FR2797766A1 - Paste in gel form for topical application, containing an anti-inflammatory, an antibiotic or a phlebotonic - Google Patents
Paste in gel form for topical application, containing an anti-inflammatory, an antibiotic or a phlebotonic Download PDFInfo
- Publication number
- FR2797766A1 FR2797766A1 FR9915677A FR9915677A FR2797766A1 FR 2797766 A1 FR2797766 A1 FR 2797766A1 FR 9915677 A FR9915677 A FR 9915677A FR 9915677 A FR9915677 A FR 9915677A FR 2797766 A1 FR2797766 A1 FR 2797766A1
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- Prior art keywords
- product
- pasty consistency
- inflammatory
- active ingredient
- gel
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Classifications
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Inorganic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
L'invention s'adresse au domaine de la chimie thérapeutique, et notamment à de nouvelles formulations galéniques. The invention is directed to the field of therapeutic chemistry, and in particular to new galenic formulations.
L'invention s'adresse plus précisément à de nouvelles formes topiques à consistance pâteuse destinées à être appliquées sur la peau et les muqueuses. The invention is more specifically directed to new topical forms with a pasty consistency intended to be applied to the skin and the mucous membranes.
L'administration de médicaments par la voie topique présente une grande importance soit pour des raisons de commodité d'application en un point, soit pour limiter les phénomènes de résorption et de passage systémique. C'est le cas des médicaments anti- inflammatoires, des médicaments antalgiques à visée locale, des antibiotiques ou des médicaments cicatrisants ou antiseptiques. Ceci vient du fait que le thérapeute cherche à traiter les affections qui touchent les muqueuses et la peau à l'emplacement précis de l'affection et a pour préoccupation l'aspect local du traitement. En effet, beaucoup d'affections qui touchent la peau et les muqueuses doivent être traitées localement et un traitement général ne s'impose pas. The administration of drugs by the topical route is of great importance either for reasons of convenience of application at a point, or to limit the phenomena of resorption and systemic passage. This is the case of anti-inflammatory drugs, local analgesic drugs, antibiotics or healing or antiseptic drugs. This is because the therapist seeks to treat conditions affecting the mucous membranes and skin at the precise location of the condition and is concerned with the local aspect of the treatment. Indeed, many conditions affecting the skin and mucous membranes must be treated locally and general treatment is not required.
Cependant, l'administration d'un médicament par voie topique pose des problèmes souvent difficiles de formulation. Il est important de déterminer si la préparation doit être grasse ou non grasse, doit être épaisse ou fluide, doit pénétrer dans le derme et dans quelle proportion... La forme galénique qui en résultera présentera alors une présentation différente. However, the administration of a drug topically poses often difficult problems of formulation. It is important to determine if the preparation should be fat or non-oily, should be thick or fluid, must penetrate into the dermis and in what proportion ... The resulting dosage form will then present a different presentation.
Le problème qui se pose est aussi celui de la quantité administrée qui doit pouvoir être déterminée et mesurée avec suffisamment de précision. Précédemment, les notices d'utilisation faisaient état de l'application d'une noix du médicament mais malheureusement ce terme est beaucoup trop imprécis pour pouvoir demeurer. A l'heure actuelle, le thérapeute a besoin de connaître la dose administrée et d'être assuré que le patient appliquera la dose prescrite. I1 est donc important que les formes galéniques topiques présentent une composition, une fluidité, une viscosité ou une rhéologie qui permettent une application aisée sur la peau. II faut en outre que la forme galénique présente une rhéologie qui autorise la distribution à l'aide d'un dispositif qui délivre à chaque fois un volume déterminé des formes galéniques tout en assurant une parfaite conservation du médicament. The problem that arises is also that of the quantity administered which must be able to be determined and measured with sufficient precision. Previously, the instructions for use reported the application of a nut of the drug but unfortunately this term is far too imprecise to stay. At present, the therapist needs to know the dose administered and to be assured that the patient will apply the prescribed dose. It is therefore important that the topical dosage forms have a composition, fluidity, viscosity or rheology that allows easy application to the skin. It is further necessary that the dosage form has a rheology that allows the distribution with the aid of a device that delivers each time a specific volume of dosage forms while ensuring a perfect preservation of the drug.
Une première approche de ce problème a été réalisée avec les formulations sous pression d'un gaz propulseur. Cette formulation présente cependant le problème de l'homogénéité de la préparation et de la mise en solution de la préparation dans le gaz propulseur. En outre, l'utilisation comme gaz propulseur des fluorocarbures ou des chloro- fluorocarbures n'a pas permis de résoudre ce problème et en a ajouté d'autres liés à l'environnement. A first approach to this problem has been made with the pressurized formulations of a propellant gas. This formulation, however, has the problem of the homogeneity of the preparation and the dissolution of the preparation in the propellant gas. In addition, the use of fluorocarbons or chlorofluorocarbons as a propellant did not solve this problem and added others related to the environment.
