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WO2001015547A2 - Preparation de principe actif pour application veterinaire et son procede de production - Google Patents

Preparation de principe actif pour application veterinaire et son procede de production Download PDF

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Publication number
WO2001015547A2
WO2001015547A2 PCT/DE2000/002525 DE0002525W WO0115547A2 WO 2001015547 A2 WO2001015547 A2 WO 2001015547A2 DE 0002525 W DE0002525 W DE 0002525W WO 0115547 A2 WO0115547 A2 WO 0115547A2
Authority
WO
WIPO (PCT)
Prior art keywords
active
active ingredient
preparation
additive
animal
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/DE2000/002525
Other languages
German (de)
English (en)
Other versions
WO2001015547A3 (fr
Inventor
Hartmut Klocke
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to AU72688/00A priority Critical patent/AU7268800A/en
Publication of WO2001015547A2 publication Critical patent/WO2001015547A2/fr
Publication of WO2001015547A3 publication Critical patent/WO2001015547A3/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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • 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
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin

Definitions

  • the invention relates to the field of veterinary medicine and here to the production and use of an anthelmintic.
  • compositions described in this publication are intended exclusively for transdermal use.
  • the object of the invention is a formulation and a production method of an active substance preparation which contains an active substance of low acceptance by the animal while ensuring the medication effect of the preparation.
  • the basic idea of the invention is to be seen in the fact that the component with low acceptance is “hidden” in a core, in the casing of which only an active ingredient is contained which does not have this unpleasant property, which is therefore essentially tasteless.
  • Fenbendazole is such a water-insoluble, taste-free active ingredient, so that the active ingredient preparation presents itself tasteless when administered orally to the animal and the first active ingredient with low acceptance is only perceived by the animal late or not at all anymore.
  • a two-component active substance preparation of this form can preferably be realized in that the active cores are produced in the form of spheronized granules (for example by means of a process as described in DE 36 23 321 A1) and in that the coating in the form of a water Active ingredient suspension is sprayed onto the granules thus produced.
  • Another particularly preferred measure provides that a strongly swellable additive is added to the coating; this measure has the effect that, when the animal takes in the preparation, there is a delay in the taste perception of the first active ingredient incorporated into the core, which is little or not accepted, since the taste is perceived only in the dissolved form of the active ingredient A.
  • the pharmaceutical and other administration properties can be modified in the usual way according to the medical or technological requirements during manufacture, without departing from the basic idea of the invention, namely the introduction of the little-accepted first active ingredient exclusively in the active core for its sensory neutralization when the Preparation by the animal.
  • Figure 1 A schematic representation of the drug preparation in its dosage form
  • FIG. 2 a schematic flow diagram for the production of the active core as spheronized granules with a preferred formulation of the starting materials
  • FIG. 3 a schematic flow diagram for applying the coating to the active core with a preferred formulation of the starting materials
  • FIG. 4 schematic representations of the equipment used for the production. Description of the preferred embodiment
  • Figure 1 shows schematically the structure of the active ingredient preparation from the active core 10 and the casing 20, the active core 10 containing the entirety of the first active ingredient A, which is not accepted by the animal, and part of a second active ingredient which is tasteless and therefore to a certain percentage can also be provided in the envelope 20.
  • the first active ingredient A is praziquantel
  • the second active ingredient B is fenbendazole.
  • FIGS. 2 and 4 The production of the active core as spheronized granules can be seen in FIGS. 2 and 4: in a compulsory mixer (FIG. 4A), praziquantel, 80% of the total amount of fenbendazole, lactose, 60% of xantane, 50% of Na lauryl sulfate, PEG 10,000, maltodextrin and microcrystalline cellulose weighed and premixed dry. Distilled water is added gradually until the mixture has become a moist, crumbly mass. This mass is taken from the mixer and placed in an extruder (FIG. 4B).
  • the strands produced in the extruder are shaped into pellets of 500 ⁇ in the subsequent spheronizer (FIG. 4C);
  • a commercially available spheronizer for example a type 602 spheronizer from the company WLS mentioned, can also be used for this purpose, which breaks the strands formed by the extruder at a speed of 300 to 400 rpm and accomplishes the formation into the pellets at 700 revolutions per minute ,
  • the homogeneous distribution of the fenbendazole dispersion in the sense of a layering together with the other components results in the desired taste coverage of the first active ingredient A (praziquantel) which is accommodated in the active core 10 and is not accepted by the animal.
  • the fillers in the active core 10 reduce the percentage of active ingredients A and B in the active ingredient preparation, so that the pellets each represent only a small dose in each case.
  • a larger number of such pellets can be distributed well in the chyme, for example; their total surface area is significantly larger than the surface area of a tablet according to the prior art, so that the active substances can be absorbed over a larger area of the mucous membrane and distributed more quickly through the bloodstream. Damage to the mucous membranes, such as can occur with local, occasionally high drug deliveries, is avoided.

