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WO1997033569A1 - Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace) - Google Patents

Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace) Download PDF

Info

Publication number
WO1997033569A1
WO1997033569A1 PCT/EP1996/001062 EP9601062W WO9733569A1 WO 1997033569 A1 WO1997033569 A1 WO 1997033569A1 EP 9601062 W EP9601062 W EP 9601062W WO 9733569 A1 WO9733569 A1 WO 9733569A1
Authority
WO
WIPO (PCT)
Prior art keywords
pellets
form according
dosage form
release dosage
dissolve
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.)
Ceased
Application number
PCT/EP1996/001062
Other languages
German (de)
English (en)
Inventor
Günter Cordes
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.)
Labtec Gesellschaft fuer Technologische Forschung und Entwicklung mbH
Labtec GmbH
Original Assignee
Labtec Gesellschaft fuer Technologische Forschung und Entwicklung mbH
Labtec GmbH
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 Labtec Gesellschaft fuer Technologische Forschung und Entwicklung mbH, Labtec GmbH filed Critical Labtec Gesellschaft fuer Technologische Forschung und Entwicklung mbH
Priority to PCT/EP1996/001062 priority Critical patent/WO1997033569A1/fr
Priority to AU51074/96A priority patent/AU5107496A/en
Publication of WO1997033569A1 publication Critical patent/WO1997033569A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs

Definitions

  • Angiotensin converting enzyme (ACE) inhibitors have been used for many years to treat hypertension and heart failure.
  • the medicinal preparations with ACE inhibitors, and here in particular captopril are usually tablets which release the active ingredient quickly without a particular delay. So these are not slow release preparations.
  • the ACE inhibitors, and here in particular the captril in particular can lead to side effects if the plasma level floods rapidly, as is the case after normally releasing medicinal preparations, e.g. a sharp drop in blood pressure, which is undesirable to this extent. For this reason, one has already started to divide the daily dose into 2-3 individual doses. In this way, one avoided a larger plasma level peak and converted it into 2 or 3 smaller peaks.
  • the ACE inhibitor in particular the captopril
  • the ACE inhibitor can be mixed with an acidic substance that is physiologically harmless in a ratio of about 1: 1, and after the addition of other auxiliaries, small spheres, so-called pellets, can be formed that have a diameter about 0.6 - 1.8 mm.
  • the production is preferably carried out by the so-called Marumerizer process, with an extrudate being produced first, which is then produced a rotating plate is converted to pellets.
  • small neutral particles such as nonpareills
  • the mixture of active ingredient such as captopril
  • the acidic substance is applied. This order is carried out in a coated tablet or in a fluidized bed apparatus.
  • the active ingredient-containing pellets can be divided into 4 different fractions.
  • Fraction 1 can be left untreated or coated with a thin film protecting against moisture during manufacture and storage.
  • Fraction 2 can, if necessary after coating the same film as in 1, be coated with another film which can dissolve at a pH of about 5.0 - 5.5.
  • Fraction 3, if necessary after application of the same film as in 1. can be coated with a coating which can dissolve at a pH of 5.5-6 and fraction 4, if necessary after application of the same film as in 1st, with a coating that dissolves at pH 6.6 - 7.
  • Acrylates can be used as coatings, e.g.
  • Eudragit® types from R ⁇ HM, Darmstadt, or ethyl cellulose or hydroxypropylmethyl cellulose as phthalate or in the form of the acetate / succinate, e.g. the AQOAT ⁇ types from SHINETSU, Japan, sold in Germany by SYNTAPHARM.
  • Eudragit 30D from Röhm can also be used as a coating.
  • the pellets are coated in drag pots or in fluidized-bed apparatuses, for example as are commercially available from the companies GLATT or HÜTTLIN.
  • the pellets are dried at 40 ° C. over a period of 24 hours. The remaining residual moisture is determined, provided that this is above 0.2%, drying is continued at 40 ° C. The pellets are then passed through a sieve with a mesh size of 1.2 mm, excess portions are removed, and smaller components are sieved through a sieve with a mesh size of 0.6 mm.
  • the apparatus was removed and divided into 4 equal parts by weight. The first faction is set aside. The second fraction is coated in the fluidized bed system with the following solution:
  • each capsule contains enough pellets to correspond to 50 mg captopril. In this example it was 362 mg / capsule.
  • each capsule contains enough pellets to correspond to 50 mg captopril.
  • captopril prepared in this way according to the invention over normal, commercially available tablets or dragées results from the release of the active substance over time. This is determined using the following method: Release principle of analysis
  • volume withdrawal 10.0 ml (with prefilter Hanson sample filters
  • the stock solution (pH 1) can be kept for a maximum of 1 day.