L'utilisation de gaz propulseurs inertes comme l'azote, le gaz carbonique ou l'oxyde d'azote, n'a pas permis davantage de résoudre le problème, car la pression est faible ou inconstante à l'intérieur du réservoir et les fuites de gaz par les valves amènent une réduction de la pression interne. The use of inert propellant gases such as nitrogen, carbon dioxide or nitrogen oxide has not further solved the problem because the pressure is low or inconsistent inside the tank and leaks of gas through the valves cause a reduction of the internal pressure.
II était donc nécessaire de mettre au point un dispositif de distribution qui permette avec sécurité de délivrer une quantité déterminée de préparation topique, de ne pas dégager dans l'atmosphère de gaz nocifs pour l'environnement et qui utilise la pression de l'air pour faire sortir la préparation aussi longtemps qu'il reste de la préparation dans le tube réservoir. It was therefore necessary to develop a dispensing device that was safe enough to deliver a certain quantity of topical preparation, not to release into the atmosphere gases harmful to the environment and that used the air pressure to take the preparation out as long as there is some preparation in the reservoir tube.
Le produit selon l'invention distribué par un tel dispositif est une préparation visqueuse et de préférence un gel contenant comme principe actif un médicament et en particulier un agent anti-inflammatoire de la série des acides arylacétiques. L'excipient est de préférence un agent gélifiant formé par un carbomère et notamment le Carbopol 940 commercialisé par la société Goodrich A.F, en solution aqueuse et un agent alcalinisant tel qu'une amine secondaire ou tertiaire comme par exemple la diéthanolamine ou la triéthanolamine. Le gel contient encore un agent solubilisant comme un alkanol pour maintenir le principe actif en solution et un agent parfumant pour rendre agréable l'application du produit. L'agent parfumant sera de préférence une essence de fleurs comme par exemple l'essence de roses, l'essence de thym, l'essence de romarin, l'essence d'ylang-ylang, l'essence de lavande ou l'essence de lavandin. The product according to the invention dispensed by such a device is a viscous preparation and preferably a gel containing as active ingredient a drug and in particular an anti-inflammatory agent of the series of arylacetic acids. The excipient is preferably a gelling agent formed by a carbomer and in particular Carbopol 940 sold by the company Goodrich A.F, in aqueous solution and an alkalinizing agent such as a secondary or tertiary amine such as diethanolamine or triethanolamine. The gel still contains a solubilizing agent such as an alkanol to maintain the active ingredient in solution and a perfuming agent to make the application of the product pleasant. The perfuming agent will preferably be a flower essence such as, for example, rose oil, thyme oil, rosemary oil, ylang-ylang oil, lavender oil or gasoline. of lavandin.
La préparation galénique contient de 20 à 50 mg de principe actif par dose distribuée. De préférence, la dose distribuée sera de 1,2 g de gel correspondant à 30 mg de principe actif. La posologie est de 3 à 12 doses administrées en 2 à 3 applications par jour en fonction des indications. The pharmaceutical preparation contains from 20 to 50 mg of active ingredient per dispensed dose. Preferably, the dispensed dose will be 1.2 g of gel corresponding to 30 mg of active ingredient. The dosage is from 3 to 12 doses administered in 2 to 3 applications per day depending on the indications.
# Entorses, contusions, veinites, post-sclérothérapie en cas de réaction inflammatoire intense : 3 doses par jour # Tendinites superficielles : 6 doses par jour, # Arthrose des petites articulations : 9 doses par jour # Lombalgie aigtie : 12 doses par jour les premiers jours puis 8 doses par jour. # Sprains, bruises, veinitis, post-sclerotherapy in case of intense inflammatory reaction: 3 doses per day # Superficial tendinitis: 6 doses per day, # Small joint osteoarthritis: 9 doses per day # Acute low back pain: 12 doses per day first days then 8 doses a day.
Parmi les principes actifs incorporés dans le gel, on citera plus particulièrement les agents anti-inflammatoires du type acide arylacétique, en particulier un acide phénylacétique et plus précisément l'acide 3-benzoyl a-méthylbenzéneacétique (ou kétoprofène) ou l'un de ses sels avec une base minérale ou organique ou l'un de ses épimères, ou encore le Diclofénac et ses sels ou l'ibuprofène sous forme racémique ou optiquement active ou l'acide tiaprofénique. Among the active ingredients incorporated in the gel, mention will be made more particularly of anti-inflammatory agents of the arylacetic acid type, in particular a phenylacetic acid and more specifically 3-benzoyl a-methylbenzeneacetic acid (or ketoprofen) or one of its salts with a mineral or organic base or one of its epimers, or Diclofenac and its salts or ibuprofen in racemic or optically active form or tiaprofenic acid.