Landscapes

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

Abstract

L'invention concerne un procédé de production d'une préparation de principe actif pour application vétérinaire, comprenant au moins un premier principe actif qui est difficilement accepté par l'animal et qui est incorporé dans des noyaux actifs en tant que constituant de ces derniers. Ces noyaux actifs sont enfermés dans une enveloppe de sorte que le premier principe actif ne puisse plus être perçu sensoriellement par l'animal et par conséquent n'entrave pas la médication. Ainsi, l'effet d'un principe actif est assuré même si ce dernier présente un goût désagréable.
PCT/DE2000/002525 1999-08-28 2000-08-01 Preparation de principe actif pour application veterinaire et son procede de production Ceased WO2001015547A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU72688/00A AU7268800A (en) 1999-08-28 2000-08-01 Active agent preparation for veterinary use and method for the production thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19941024.0 1999-08-28
DE1999141024 DE19941024A1 (de) 1999-08-28 1999-08-28 Wirkstoffpräparat für tierärztliche Applikation und Verfahren zu seiner Herstellung

Publications (2)

Publication Number Publication Date
WO2001015547A2 true WO2001015547A2 (fr) 2001-03-08
WO2001015547A3 WO2001015547A3 (fr) 2001-08-02

Family

ID=7920027

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE2000/002525 Ceased WO2001015547A2 (fr) 1999-08-28 2000-08-01 Preparation de principe actif pour application veterinaire et son procede de production

Country Status (3)

Country Link
AU (1) AU7268800A (fr)
DE (1) DE19941024A1 (fr)
WO (1) WO2001015547A2 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763583B2 (en) 2003-12-13 2010-07-27 Bayer Animal Health Gmbh Endoparasiticidal compositions for topical application
WO2013037650A1 (fr) 2011-09-15 2013-03-21 Friulchem Spa Compositions pour administration orale aux animaux, leurs procedes d'obtention et leurs utilisations
WO2014033230A1 (fr) 2012-08-31 2014-03-06 Friulchem Spa Compositions pour administration orale aux animaux, leurs procedes d'obtention et leurs utilisations
CN103933045A (zh) * 2014-05-14 2014-07-23 深圳市红瑞生物科技有限公司 驱虫药物及其制备方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2403407B (en) * 2003-07-03 2006-12-13 Michael Hilary Burke Palatable oral anthelmintic composition

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2841668A1 (de) * 1978-09-25 1980-04-10 Bayer Ag Medikiertes tierfutter auf basis lebermehl
GB8707740D0 (en) * 1987-04-01 1987-05-07 Strathclyde Minerals Ltd Composition
FR2623976B1 (fr) * 1987-12-08 1994-02-25 So Ge Val Comprime pour animal domestique
AUPM969994A0 (en) * 1994-11-28 1994-12-22 Virbac S.A. Equine anthelmintic formulations

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763583B2 (en) 2003-12-13 2010-07-27 Bayer Animal Health Gmbh Endoparasiticidal compositions for topical application
WO2013037650A1 (fr) 2011-09-15 2013-03-21 Friulchem Spa Compositions pour administration orale aux animaux, leurs procedes d'obtention et leurs utilisations
US11103524B2 (en) 2011-09-15 2021-08-31 Friulchem Spa Compositions for oral administration to animals, processes for obtaining the same and the uses thereof
WO2014033230A1 (fr) 2012-08-31 2014-03-06 Friulchem Spa Compositions pour administration orale aux animaux, leurs procedes d'obtention et leurs utilisations
CN103933045A (zh) * 2014-05-14 2014-07-23 深圳市红瑞生物科技有限公司 驱虫药物及其制备方法

Also Published As

Publication number Publication date
WO2001015547A3 (fr) 2001-08-02
AU7268800A (en) 2001-03-26
DE19941024A1 (de) 2001-03-01

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