Tablet formulations of pesticides

Details Tablet formulations of pesticides Tablet formulations of pesticides

1990-12-06

1993-01-19

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Biocides; animal or insect repellents or attractants

424405, 424465, 424466, 424717, A01N 2512, A61K 946

Patent

active

051805871

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

This invention concerns specific pesticide formulations especially suited for commercial use in tablet form. Several types of tablet formulations are known in the art. See, for instance, G. B. 2,139,893; G. B. 2,184,946; U.S. Pat. No. 4,182,620 and Kokai 51088641. However, these publications do not disclose or suggest the specific combinations of active ingredient(s) and delivery system(s) of this invention. The formulations of this invention afford rapid disintegration and dispersion, even in cold water, of pesticidally active compounds that are water insoluble or of very low water solubility.


SUMMARY OF THE INVENTION

This invention concerns a tablet formulation consisting essentially of, by total weight of the formulated composition: least about 100.degree. C. and solubility in neutral water at 20.degree. C. of no more than about 5% by weight, and components complementary to the pesticide of (i).
Typically, the delivery system (ii) will contain the following components in these amounts by weight of the total composition: mixture thereof; or a mixture thereof; and (a) to (e) in the recited ranges to effect rapid disintegration of finely dispersed pesticide particles (i).
By "tablet formulation" is meant the tablet made from the composition described herein, as well as the composition formulated in accordance with this disclosure but not in tablet form.
Contemplated pesticides include those selected from the following classes, including mixtures thereof: herbicides, fungicides, bactericides, insecticides, nematocides, acaricides, and growth regulants.
Preferred dibasic and tribasic organic carboxylic acids include citric, fumaric, phthalic, maleic, malic, oxalic, adipic, glutaric, 2-methyl glutaric, succinic and tartaric, or mixtures of any of them. Preferred carbonates and bicarbonates include the lithium, sodium, and potassium salts or mixtures of any of them.
The term "dispersants" includes sodium salts of naphthalene formaldehyde condensates; sodium, potassium and calcium salts of naphthalene sulfonic acid condensates; lithium, sodium, potassium, calcium, and ammonium salts of lignosulfonates such as Polyfon H.RTM. and Lignosol TSF.RTM.; sodium, potassium and ammonium salts of polyacrylates and carboxylates, e.g., Tamol 731 SD; sodium salts of maleic anhydride-isobutylene copolymers; and water soluble nonionic polymers such as polyvinylpyrrolidone, polyethylene oxides and cellulose derivatives. Preferred dispersants include the sodium, potassium, ammonium and calcium salts of naphthalene sulfonic acid condensates, with the ammonium salts, specifically Lomar PWA, more preferred.
Water-insoluble, cross-linked polyvinylpyrrolidone disintegrant refers to any of the generic crospovidone disintegrating agents. Specifically preferred is Polyplasdone.RTM. XL 10.
The term "anionic wetting agent" includes alkylbenzene sulfonates, alkyl and dialkylnaphthalene sulfonates, alkyl and alcohol sulfates, sulfoalkylamides, carboxylates, alpha-olefin sulfonates and dialkyl sulfosuccinates. The term "nonionic wetting agent" includes acetylenic diols, ethylene oxidepropylene oxide copolymers, alkylphenol ethoxylates, fatty acid ethoxylates, alcohol ethoxylates, sorbitan fatty acid ester ethoxylates and castor oil ethoxylates. The preferred wetting agents are sodium dialkyl sulfosuccinates of which sodium diisobutyl sulfosuccinate (Monawet MB-100), sodium diamyl sulfosuccinate and sodium dicyclohexyl sulfosuccinate are more preferred.


DETAILS OF THE INVENTION

Preferred pesticides are those listed in Table 1.


TABLE 1 __________________________________________________________________________ Cmpd. No. Common Name m.p. (.degree.C.) Chemical Name __________________________________________________________________________ HERBICIDES 1 acifluorfen 142-160 5-[2-(chloro-4-(trifluoro methyl)phenoxy]-2-nitro- benzoic acid 2 asulam 142-144 methyl [(4-aminophenyl)- sulfonyl]carbamate 3 atrazine 175-177 6-chloro-N-ethyl-N'-(1- methylethyl)-1,3,5- triazine-2,4-diamine 4 bensulfuron

REFERENCES:
patent: 3518343 (1970-06-01), Welsh et al.
patent: 4111202 (1978-09-01), Theeuwes
patent: 4564363 (1986-01-01), Bagnall et al.
patent: 4888177 (1989-12-01), Gergely et al.
patent: 4994273 (1991-02-01), Zentner et al.

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