D'autres principes actifs comme les antibiotiques (erythromycine, miocamycine), des anti-inflammatoires du type oxicam (isoxicam, piroxicam, tenoxicam) ou des phlébotoniques (diosmine, escine, troxerutine) peuvent également être incorporés dans ce gel. Other active ingredients such as antibiotics (erythromycin, miocamycin), anti-inflammatories such as oxicam (isoxicam, piroxicam, tenoxicam) or phlebotonics (diosmin, escin, troxerutin) can also be incorporated in this gel.
La masse de produit disposée dans le réservoir cylindrique peut varier de 50 à<B>150</B> g et plus précisément de 60 à 100 g. Le volume du réservoir cylindrique varie en général de 140 à 150 g.The mass of product disposed in the cylindrical reservoir may vary from 50 to 150 g, and more specifically from 60 to 100 g. The volume of the cylindrical reservoir generally varies from 140 to 150 g.
Claims (8)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9915677A FR2797766B1 (en) | 1999-08-27 | 1999-12-13 | NEW TOPICAL FORMS WITH A PASTY CONSISTENCY IN THE FORM OF A GEL DISTRIBUTED IN DOSES |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9910871A FR2797854B1 (en) | 1999-08-27 | 1999-08-27 | DISPENSING DEVICE FOR TOPICAL FORMS WITH PASTY CONSISTENCY |
FR9915677A FR2797766B1 (en) | 1999-08-27 | 1999-12-13 | NEW TOPICAL FORMS WITH A PASTY CONSISTENCY IN THE FORM OF A GEL DISTRIBUTED IN DOSES |
Publications (2)
Publication Number | Publication Date |
---|---|
FR2797766A1 true FR2797766A1 (en) | 2001-03-02 |
FR2797766B1 FR2797766B1 (en) | 2003-04-04 |
Family
ID=26235089
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FR9915677A Expired - Lifetime FR2797766B1 (en) | 1999-08-27 | 1999-12-13 | NEW TOPICAL FORMS WITH A PASTY CONSISTENCY IN THE FORM OF A GEL DISTRIBUTED IN DOSES |
Country Status (1)
Country | Link |
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FR (1) | FR2797766B1 (en) |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BE886486A (en) * | 1979-12-05 | 1981-04-01 | Menarini Sas | PHARMACEUTICAL FORM "GEL" CONTAINING 2- (3-BENZOYL-PHENYL) -PROPIONIC ACID AND ITS USE IN THERAPEUTICS FOR LOCAL USE |
EP0338291A1 (en) * | 1988-04-21 | 1989-10-25 | American Cyanamid Company | Antiinflammatory Gel |
EP0479518A1 (en) * | 1990-10-01 | 1992-04-08 | Diomed Developments Limited | Compositions for topical application |
US5196410A (en) * | 1986-10-31 | 1993-03-23 | Pfizer Inc. | Transdermal flux enhancing compositions |
US5436241A (en) * | 1994-01-14 | 1995-07-25 | Bristol-Myers Squibb Company | Topical anti-inflammatory compositions containing piroxicam |
WO1998055113A1 (en) * | 1997-06-04 | 1998-12-10 | Laboratorios Menarini S.A. | Semisolid pharmaceutical formulation containing dexketoprofen trometamol |
-
1999
- 1999-12-13 FR FR9915677A patent/FR2797766B1/en not_active Expired - Lifetime
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BE886486A (en) * | 1979-12-05 | 1981-04-01 | Menarini Sas | PHARMACEUTICAL FORM "GEL" CONTAINING 2- (3-BENZOYL-PHENYL) -PROPIONIC ACID AND ITS USE IN THERAPEUTICS FOR LOCAL USE |
US5196410A (en) * | 1986-10-31 | 1993-03-23 | Pfizer Inc. | Transdermal flux enhancing compositions |
EP0338291A1 (en) * | 1988-04-21 | 1989-10-25 | American Cyanamid Company | Antiinflammatory Gel |
EP0479518A1 (en) * | 1990-10-01 | 1992-04-08 | Diomed Developments Limited | Compositions for topical application |
US5436241A (en) * | 1994-01-14 | 1995-07-25 | Bristol-Myers Squibb Company | Topical anti-inflammatory compositions containing piroxicam |
WO1998055113A1 (en) * | 1997-06-04 | 1998-12-10 | Laboratorios Menarini S.A. | Semisolid pharmaceutical formulation containing dexketoprofen trometamol |
Non-Patent Citations (1)
Title |
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"VIDAL 1997", XP002138765 * |
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Publication number | Publication date |
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FR2797766B1 (en) | 2003-04-04 |
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