WO2008045009A2 - Forme posologique pharmaceutique - Google Patents

Forme posologique pharmaceutique Download PDF

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Publication number
WO2008045009A2
WO2008045009A2 PCT/TR2007/000121 TR2007000121W WO2008045009A2 WO 2008045009 A2 WO2008045009 A2 WO 2008045009A2 TR 2007000121 W TR2007000121 W TR 2007000121W WO 2008045009 A2 WO2008045009 A2 WO 2008045009A2
Authority
WO
WIPO (PCT)
Prior art keywords
dosage form
pharmaceutical dosage
form according
pantoprazole
pharmaceutical
Prior art date
Application number
PCT/TR2007/000121
Other languages
English (en)
Other versions
WO2008045009A3 (fr
Inventor
Abdullah Uslu
Original Assignee
Nobel Ilac San. Ve Tic. A.S.
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 Nobel Ilac San. Ve Tic. A.S. filed Critical Nobel Ilac San. Ve Tic. A.S.
Priority to EP07852324A priority Critical patent/EP2086517A2/fr
Publication of WO2008045009A2 publication Critical patent/WO2008045009A2/fr
Publication of WO2008045009A3 publication Critical patent/WO2008045009A3/fr

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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Definitions

  • This present invention relates to a stable pharmaceutical dosage form including pantoprazole active ingredient or pharmaceutical acceptable salt.
  • Pantoprazole which is a proton-pump inhibitor derivative binds to H + , K + ATPaz enzyme and inhibits it by turning into active form in acid environment in parietal cells canal lumen of stomach mucosa. Pantoprazole pressurize both the basal and inhibited the gastric acid secretion by H + , K + ATPaz inhibition. The anti-secretary effect after enzyme inhibition lasts more than 24 hours.
  • pantoprazole active ingredient are used to treat duodenal and gastric peptic ulcer, gastroesophageal reflux disease and reflux esophagi; by the combination of two suitable antibiotics to reduce the replication of duodenal and gastric ulcer which occurs because of Helicobacter pylori.
  • Pantoprazole active ingredient (S)-5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinile), is first disclosed in US patent US4758579.
  • pantoprazole formulations from benzimidazole and the group of benzimidazole is very difficult because of the sensitivity to acidic environment, heat and humidity of the molecules.
  • European Patent application EP0589981 discloses stable pantoprazole formulation. It is stated that in this document commonly used binders and the fillers, such as lactose, microcrystalline cellulose or hydroxypropylcellulose cause stability problems in the pantoprazole formulation. In the same patent is explained that the problem can be solved by using mannitol as filler. European Patent EP0589981 discloses the use of a suitable binder (high molecular weighted binder) preferably PVP and/or hydroxypropylcellulose (HPMC) to obtain the tablet in a desired strength. In addition it is stated in this document that using sodium carbonate as basic material in the formulation. To add basic material in the active ingredient formulations of benzimidazole derivatives is a known technique.
  • the binder which will be used in the stable pharmaceutical compound including pantoprazole should be ' compatible with other ancillary compounds and should have the suitable binding capability to make the tablet in the desired strength.
  • Sodium carboxymethylcellulose is more basic binder than hydroxypropylcellulose and PVP and it is obvious advantage for the formulation especially stability. But, in the patent EP0589981 which mannitol is used as filler, using sodium carboxymethylcellulose as stable making binders is not stated. The binders in this patent are restricted with PVP and hydroxypropylmethylcellulose. The reason for that is the pantoprazole formulation including mannitol does not provide the desired strength values. Although sodium carboxymethylcellulose is more desired than HPMC and PVP for their basic properties, they are not used in the pantoprazole tablet formulations because of the undesired strength values.
  • Another document EP1257256 Bl explains a group filler including mannitol to be used in the pellet formulation.
  • This patent protects filler materials, mannitol, sucrose, fructose, fructo-oligo saccharine, inulin, sorbitol, xylitol, inositol, isomalt and maltodextrin to be used as pellet formulation.
  • this patent does not give any information about neither the usage of these fillers in the pantoprazole formulation nor tablet formulations.
  • the most filler used in this patent causes staining in the pantoprazole formulations.
  • the objective of the present invention is to develop a new pantoprazole tablet formulation having suitable stability values and administrated orally.
  • pantoprazole active ingredient containing subject invention includes pharmaceutical solid dosage form core tablet, an enteric coating and a pre-coating between core tablet and enteric coating.
  • the core tablet includes both sodium carboxymethylcellulose as binder and isomalt as filler.
  • pantoprazole formulation To use isomalt as filler in pantoprazole formulation contribute the production of stable pantoprazole formulation.
  • isomalt filler with sodium carboxymethylcellulose unexpectedly provides the desired core tablet strength values.
  • the core tablet includes also tri-basic sodium phosphate as basic material.
  • the core tablet includes also sodium stearil fumarate as lubricant agent.
  • the protective coating between core tablet and enteric coating consist of Pharmacoat 603, PVP K 25, Sepisperse AP3232, Propylene glycol.
  • the enteric coating includes Eudragit ® , Citroflex and Simeticone Emulsion or Dimethicone Emulsion.
  • pantoprazole formulation The preferred tablet formulation of pantoprazole formulation is explained in Example 1.
  • pantoprazole containing pharmaceutical compound The open formula of the pantoprazole containing pharmaceutical compound is shown above and the production process is given below.
  • the aqueous solution of NaCMC - 7MXF was prepared. Some of tri-basic phosphate was added and the granulation solution was prepared (pH > 10). The pantoprazole sodium sesquihydrate transferred into the wet granulation cauldron and some of crospovidone, isomalt LM-PF, anhydrous tri-basic sodium phosphate and rest of NaCMC — 7MXF were mixed to obtain a suitable mixture. This mixture is granulated by granulation solution in a fluidized bed. Obtained granules, rest of crospovidone and sodium stearate fumarate were mixed and the solid mixture was made tablet by suitable tablet machine. The pre-coating process and then enteric-coating process were made respectively.
  • the tablets were packed in aluminum/aluminum blisters and stored under accelerated stability test conditions of 30 0 C, 65 % relative humidity and 40 0 C, 75 % relative humidity for 6 months and the obtained results are below.

