CA2245506C - Granules from triazines - Google Patents
Granules from triazines Download PDFInfo
- Publication number
- CA2245506C CA2245506C CA002245506A CA2245506A CA2245506C CA 2245506 C CA2245506 C CA 2245506C CA 002245506 A CA002245506 A CA 002245506A CA 2245506 A CA2245506 A CA 2245506A CA 2245506 C CA2245506 C CA 2245506C
- Authority
- CA
- Canada
- Prior art keywords
- granules
- weight
- particle size
- active compound
- polyvinylpyrrolidone
- 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.)
- Expired - Fee Related
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
- A61K9/14—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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—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
- A61K9/14—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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
The present invention relates to triazine granules of the following composition a) active compound 0.5 to 10% (weight) b) starch 10 to 40% (weight) c) lactose 30 to 60% (weight) d) polyvinylpyrrolidone 5 to 35% (weight) having a particle size distribution of between 40 to 400 .mu. and an upper limit of the particle size at 2 000 .mu..
Description
GRANULES FROM TRIAZINES
The present invention relates to triazine granules and their preparation.
Toltrazuril (1-methyl-3-(3-methyl-4-(4-(trifluoromethyl)thio)phenoxy)phenyl)-1,3,5-triazine-2,4,6(1H, 3H, 5H)trione) is a known active compound against coccidia.
It is customarily used in the form of aqueous solutions or suspensions. For many application areas, the solutions can only be employed with difficulty.
The present invention relates to triazine granules of the following composition a) active compound 0.5 to 10% (weight) b) starch 10 to 40% (weight) c) lactose 30 to 60% (weight) d) polyvinylpyrrolidone 5 to 35% (weight) having an average particle size distribution of between 40 to 400 m and an upper limit of the particle size of 2 000 m.
The granules are prepared by premixing the components a) to d) in a suitable mixing or stirring vessel and spraying with a solution of polyvinylpyrrolidone. The granules are subsequently dried and, if necessary, screened off.
Dust-free, dry, easily flowing and easily dosable granules are obtained. These granules are preferably employed for the treatment of coccidiosis disorders of cats and other domestic animals and pets. Besides cats, the domestic animals and pets include dogs, rabbits and ornamental birds.
The granules are administered by mixing with solid, semi-solid or liquid feed.
According to experience, feed which has been treated with the granules according to the invention is absorbed without problems even by sensitive animals.
The present invention relates to triazine granules and their preparation.
Toltrazuril (1-methyl-3-(3-methyl-4-(4-(trifluoromethyl)thio)phenoxy)phenyl)-1,3,5-triazine-2,4,6(1H, 3H, 5H)trione) is a known active compound against coccidia.
It is customarily used in the form of aqueous solutions or suspensions. For many application areas, the solutions can only be employed with difficulty.
The present invention relates to triazine granules of the following composition a) active compound 0.5 to 10% (weight) b) starch 10 to 40% (weight) c) lactose 30 to 60% (weight) d) polyvinylpyrrolidone 5 to 35% (weight) having an average particle size distribution of between 40 to 400 m and an upper limit of the particle size of 2 000 m.
The granules are prepared by premixing the components a) to d) in a suitable mixing or stirring vessel and spraying with a solution of polyvinylpyrrolidone. The granules are subsequently dried and, if necessary, screened off.
Dust-free, dry, easily flowing and easily dosable granules are obtained. These granules are preferably employed for the treatment of coccidiosis disorders of cats and other domestic animals and pets. Besides cats, the domestic animals and pets include dogs, rabbits and ornamental birds.
The granules are administered by mixing with solid, semi-solid or liquid feed.
According to experience, feed which has been treated with the granules according to the invention is absorbed without problems even by sensitive animals.
Active compounds which may be mentioned are symmetrical 1,3,5-triazine-2,4,6(IH, 3H, 5H)-triones such as toltrazuril, unsymmetrical 1,2,4-triazine-3,5-diones such as diclazuril (2,6-dichloro-a-(4-chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)-phenylacetonitrile).
Toltrazuril may be preferably mentioned. The active compounds are employed at 0.5 to 10, preferably 1 to 5, particularly preferably 2 to 4% by weight.
Starches which may be mentioned are the customary types of starch such as potato starch, maize starch, cereal starch. Maize starch may preferably be mentioned.
