption orale comme il est rappelé ci-dessus.
L'ensemble de ces compositions se conserve très bien à l'abri de l'humidité.
L'invention concerne encore des compositions comportant en sus des ingrédients sus-indiqués, des lyophilisats de jus de fruit permettant l'aromatisation de la composition. Il est important que ces produits lyophilisés ne soient pas conservés en mélange avec celles contenant l'aspirine.
Dans le cas où l'on a recours à la "poudre composée" obtenue au terme de l'étape 4) ci-dessus, déjà à l'état pré-mélangé, il conviendra de présenter la poudre de jus de fruit, notamment d'orange, dans un emballage distinct. En revanche, dans l'hypothèse où le bicarbonate de sodium serait conservé dans un emballage distinct, celui-ci contiendra également, le cas échéant, le lyophilisat de jus de fruit.
Par mélange de ces différents constituants, on obtient par conséquent une aspirine dispersée dont la biodisponibilité est nettement améliorée, sous une forme aromatisée rendant son absorption plus agréable.
L'invention concerne aussi un procédé d'enrobage tensioactif, avec du dioctylsulfosuccinate de sodium, d'aspirine micronisée qui, après incorporation dans une mélange effervescent extemporané, ensuite mis en contact avec de l'eau, conduit à une solution tamponnée entre pH 5 et 6, de biodisponibilité améliorée. La biodisponibilité vérifiée in vivo, chez l'homme dans un centre de biogalénique avec le procédé d'enrobage ci-dessous appliqué à la formule dosée à 300 mg d'aspirine, comparée à une formule courante déjà commercialisée d'aspirine (sans enrobage tensioactif) au même dosage, montre, pour une même dose d'aspirine, une concentration plasmatique 30 % supérieure.
Plusieurs exemples de présentation sous un ou plusieurs emballages de la composition selon l'invention, sont présentés ci-après.
1er exemple de présentation d'une "formule poudre" :
A cette composition, stable en l'absence d'humidité, peut être associé, notamment sous un emballage différent, un lyophilisat de jus de fruit, notamment d'orange, pris en des proportions appropriées pour conférer à la solution effervescente obtenue, lorsque la "formule poudre" sus-indiquée est versée dans l'eau, une aromatisation plaisante au palais.
Deuxième présentation (en des emballages distincts) des constituants principaux de la composition selon l'invention 1er emballage :
optionnellement, Excipient sucré contenant un lyophilisat de jus de fruit : q.s.
Il va sans dire que les indications ci-dessus, quant aux contenus des emballages, ne sont pas exclusives de la présence éventuelle d'autres ingrédients (excipients ou principes actifs) dans ces emballages.ACETYLSALICYLIC ACID-BASED COMPOSITION WITH IMPROVED ABILITABILITY AND PROCESS FOR PRODUCING THE SAME
The invention relates to a composition or galenic formula based on acetylsalicylic acid (aspirin), for use in extemporaneous effervescent presentation at buffered pH, in particular at values of 5 to 6. It contains particles of aspirin, having passing sizes. sieves 160 or 180, characterized by a sodium dioctylsulfosuccinate surfactant coating. This coating allows dispersion and solubilization of aspirin to improve its bioavailability blood.
The invention also relates to a process for the manufacture of this composition. It includes the following steps:
1) the ground or "micronised" aspirin, in particular in particles having sieve sizes 160 or 180, is wetted, in a controlled humidity atmosphere, with an alcoholic solution containing the surfactant, sodium dioctylsulfosuccinate (DOSS ), in a proportion of 0.1 to 1, for example of the order of 0.5 of DOSS per cent by weight of aspirin; 2) drying the preparation by pulsed dry air flow or oven 40 [deg] C, especially for 6 hours; 3) incorporation of the surfactant-coated aspirin grains (DOSS) into a powder containing anhydrous citric acid in a double proportion of the aspirin dose.
4) optionally, incorporating the resulting acid mixture into an alkaline powder containing sodium bicarbonate in a triple dose of the aspirin dose.
The compound powder thus obtained at the end of step 4) is stable. Poured into the water for oral absorption, this compound powder determines the dispersion of the aspirin coated in this reconstituted trisodium citrate-buffered effervescent solution (pH between 5 and 6), resulting in the solubilization of the aspirin grains with, as a result, an improvement in the bioavailability of this aspirin.
The invention also relates to compositions that may be in various packages, more particularly to a composition as obtained at the end of step 3), on the one hand, and in a different package, the alkaline powder defined in Step 4), on the other hand. The contents of the two packages can then be mixed extemporaneously or poured into the water for oral absorption as recalled above.
All of these compositions are very well preserved in the absence of moisture.
