WO2008089774A1 - Formulation of an orodispersible tablet based on coated paracetamol - Google Patents
Formulation of an orodispersible tablet based on coated paracetamol Download PDFInfo
- Publication number
- WO2008089774A1 WO2008089774A1 PCT/DZ2007/000003 DZ2007000003W WO2008089774A1 WO 2008089774 A1 WO2008089774 A1 WO 2008089774A1 DZ 2007000003 W DZ2007000003 W DZ 2007000003W WO 2008089774 A1 WO2008089774 A1 WO 2008089774A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- paracetamol
- formulation
- orodispersible tablet
- orodispersible
- coated
- Prior art date
Links
Classifications
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5015—Organic compounds, e.g. fats, sugars
Definitions
- the invention relates to the formulation of an orodispersible tablet based on the active ingredient paracetamol acid coated at various doses.
- Paracetamol has analgesic and antipyretic effects that do not differ significantly from those of aspirin, although it has only a weak anti-inflammatory effect. Minor metabolites contribute significantly to the toxic actions of paracetamol. The pharmacological properties of paracetamol have been reviewed by clissold (1986). In addition, paracetamol does not inhibit neutrophil activation as do NSAIDs.
- paracetamol Whether administered as a single or repeated dose, paracetamol has no action on the cardiovascular and respiratory system. It does not cause acid-base changes, gastric irritation, erosion or bleeding, as may occur after administration of salicylate.O it also has no action on platelets, bleeding time and excretion of uric acid. Paracetamol is known for its following properties: • Paracetamol is an analgesic and antipyretic - Analgesic action
- Paracetamol has an analgesic activity of intensity comparable to that of acetylsalicylic acid and relieves the same type of pain: headache, pain of muscular or articular origin, neuralgia. Unlike salicylates paracetamol lacks anti-inflammatory properties and its analgesic action seems isolated. - Antipyretic action:
- coated paracetamol active ingredient exists in the orodispersible tablet form but its manufacturing formula is rather complicated and involves several disintegrating agents and a conventional flavoring agent (mint flavoring).
- Paracetamol coated at dosages of 80 mg and 160 mg does not exist in the domestic market.
- the object of the invention is to formulate a paracetamol-based orodispersible tablet coated at various doses: 80 mg and 160 mg using a matrix composed of a mixture of powders based on mannitol, sorbitol, crospovidone and silica for rapid disintegration.
- the present invention provides the formulation of an orodispersible tablet containing paracetamol coated at dosages: 80 mg and 160 mg.
- the formulated orodispersible tablet is based on (25-35)% of active ingredient (coated paracetamol), (50-80)% of mannitol,
- sorbitol (20-30)% sorbitol, (2-20)% crospovidone, (0.1 to 10)% colloidal silica, (1-5)% sodium saccharin, (1-5)% citric acid monohydrate ( 0.1-5) strawberry flavor (80 mg dosage) and orange flavoring (160 mg dosage), (0.1-2)% sun-lacquer coloring (160 mg dosage) and erythrosine lacquer dye (80 mg dosage) and (0.5 -4)% stearyl sodium fumarate.
- a powder mixture is made by mixing all the raw materials with the exception of the lubricant which is sodium stearyl fumarate for a time sufficient to obtain a mixture. homogeneous then the lubricant is added and a remixing is performed for a specified time.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to the formulation of an orodispersible tablet based on the active ingredient coated paracetamol acid with different dosages.
Description
FORMULATION D'UN COMPRIME ORODISPERSIBLE A BASE DE PARACETAMOL FORMULATION OF ORODISPERSIBLE COMPRESSOR BASED ON PARACETAMOL
ENROBE Domaine technique auquel se rapporte l' invention L'invention concerne la formulation d'un comprimé orodispersible à base du principe actif acide paracétamol enrobé à différents dosagesThe invention relates to the formulation of an orodispersible tablet based on the active ingredient paracetamol acid coated at various doses.
Le paracétamol a des effets analgésiques et antipyrétiques qui ne diffèrent pas de manière significative de ceux de l'aspirine, bien qu'il n'ait qu'une faible action anti-inflammatoire. Les métabolites mineurs contribuent significativement aux actions toxiques du paracétamol. Les propriétés pharmacologiques du paracétamol ont été passées en revue par clissold (1986). De plus, le paracétamol n'inhibe pas l'activation des neutrophiles comme le font les AINS.Paracetamol has analgesic and antipyretic effects that do not differ significantly from those of aspirin, although it has only a weak anti-inflammatory effect. Minor metabolites contribute significantly to the toxic actions of paracetamol. The pharmacological properties of paracetamol have been reviewed by clissold (1986). In addition, paracetamol does not inhibit neutrophil activation as do NSAIDs.