Landscapes

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

Abstract

L'invention concerne un procédé de préparation de formes à effet retard à administration par voie orale contenant pour principe actif du captopril.
PCT/EP1996/001062 1996-03-13 1996-03-13 Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace) Ceased WO1997033569A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/EP1996/001062 WO1997033569A1 (fr) 1996-03-13 1996-03-13 Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace)
AU51074/96A AU5107496A (en) 1996-03-13 1996-03-13 Medicament preparation for angiotensin converting enzyme (ace)-inhibitors

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP1996/001062 WO1997033569A1 (fr) 1996-03-13 1996-03-13 Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace)

Publications (1)

Publication Number Publication Date
WO1997033569A1 true WO1997033569A1 (fr) 1997-09-18

Family

ID=8166177

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/001062 Ceased WO1997033569A1 (fr) 1996-03-13 1996-03-13 Preparation medicamenteuse pour inhibiteurs de l'enzyme de conversion de l'angiotensine (ace)

Country Status (2)

Country Link
AU (1) AU5107496A (fr)
WO (1) WO1997033569A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19625201A1 (de) * 1996-06-24 1998-01-08 Hans Peter Buerkle Darreichungsform für einen Wirkstoff
WO2009087483A3 (fr) * 2007-11-08 2009-10-22 Glaxo Group Limited Préparations pharmaceutiques
CN107213138A (zh) * 2017-08-07 2017-09-29 北京罗诺强施医药技术研发中心有限公司 定时释放药物治疗高血压的方法和药物组合物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0129382A2 (fr) * 1983-06-15 1984-12-27 Shionogi & Co., Ltd. Formulation de céfaclor à action prolongée et sa préparation
EP0348808A2 (fr) * 1988-06-30 1990-01-03 Klinge Pharma GmbH Formulations pharmaceutiques et procédé pour leur préparation
US5158777A (en) * 1990-02-16 1992-10-27 E. R. Squibb & Sons, Inc. Captopril formulation providing increased duration of activity
WO1995019168A1 (fr) * 1994-01-14 1995-07-20 Laboratoires Des Produits Ethiques Ethypharm Microgranules de derives de 5-nitro imidazole
DE4431832A1 (de) * 1994-09-07 1996-03-14 Cordes Guenter Dr Arzneimittelzubereitung für ACE-Hemmer

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0129382A2 (fr) * 1983-06-15 1984-12-27 Shionogi & Co., Ltd. Formulation de céfaclor à action prolongée et sa préparation
EP0348808A2 (fr) * 1988-06-30 1990-01-03 Klinge Pharma GmbH Formulations pharmaceutiques et procédé pour leur préparation
US5158777A (en) * 1990-02-16 1992-10-27 E. R. Squibb & Sons, Inc. Captopril formulation providing increased duration of activity
WO1995019168A1 (fr) * 1994-01-14 1995-07-20 Laboratoires Des Produits Ethiques Ethypharm Microgranules de derives de 5-nitro imidazole
DE4431832A1 (de) * 1994-09-07 1996-03-14 Cordes Guenter Dr Arzneimittelzubereitung für ACE-Hemmer

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19625201A1 (de) * 1996-06-24 1998-01-08 Hans Peter Buerkle Darreichungsform für einen Wirkstoff
WO2009087483A3 (fr) * 2007-11-08 2009-10-22 Glaxo Group Limited Préparations pharmaceutiques
AU2008346205B2 (en) * 2007-11-08 2012-07-19 Capsugel Belgium Nv Pharmaceutical formulations
CN107213138A (zh) * 2017-08-07 2017-09-29 北京罗诺强施医药技术研发中心有限公司 定时释放药物治疗高血压的方法和药物组合物
CN107213138B (zh) * 2017-08-07 2020-12-18 北京罗诺强施医药技术研发中心有限公司 定时释放药物治疗高血压的方法和药物组合物

Also Published As

Publication number Publication date
AU5107496A (en) 1997-10-01

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