Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1998-07-31
1999-12-21
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424501, 424502, 424489, 424438, 424442, 514241, 514246, 514951, A61K 3153, A61K 914
Patent
active
06004585&
DESCRIPTION:
BRIEF SUMMARY
THIS APPLICATION IS A 371 OF PCT/EP97/00310, FILED JAN. 23, 1997.
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-tri azine-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 an upper limit of the particle size of 2000.mu..
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(1H, 3H, 5H)-triones such as toltrazuril, unsymmetrical 1,2,4-triazine-3,5-diones such as diclazuril (2,6-dichloro-.alpha.-(4-chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-tria zin-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 28000 to 34000. 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.mu., preferably between 80 and 200.mu., with an upper limit at 2000.mu., preferably at 1000.mu..
The granules according to the invention are prepared in solid mixers, preferably in fluidized bed granulators.
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.degree. C., preferably at 25 to 40.degree. C.
The granules are then dried at about 40 to 70.degree. C., preferably at 50 to 60.degree. C.
EXAMPLE 1
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. g of lactose are initially introduced into a fluidized bed granulator of the Aeromatic S 2 type. The mixture is homogenized for 10 minutes in a fluidized bed with fluidization at 150 to 200 m.sup.3 /h and temperature control at 25 to 30.degree. C. temperature should be 2 to 4 minutes. spraying pressure of 2 bar with 35
REFERENCES:
patent: 4826842 (1989-05-01), Mehlhorn et al.
patent: 5629312 (1997-05-01), Bousseau et al.
patent: 5866597 (1999-02-01), Baxter
Grofmeyer Dorothea
Mundt Christian
Wegner Christian
Akorli Godfried R.
Bayer Aktiengesellschaft
Gil Joseph C.
Page Thurman K.
Seidleck Brian K.
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