The invention also relates to compositions comprising, in addition to the above-mentioned ingredients, lyophilizates of fruit juice allowing the aromatization of the composition. It is important that these freeze-dried products are not kept in a mixture with those containing aspirin.
In the case where the "compound powder" obtained at the end of step 4) above, already in the premixed state, is used, it will be necessary to present the fruit juice powder, in particular orange, in a separate package. On the other hand, in the event that sodium bicarbonate is kept in a separate package, it will also contain, where appropriate, the lyophilisate of fruit juice.
By mixing these different constituents, a dispersed aspirin is thus obtained whose bioavailability is significantly improved, in a flavored form making its absorption more pleasant.
The invention also relates to a surfactant coating method, with sodium dioctylsulfosuccinate, micronised aspirin which, after incorporation into an extemporaneous effervescent mixture, then brought into contact with water, leads to a buffered solution between pH 5 and 6, improved bioavailability. The bioavailability verified in vivo, in humans in a biogalenic center with the coating process below applied to the formula dosed at 300 mg of aspirin, compared to a common commercial formula of aspirin (without surfactant coating ) at the same dosage shows, for the same dose of aspirin, a 30% higher plasma concentration.
Several examples of presentation in one or more packages of the composition according to the invention are presented below.
1st example of presentation of a "powder formula":
To this composition, stable in the absence of moisture, can be combined, especially in a different package, a lyophilisate of fruit juice, especially orange, taken in appropriate proportions to give the effervescent solution obtained, when the The above-mentioned "powder formula" is poured into the water, a pleasant aroma on the palate.
Second presentation (in separate packages) of the main constituents of the composition according to the invention 1st packaging:
optionally, sweet excipient containing a lyophilisate of fruit juice: qs
It goes without saying that the above indications as to the contents of the packaging are not exclusive of the possible presence of other ingredients (excipients or active ingredients) in these packages.
REVENDICATIONS
1. Composition ou forme galénique à base d'acide acétylsalicylique, pour usage en présentation effervescente extemporanée à pH tamponné, de préférence entre des valeurs de pH de 5 à 6, caractérisée en ce qu'elle contient, dans un emballage unique ou dans des emballages distincts : - des particules d'acide acétylsalicylique, ayant notamment des tailles passant au tamis 160 ou 180 microns, enrobées par un agent tensioactif, tel que le dioctylsulfosuccinate de sodium ; - une poudre contenant de l'acide citrique anhydre dans une proportion double de la quantité d'acide acétylsalicylique ; - une poudre alcaline contenant du bicarbonate de sodium dans une proportion triple de la dose d'aspirine. 1. Composition or dosage form based on acetylsalicylic acid, for use in extemporaneous effervescent presentation at pH buffered, preferably between pH values of 5 to 6, characterized in that it contains, in a single package or in separate packages: acetylsalicylic acid particles, especially having sieve sizes of 160 or 180 microns, coated with a surfactant, such as sodium dioctylsulphosuccinate; a powder containing anhydrous citric acid in a double proportion of the amount of acetylsalicylic acid; an alkaline powder containing sodium bicarbonate in a triple proportion of the aspirin dose.
Claims (4)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9308013A FR2708853A1 (en) | 1993-06-30 | 1993-06-30 | Acetylsalicylic acid composition with improved bioavailability and process for producing it |
FR9408109A FR2708852B1 (en) | 1993-06-30 | 1994-06-30 | A composition based on acetylsalicylic acid with improved bioavailability and process for producing it. |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9308013A FR2708853A1 (en) | 1993-06-30 | 1993-06-30 | Acetylsalicylic acid composition with improved bioavailability and process for producing it |
FR9408109A FR2708852B1 (en) | 1993-06-30 | 1994-06-30 | A composition based on acetylsalicylic acid with improved bioavailability and process for producing it. |
Publications (1)
Publication Number | Publication Date |
---|---|
FR2708853A1 true FR2708853A1 (en) | 1995-02-17 |
Family
ID=26230450