Starch is employed at 10 to 40, preferably 20 to 30, particularly preferably about 25% by weight.
Lactose is employed as a monohydrate in concentrations of from 30 to 60, preferably 50 to 60, particularly preferably about 60% by weight.
Polyvinylpyrrolidone (PVP) is preferably employed as an average molecular weight PVP having a K value of 24 to 32. PVP having a K value of 24 to 30, particularly preferably 25, is particularly preferred. The solvent employed for PVP is preferably water. Solvents which may also be mentioned are organic solvents on their own or as a mixture with water.
A K value of 25 corresponds to a weight average of the molecular mass of 28 000 to 34 000. The K value characterizes the average molecular mass.
PVP is preferably employed in a total amount of from 10 to 30% by weight.
The particle size distribution is between 40 to 400 m, preferably between 80 and 200 m, with an upper limit at 2 000 m, preferably at 1 000 m.
The granules according to the invention are prepared in solid mixers, preferably in fluidized bed granulators.
I,e A 31 566-Foreign Countries For the preparation, the individual components are homogeneously mixed at room temperature. The mixture is then sprayed with a 10 to 50% strength, preferably 30 to 40% strength, particularly preferably a 30% strength, aqueous PVP solution and optionally sprayed with further water. Per kg of mixture, 100 to 300, preferably 150 to 200 ml, of spray solution are employed. Granulation is carried out at 20 to 50 C, preferably at 25 to 40 C.
The granules are then dried at about 40 to 70 C, preferably at 50 to 60 C.
Toltrazuril may be preferably mentioned. The active compounds are employed at 0.5 to 10, preferably 1 to 5, particularly preferably 2 to 4% by weight.
Starches which may be mentioned are the customary types of starch such as potato starch, maize starch, cereal starch. Maize starch may preferably be mentioned.
Starch is employed at 10 to 40, preferably 20 to 30, particularly preferably about 25% by weight.
Lactose is employed as a monohydrate in concentrations of from 30 to 60, preferably 50 to 60, particularly preferably about 60% by weight.
Polyvinylpyrrolidone (PVP) is preferably employed as an average molecular weight PVP having a K value of 24 to 32. PVP having a K value of 24 to 30, particularly preferably 25, is particularly preferred. The solvent employed for PVP is preferably water. Solvents which may also be mentioned are organic solvents on their own or as a mixture with water.
A K value of 25 corresponds to a weight average of the molecular mass of 28 000 to 34 000. The K value characterizes the average molecular mass.
PVP is preferably employed in a total amount of from 10 to 30% by weight.
The particle size distribution is between 40 to 400 m, preferably between 80 and 200 m, with an upper limit at 2 000 m, preferably at 1 000 m.
The granules according to the invention are prepared in solid mixers, preferably in fluidized bed granulators.
I,e A 31 566-Foreign Countries For the preparation, the individual components are homogeneously mixed at room temperature. The mixture is then sprayed with a 10 to 50% strength, preferably 30 to 40% strength, particularly preferably a 30% strength, aqueous PVP solution and optionally sprayed with further water. Per kg of mixture, 100 to 300, preferably 150 to 200 ml, of spray solution are employed. Granulation is carried out at 20 to 50 C, preferably at 25 to 40 C.
The granules are then dried at about 40 to 70 C, preferably at 50 to 60 C.
Example 1 Preparation:
1. 500 g of polyvinylpyrrolidone having a K value of 25 = PVP-25 are introduced into 1250 g of water (demineralized) at room temperature in the course of 2 hours with stirring using a toothed disc stirrer. The mixture is stirred for 1 hour until dissolution is complete.
2. 2500 g of maize starch, 1000 g of PVP-25, 200 g of toltrazuril and 5800 g of lactose are initially introduced into a fluidized bed granulator of the TM
Aeromatic S 2 type. The mixture is homogenized for 10 minutes in a fluidized bed with fluidization at 150 to 200 m3/h and temperature control at 25 to 30 C.
3. The prewarming phase up to reaching 25 to 40 C admitted air temperature should be 2 to 4 minutes.
4. In the fluidized bed granulator, the premixture is granulated at a spraying pressure of 2 bar with 35 to 40 C admitted air, 22 to 30 C waste air and an admitted air amount of 150 to 200 m3/h with spraying of 30 g of spray solution/minute.