Qu'il soit administré en dose unique ou répétée, le paracétamol n'a pas d'action sur le système cardio - vasculaire et respiratoire. Il ne provoque pas de modifications acido- basiques, ni d'irritation gastrique, érosion ou saignement, comme cela peut arriver après administration de salicylate.O il n'a pas non plus d'action sur les plaquettes, le temps de saignement et l'excrétion d'acide urique. Le paracétamol est connu pour ses propriétés suivantes : • Le paracétamol est un analgésique et un antipyrétique - Action analgésiqueWhether administered as a single or repeated dose, paracetamol has no action on the cardiovascular and respiratory system. It does not cause acid-base changes, gastric irritation, erosion or bleeding, as may occur after administration of salicylate.O it also has no action on platelets, bleeding time and excretion of uric acid. Paracetamol is known for its following properties: • Paracetamol is an analgesic and antipyretic - Analgesic action
Le paracétamol a une activité analgésique d'intensité comparable à celle de l'acide acétylsalicylique et soulage le même type de douleurs : céphalées, douleurs d'origine musculaire ou articulaire, névralgies. Contrairement aux salicylés le paracétamol est dépourvu de propriétés anti-inflammatoires et son action analgésique paraît isolée. - Action antipyrétique :Paracetamol has an analgesic activity of intensity comparable to that of acetylsalicylic acid and relieves the same type of pain: headache, pain of muscular or articular origin, neuralgia. Unlike salicylates paracetamol lacks anti-inflammatory properties and its analgesic action seems isolated. - Antipyretic action:
Comme dans le cas des salicylés, l'action antipyrétique du paracétamol provient d'un accroissement de la thermolyse, d'origine hypothalamique .
L' inhibition de la synthèse des prostaglandines centrales paraît être le mécanisme responsable, le paracétamol déprimant cette synthèse aussi efficacement que les salicylés.As in the case of salicylates, the antipyretic action of paracetamol results from an increase in thermolysis, of hypothalamic origin. Inhibition of central prostaglandin synthesis appears to be the mechanism responsible, paracetamol depressing this synthesis as effectively as salicylates.
Etat de la technique antérieureState of the art
Le principe actif paracétamol enrobé existe sous la forme comprimé orodispersible par contre sa formule de fabrication est assez compliquée et fait intervenir plusieurs agents désintégrants et un aromatisant classique (arôme menthe)The coated paracetamol active ingredient exists in the orodispersible tablet form but its manufacturing formula is rather complicated and involves several disintegrating agents and a conventional flavoring agent (mint flavoring).
Le paracétamol enrobé aux dosages de 80 mg et 160 mg n'existe pas sur le marché national.Paracetamol coated at dosages of 80 mg and 160 mg does not exist in the domestic market.
But de l' invention Le but de l'invention est de formuler un comprimé orodispersible à base de paracétamol enrobé à différents dosages : 80 mg et 160 mg en utilisant une matrice composée d'un mélange de poudres à base de mannitol, sorbitol, crospovidone et de silice pour la désintégration rapide.OBJECT OF THE INVENTION The object of the invention is to formulate a paracetamol-based orodispersible tablet coated at various doses: 80 mg and 160 mg using a matrix composed of a mixture of powders based on mannitol, sorbitol, crospovidone and silica for rapid disintegration.
Présentation de l'essence (la substance) de l'invention La présente invention propose la formulation d'un comprimé orodispersible à base de paracétamol enrobé aux dosages : 80mg et 160 mg. Le comprimé orodispersible formulé est à base de (25-35)% de principe actif (paracétamol enrobé) , (50-80) % de mannitol,Presentation of the Essence (the Substance) of the Invention The present invention provides the formulation of an orodispersible tablet containing paracetamol coated at dosages: 80 mg and 160 mg. The formulated orodispersible tablet is based on (25-35)% of active ingredient (coated paracetamol), (50-80)% of mannitol,
(20-30) % de sorbitol, (2-20)% de crospovidone, (0.1 à 10) % de silice colloïdale, (1-5) % de saccharinate de sodium, (1-5) % de acide citrique monohydrate (0.1-5) d'arôme fraise (dosage 80 mg) et arôme orange (dosage 160 mg) , (0.1-2) % de colorant laque soleil (dosage 160 mg) et de colorant laque érythrosine (dosage 80 mg) et (0.5-4) % de stéaryle Fumarate de sodium. Le procédé de fabrication étant classique, un mélange de poudre est effectué en mélangeant la totalité des matières premières à l'exception du lubrifiant qui est le stéaryle fumarate de sodium pendant un temps suffisant pour l'obtention d'un mélange
homogène puis le lubrifiant est rajouté et un remélange est effectué pendant un temps indiqué.