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FR9308013A Pending FR2708853A1 (en) | 1993-06-30 | 1993-06-30 | Acetylsalicylic acid composition with improved bioavailability and process for producing it |
FR9408109A Expired - Fee Related FR2708852B1 (en) | 1993-06-30 | 1994-06-30 | A composition based on acetylsalicylic acid with improved bioavailability and process for producing it. |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FR9408109A Expired - Fee Related FR2708852B1 (en) | 1993-06-30 | 1994-06-30 | A composition based on acetylsalicylic acid with improved bioavailability and process for producing it. |
Country Status (1)
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FR (2) | FR2708853A1 (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5723453A (en) * | 1995-11-13 | 1998-03-03 | Health Corporation | Stabilized, water-soluble aspirin composition |
WO2001030949A2 (en) * | 1999-10-28 | 2001-05-03 | The Procter & Gamble Company | Detergent compositions |
ES2189639A1 (en) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Aqueous medicinal composition containing dissolved acid consists of an oral medicine containing acetyl salicylic acid dissolved in water, with additives |
US8580853B2 (en) | 2011-06-13 | 2013-11-12 | Howard PHYKITT | Analgesic composition and method of making the same |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19502789A1 (en) * | 1995-01-28 | 1996-08-01 | Dirk Krischenowski | Medicament contg. analgesic, antacid, and/or vitamin etc. |
ITMI20022619A1 (en) * | 2002-12-11 | 2004-06-12 | Ind Italiana Integratori Trei S P A | PHARMACEUTICAL PREPARATIONS FOR VETERINARY USE CONTAINING ACETYLSALICYLIC ACID IN THE FORM OF SOLUBLE BUFFERED POWDER. |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2073431A1 (en) * | 1969-11-28 | 1971-10-01 | Aspro Nicholas Ltd | |
US3729553A (en) * | 1972-03-17 | 1973-04-24 | Richardson Merrell Inc | Packaged effervescent composition |
FR2239239A1 (en) * | 1973-07-30 | 1975-02-28 | Orinex Laboratoires | Bipocket sachet contg. histidine - which is stable on storage and gives an oral treatment of peptic ulcer |
FR2350102A1 (en) * | 1976-05-05 | 1977-12-02 | Beecham Group Ltd | ANALGESIC PHARMACEUTICAL COMPOSITION |
AT368880B (en) * | 1980-05-02 | 1982-11-25 | Gergely Gerhard | METHOD FOR PRODUCING A WATER-INSOLUBLE DRY INSTRUMENT PRESS [PARATES |
BE893729A (en) * | 1981-07-01 | 1983-01-03 | Bristol Myers Co | PRESSED AND SHAPED ALKALINE CONSTITUENT SUITABLE FOR A BUFFER-BASED ASPIRIN PRODUCT |
WO1986003675A1 (en) * | 1984-12-14 | 1986-07-03 | Gerhard Gergely | Particles from a hydrophobic or poorly soluble substance and process for rendering them hydrophilic |
-
1993
- 1993-06-30 FR FR9308013A patent/FR2708853A1/en active Pending
-
1994
- 1994-06-30 FR FR9408109A patent/FR2708852B1/en not_active Expired - Fee Related
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2073431A1 (en) * | 1969-11-28 | 1971-10-01 | Aspro Nicholas Ltd | |
US3729553A (en) * | 1972-03-17 | 1973-04-24 | Richardson Merrell Inc | Packaged effervescent composition |
FR2239239A1 (en) * | 1973-07-30 | 1975-02-28 | Orinex Laboratoires | Bipocket sachet contg. histidine - which is stable on storage and gives an oral treatment of peptic ulcer |
FR2350102A1 (en) * | 1976-05-05 | 1977-12-02 | Beecham Group Ltd | ANALGESIC PHARMACEUTICAL COMPOSITION |
AT368880B (en) * | 1980-05-02 | 1982-11-25 | Gergely Gerhard | METHOD FOR PRODUCING A WATER-INSOLUBLE DRY INSTRUMENT PRESS [PARATES |
BE893729A (en) * | 1981-07-01 | 1983-01-03 | Bristol Myers Co | PRESSED AND SHAPED ALKALINE CONSTITUENT SUITABLE FOR A BUFFER-BASED ASPIRIN PRODUCT |
WO1986003675A1 (en) * | 1984-12-14 | 1986-07-03 | Gerhard Gergely | Particles from a hydrophobic or poorly soluble substance and process for rendering them hydrophilic |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5723453A (en) * | 1995-11-13 | 1998-03-03 | Health Corporation | Stabilized, water-soluble aspirin composition |
WO2001030949A2 (en) * | 1999-10-28 | 2001-05-03 | The Procter & Gamble Company | Detergent compositions |
WO2001030949A3 (en) * | 1999-10-28 | 2002-02-21 | Procter & Gamble | Detergent compositions |
ES2189639A1 (en) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Aqueous medicinal composition containing dissolved acid consists of an oral medicine containing acetyl salicylic acid dissolved in water, with additives |
US8580853B2 (en) | 2011-06-13 | 2013-11-12 | Howard PHYKITT | Analgesic composition and method of making the same |
Also Published As
Publication number | Publication date |
---|---|
FR2708852B1 (en) | 1996-05-31 |
FR2708852A1 (en) | 1995-02-17 |
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