The PVP initial solution from Preparation 1 is sprayed.
For rinsing the nozzle, approximately 100 g of denat. water are, added.
Drying is then carried out at 150-200 m3/h with 55 C admitted air to 42-45 C
waste air temperature.
1. 500 g of polyvinylpyrrolidone having a K value of 25 = PVP-25 are introduced into 1250 g of water (demineralized) at room temperature in the course of 2 hours with stirring using a toothed disc stirrer. The mixture is stirred for 1 hour until dissolution is complete.
2. 2500 g of maize starch, 1000 g of PVP-25, 200 g of toltrazuril and 5800 g of lactose are initially introduced into a fluidized bed granulator of the TM
Aeromatic S 2 type. The mixture is homogenized for 10 minutes in a fluidized bed with fluidization at 150 to 200 m3/h and temperature control at 25 to 30 C.
3. The prewarming phase up to reaching 25 to 40 C admitted air temperature should be 2 to 4 minutes.
4. In the fluidized bed granulator, the premixture is granulated at a spraying pressure of 2 bar with 35 to 40 C admitted air, 22 to 30 C waste air and an admitted air amount of 150 to 200 m3/h with spraying of 30 g of spray solution/minute.
The PVP initial solution from Preparation 1 is sprayed.
For rinsing the nozzle, approximately 100 g of denat. water are, added.
Drying is then carried out at 150-200 m3/h with 55 C admitted air to 42-45 C
waste air temperature.
5. In order to exclude any coarse granules or wall deposits possibly present, granules over 2000 m are screened off.
Claims (12)
1. Granules of a triazine, with the exception of lamotrigine, of the following composition, by weight:
(a) active compound 0.5 to 10%;
(b) starch 10 to 40%;
(c) lactose 30 to 60%; and (d) polyvinylpyrrolidone 5 to 35%, having an average particle size distribution of between 40 to 400 µm and an upper limit of the particle size at 2 000 µm.
(a) active compound 0.5 to 10%;
(b) starch 10 to 40%;
(c) lactose 30 to 60%; and (d) polyvinylpyrrolidone 5 to 35%, having an average particle size distribution of between 40 to 400 µm and an upper limit of the particle size at 2 000 µm.
2. The granules of claim 1, wherein the active compound is toltrazuril.
3. The granules of claim 1, wherein the active compound is diclazuril.
4. The granules of any one of claims 1 to 3, wherein the active compound is contained in an amount of 1 to 5% by weight.
5. The granules of any one of claims 1 to 4, wherein starch is contained in an amount of 20 to 30% by weight.
6. The granules of any one of claims 1 to 5, wherein lactose is contained in an amount of 50 to 60% by weight.
7. The granules of any one of claims 1 to 6, wherein polyvinylpyrrolidone is contained in an amount of 10 to 30%
by weight.
by weight.
8. The granules of any one of claims 1 to 7, wherein the average particle size distribution is between 80 to 200 µm.
9. The granules of any one of claims 1 to 8, wherein the upper limit of the particle size is 1000 µm.
10. A process for the preparation of granules of a triazine as defined in claim 1, wherein the components (a) to (d) are premixed in a suitable mixing or stirring vessel and sprayed with a solution of polyvinylpyrrolidone and dried.
11. The process of claim 10, wherein after drying the granules are screened off.
12. Use of the granules of any one of claims 1 to 9 for treating a coccidiosis disorder in an animal.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19603984A DE19603984A1 (en) | 1996-02-05 | 1996-02-05 | Granules of triazines |
| DE19603984.3 | 1996-02-05 | ||
| PCT/EP1997/000310 WO1997028804A1 (en) | 1996-02-05 | 1997-01-23 | Granules from triazines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2245506A1 CA2245506A1 (en) | 1997-08-14 |
| CA2245506C true CA2245506C (en) | 2007-07-10 |
Family
ID=38254954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002245506A Expired - Fee Related CA2245506C (en) | 1996-02-05 | 1997-01-23 | Granules from triazines |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA2245506C (en) |
-
1997
- 1997-01-23 CA CA002245506A patent/CA2245506C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CA2245506A1 (en) | 1997-08-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20140123 |