(20-30)% sorbitol, (2-20)% crospovidone, (0.1 to 10)% colloidal silica, (1-5)% sodium saccharin, (1-5)% citric acid monohydrate ( 0.1-5) strawberry flavor (80 mg dosage) and orange flavoring (160 mg dosage), (0.1-2)% sun-lacquer coloring (160 mg dosage) and erythrosine lacquer dye (80 mg dosage) and (0.5 -4)% stearyl sodium fumarate. As the manufacturing method is conventional, a powder mixture is made by mixing all the raw materials with the exception of the lubricant which is sodium stearyl fumarate for a time sufficient to obtain a mixture. homogeneous then the lubricant is added and a remixing is performed for a specified time.
Claims
1. La forme comprimé orodispersible appliquée au principe actif paracétamol enrobé aux dosages 80 mg et 160 mg.1. The orodispersible tablet form applied to the active ingredient paracetamol coated at dosages 80 mg and 160 mg.
2. Composition pharmaceutique selon la revendication 1 caractérisée en ce qu'elle se présente sous forme des comprimés orodispersibles .2. Pharmaceutical composition according to claim 1 characterized in that it is in the form of orodispersible tablets.
3. La formule de fabrication selon la revendication 2 qui est à base d'une matrice composée d'un mélange de poudres composé de mannitol, sorbitol, crospovidone et silice, (permettant la désintégration rapide) .3. The manufacturing formula according to claim 2 which is based on a matrix composed of a mixture of powders composed of mannitol, sorbitol, crospovidone and silica, (allowing rapid disintegration).
4. Composition pharmaceutique selon la revendication 3 caractérisée en ce qu'elle comprend également un ou plusieurs édulcorant un lubrifiant et un arôme.4. Pharmaceutical composition according to claim 3 characterized in that it also comprises one or more sweetener a lubricant and a flavor.
5. Comprimés orodispersibles selon la revendication 4 caractérisés en ce qu'ils sont obtenus par compression directe 5. orodispersible tablets according to claim 4, characterized in that they are obtained by direct compression
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/DZ2007/000003 WO2008089774A1 (en) | 2007-01-22 | 2007-01-22 | Formulation of an orodispersible tablet based on coated paracetamol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/DZ2007/000003 WO2008089774A1 (en) | 2007-01-22 | 2007-01-22 | Formulation of an orodispersible tablet based on coated paracetamol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2008089774A1 true WO2008089774A1 (en) | 2008-07-31 |
Family
ID=38310007
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/DZ2007/000003 WO2008089774A1 (en) | 2007-01-22 | 2007-01-22 | Formulation of an orodispersible tablet based on coated paracetamol |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2008089774A1 (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001000178A1 (en) * | 1999-06-29 | 2001-01-04 | Takeda Chemical Industries, Ltd. | Tablets quickly disintegrating in mouth |
| US20020022057A1 (en) * | 2000-08-17 | 2002-02-21 | Battey Alyce S. | Oral delivery of pharmaceuticals via encapsulation |
| WO2004069135A2 (en) * | 2003-02-05 | 2004-08-19 | Ethypharm | Composition comprising a mixture of active principles, and method of preparation |
| CN1559390A (en) * | 2004-02-27 | 2005-01-05 | 中奇制药技术（石家庄）有限公司 | Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor |
| CN1732938A (en) * | 2005-08-31 | 2006-02-15 | 上海医药(集团)有限公司 | Orally integrating tablet of compound paracetamol |
-
2007
- 2007-01-22 WO PCT/DZ2007/000003 patent/WO2008089774A1/en active Application Filing
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001000178A1 (en) * | 1999-06-29 | 2001-01-04 | Takeda Chemical Industries, Ltd. | Tablets quickly disintegrating in mouth |
| US20020022057A1 (en) * | 2000-08-17 | 2002-02-21 | Battey Alyce S. | Oral delivery of pharmaceuticals via encapsulation |
| WO2004069135A2 (en) * | 2003-02-05 | 2004-08-19 | Ethypharm | Composition comprising a mixture of active principles, and method of preparation |
