WO2001015547A2 - Wirkstoffpräparat für tierärztliche applikation und verfahren zu seiner herstellung - Google Patents
Wirkstoffpräparat für tierärztliche applikation und verfahren zu seiner herstellung Download PDFInfo
- 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
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)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (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
Description
Claims
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 |
---|---|---|---|
DE1999141024 DE19941024A1 (de) | 1999-08-28 | 1999-08-28 | Wirkstoffpräparat für tierärztliche Applikation und Verfahren zu seiner Herstellung |
DE19941024.0 | 1999-08-28 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001015547A2 true WO2001015547A2 (de) | 2001-03-08 |
WO2001015547A3 WO2001015547A3 (de) | 2001-08-02 |
Family
ID=7920027
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/DE2000/002525 WO2001015547A2 (de) | 1999-08-28 | 2000-08-01 | Wirkstoffpräparat für tierärztliche applikation und verfahren zu seiner herstellung |
Country Status (3)
Country | Link |
---|---|
AU (1) | AU7268800A (de) |
DE (1) | DE19941024A1 (de) |
WO (1) | WO2001015547A2 (de) |
Cited By (4)
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2403407B (en) * | 2003-07-03 | 2006-12-13 | Michael Hilary Burke | Palatable oral anthelmintic composition |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4283400A (en) * | 1978-09-25 | 1981-08-11 | Bayer Aktiengesellschaft | Medicated animal feed based on liver meal |
EP0293070A1 (de) * | 1987-04-01 | 1988-11-30 | Strathclyde Chemical Co. Ltd. | Orales Mittel zur Verabreichung einer Wirksubstanz an ein Tier |
EP0320320A2 (de) * | 1987-12-08 | 1989-06-14 | So.Ge.Val S.A. | Tablette für Haustiere |
EP0717993A2 (de) * | 1994-11-28 | 1996-06-26 | Virbac S.A. | Antihelmintische Zusammensetzungen für Pferde |
-
1999
- 1999-08-28 DE DE1999141024 patent/DE19941024A1/de not_active Withdrawn
-
2000
- 2000-08-01 WO PCT/DE2000/002525 patent/WO2001015547A2/de active Application Filing
- 2000-08-01 AU AU72688/00A patent/AU7268800A/en not_active Abandoned
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4283400A (en) * | 1978-09-25 | 1981-08-11 | Bayer Aktiengesellschaft | Medicated animal feed based on liver meal |
EP0293070A1 (de) * | 1987-04-01 | 1988-11-30 | Strathclyde Chemical Co. Ltd. | Orales Mittel zur Verabreichung einer Wirksubstanz an ein Tier |
EP0320320A2 (de) * | 1987-12-08 | 1989-06-14 | So.Ge.Val S.A. | Tablette für Haustiere |
EP0717993A2 (de) * | 1994-11-28 | 1996-06-26 | Virbac S.A. | Antihelmintische Zusammensetzungen für Pferde |
Cited By (5)
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 (de) | 2001-08-02 |
AU7268800A (en) | 2001-03-26 |
DE19941024A1 (de) | 2001-03-01 |
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