Landscapes

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

Abstract

La présente invention comprenant un ingrédient actif pantoprazole consiste en un comprimé de cœur de forme posologique solide pharmaceutique, un enrobage entérique et un pré-enrobage entre le comprimé de cœur et l'enrobage entérique. Le comprimé de cœur contient l'ingrédient actif pantoprazole conjointement avec de la carboxyméthylcellulose sodique en tant que liant et de l'isomalt en tant que charge.
PCT/TR2007/000121 2006-10-10 2007-10-10 Forme posologique pharmaceutique WO2008045009A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP07852324A EP2086517A2 (fr) 2006-10-10 2007-10-10 Forme posologique pharmaceutique

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2006/05624 2006-10-10
TR2006/05624A TR200605624A2 (tr) 2006-10-10 2006-10-10 Farmasötik dozaj şekli

Publications (2)

Publication Number Publication Date
WO2008045009A2 true WO2008045009A2 (fr) 2008-04-17
WO2008045009A3 WO2008045009A3 (fr) 2008-12-31

Family

ID=39283297

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/TR2007/000121 WO2008045009A2 (fr) 2006-10-10 2007-10-10 Forme posologique pharmaceutique

Country Status (3)

Country Link
EP (1) EP2086517A2 (fr)
TR (1) TR200605624A2 (fr)
WO (1) WO2008045009A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105380919A (zh) * 2015-11-20 2016-03-09 世贸天阶制药（江苏）有限责任公司 一种泮托拉唑钠肠溶片及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996001624A1 (fr) * 1994-07-08 1996-01-25 Astra Aktiebolag Preparation pharmaceutique composite renfermant un inhibiteur de pompe a protons
DE19752843A1 (de) * 1997-11-28 1999-07-01 Byk Gulden Lomberg Chem Fab Arzneimittelzubereitung in Tabletten- oder Pelletform für Pantoprazol und Omeprazol
EP1257256A1 (fr) * 2000-02-17 2002-11-20 Alpharma APS Procede de production de pellets vecteurs de medicaments

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996001624A1 (fr) * 1994-07-08 1996-01-25 Astra Aktiebolag Preparation pharmaceutique composite renfermant un inhibiteur de pompe a protons
DE19752843A1 (de) * 1997-11-28 1999-07-01 Byk Gulden Lomberg Chem Fab Arzneimittelzubereitung in Tabletten- oder Pelletform für Pantoprazol und Omeprazol
EP1257256A1 (fr) * 2000-02-17 2002-11-20 Alpharma APS Procede de production de pellets vecteurs de medicaments

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105380919A (zh) * 2015-11-20 2016-03-09 世贸天阶制药（江苏）有限责任公司 一种泮托拉唑钠肠溶片及其制备方法

Also Published As

Publication number Publication date
TR200605624A2 (tr) 2008-05-21
WO2008045009A3 (fr) 2008-12-31
EP2086517A2 (fr) 2009-08-12

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