Method for preparing granules containing one or more active prin

Details Method for preparing granules containing one or more active prin Method for preparing granules containing one or more active prin

1996-06-20

1998-01-06

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424405, 424409, 424408, 424470, A61K 914

Patent

active

057051933

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a new process for preparing emulsions or suspo-emulsions, dry or extruded in the form of granules, and the granules thus obtained.
The presentation of the active material in the form of an emulsion allows granules to be obtained which are endowed with a biological activity superior to that of a granule dispersible in water obtained by drying of a concentrated suspension of an active principle.
The subject of the invention is a process for preparing granules containing one or more active principles characterized in that the said active principle or principles is or are dissolved in a solvent, a solution is obtained which is absorbed on a support (or a filler) which may contain another active principle, a product is obtained to which water is or is not added, and which is dried and given the form of granules.
The support or filler can be chosen from the group of the following products: clays, bentonites, lactoses, starches, silicas, silicates, sulphates, and chlorides of alkaline and alkaline-earth metals.
In a preferred embodiment, the quantity of support used is less than 60% (m/m) of the total quantity of the ingredients used.
Citable as solvent are aromatic hydrocarbons, such as 1-methylnaphthalene, tetrahydronaphthalene, decahydronaphthalene, 2-methylnaphthalene or dimethylnaphthalene, alkylbenzenes, xylene (including Solvesso 200.RTM.), mixtures of isomers of dibenzyltoluene such as Marlotherm S.RTM.) or mixtures of isomers of benzyltoluene such as Marlotherm L.RTM., aliphatic hydrocarbons, mineral or vegetable oils, alcohols such as cyclohexanol, C8 alcohols, ethers such as dibenzylether, ketones such as cyclohexanone or 4-methylcyclohexanone, amides such as N,N-dimethylcaprylamide capramide (HALLCOMID.RTM. M 8-10), esters such as alkyl benzoates (ethyl, propyl, n-butyl for example), mono and dialkyl phthalates (of ethyl, of propyl or of n-butyl, for example), pyrrolidones such as N-methylpyrrolidone, N-octylpyrrolidone (AG SOL EX 8.RTM.), N-dodecylpyrrolidone (AG SOL EX 12.RTM.), N-cyclohexylpyrrolidone or mixtures of these solvents, such as Surfadone LP 100.RTM.. Also citable are TBP or tributyl phosphate, dibenzylether, N-butyl benzoate.
Citable as preferred solvent are aromatic solvents such as Solvesso 200.RTM., or pyrrolidones such as Surfadone LP 100.RTM..
In a preferred embodiment, the quantity of solvent used is between 20 and 40% (m/m) of the total quantity of the ingredients used.
The active principle can be of a very varied nature: it is preferably a pesticide.
The subject of the invention is in particular the process characterized in that the active principle is a herbicide, an insecticide or a fungicide.
The subject of the invention is more particularly the process characterized in that the active principle has a melting point above 70.degree. C.
The subject of the invention is quite particularly a process which is characterized in that the active principle is a pyrethrinoid. The latter can be alone or associated with other active principles such as pyrimicarb or the derivatives of .beta.-methoxy acrylic acid or the lipidamides.
Among the pyrethrinoids usable for the preparation of the granules of the invention can be cited deltamethrin, cypermethrin, alphamethrin, tralomethrin, cyalothrine, fenvalerate, cyfluthrine, flucythrinate, fluvalinate, fenpropathrine, tefluthrine, bifenthrine, acrinathrine, esfenvalerate, betacyfluthrine, taufluvalinate or lambdacyhalothrine.
Deltamethrin can be cited as preferred pyrethrinoid.
In a preferred embodiment, the quantity of active principle used is less than 20% of the total quantity of the ingredients used.
The subject of the invention is in particular a preparation process which is characterized in that one or more of the following ingredients is added to the solvent: emulsifiers and stabilizers.
The subject of the invention is also a process which is characterized in that one or more of the following elements is also added: dispersants, wetting agents, binders, colorants, anti-foaming agents and adjuvants facilita

REFERENCES:
patent: 4261921 (1981-04-01), Smeltz
patent: 4913722 (1990-04-01), Felix et al.

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