| CN1559390A (en) * | 2004-02-27 | 2005-01-05 | 中奇制药技术（石家庄）有限公司 | Oral disintegration tablets contg. p-acetaminophenol, and prepn. method therefor |
| CN1732938A (en) * | 2005-08-31 | 2006-02-15 | 上海医药(集团)有限公司 | Orally integrating tablet of compound paracetamol |
Non-Patent Citations (1)
| Title |
|---|
| ABDELBARY G ET AL: "Determination of the in vitro disintegration profile of rapidly disintegrating tablets and correlation with oral disintegration", INTERNATIONAL JOURNAL OF PHARMACEUTICS, AMSTERDAM, NL, vol. 292, no. 1-2, 23 March 2005 (2005-03-23), pages 29 - 41, XP004752468, ISSN: 0378-5173 * |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU720132B2 (en) | Pharmaceutical compositions | |
| Ali et al. | Some phytochemical, pharmacological and toxicological properties of ginger (Zingiber officinale Roscoe): a review of recent research | |
| JP6210872B2 (en) | Pharmaceutical composition 2 containing loxoprofen | |
| US20040219240A1 (en) | Anti-inflammatory pharmaceutical compositions for reducing inflammation and the treatment or prevention of gastric toxicity | |
| KR0145739B1 (en) | Effervescent tablet | |
| JP2009534462A (en) | Novel low dose pharmaceutical composition containing nimesulide, its preparation and use | |
| AU2015220913B2 (en) | Compositions containing extracts of Curcuma Longa and Echinacea angustifolia which are useful to reduce peripheral inflammation and pain | |
| Bashyal | Ibuprofen and its different analytical and manufacturing methods: a review | |
| FR2717388A1 (en) | Sustained release galenic forms of alfuzosin hydrochloride. | |
| FR2735369A1 (en) | PHARMACEUTICAL COMPOSITIONS BASED ON SODIUM SALT OF DICLOFENAC AND THIOCOLCHICOSIDE | |
| Ponce-Monter et al. | Spasmolytic and anti-inflammatory effects of Aloysia triphylla and citral, in vitro and in vivo studies | |
| KR20080034166A (en) | Organoleptically acceptable ibuprofen oral dosage formulations, methods of making and using the same | |
| JPH1036269A (en) | Drug for reducing dysmenorrhoe and/or syndrome before menstruation | |
| AU2004283065B2 (en) | Anti-inflammatory pharmaceutical compositions for reducing inflammation and the treatment or prevention of gastric toxicity | |
| Bernareggi | Clinical pharmacokinetics and metabolism of nimesulide | |
| US7807203B2 (en) | Anti-inflammatory pharmaceutical compositions for reducing inflammation and the treatment or prevention of gastric toxicity | |
| WO2008089774A1 (en) | Formulation of an orodispersible tablet based on coated paracetamol | |
| RU2589507C1 (en) | Agent based on dry motherwort extract and method for production thereof | |
| WO2019098983A1 (en) | Combinations of diclofenac, h2 receptor antagonists and alkali metal bicarbonates for the treatment of pain and inflammation | |
| JP2004010611A (en) | Masking composition | |
| JP7229012B2 (en) | Pharmaceutical composition for internal use | |
| Soni et al. | Evaluation of analgesic, anti-inflammatory and ulcerogenic liability of oral solution (syrup) formulation developed by novel mixed solvency concept | |
| RU2155033C1 (en) | Soluble sparkling therapeutic composition | |
| US20160346249A1 (en) | Use of amitifadine, (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane in methods and compositions with enhanced efficacy and reduced metabolic side effects and toxicity for treatment of depression and other central nervous system disorders and conditions affected by monoamine neurotransmitters | |
| WO2023128991A1 (en) | Inhibitory effects of standardized extracts of taraxacum officinale aerial parts on cox-1, cox-2 and lox enzymes |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 07702540 Country of ref document: EP Kind code of ref document: A1 |
|
| NENP | Non-entry into the national phase |
Ref country code: DE |
|
| 122 | Ep: pct application non-entry in european phase |
Ref document number: 07702540 Country of ref document: EP Kind code of ref document: A1 |