Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Polymer from ethylenic monomers only
Patent
1989-05-12
1991-09-03
Page, thurman K.
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Polymer from ethylenic monomers only
514129, 514 75, 514103, 514143, A61K 3174, A01N 5700
Patent
active
050453114
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The invention relates to am emulsifiable microemulsion concentrate containing an ester of phosphoric or thiophosphoric acid or their mixture as active ingredient.
BACKGROUND OF THE INVENTION
The preparation of plant-protective agents poses two kinds of problems:
1) the preparation of an active ingredient possessing the desired biological activity; and
2) the formulation of the active ingredient in a composition providing easy handling for the user.
Among the usual formulations of plant-protective agents, the wettable powders (WP-s) and emulsifiable concentrates (EC-s) are most important and represent nearly 90% of the plant-protective agents available commercially at present. Being liquids, the EC compositions are easier to handle, their portioning can be handled by a simple volumetric measurement and, from the viewpoint of labor-safety it is advantageous that during mixing the release of the health-damaging materials into the air is not a problem (which is practically inevitable in the course of e.g. transferring powders from bags to mixing tanks). In addition, the biological activity of the EC compositions is higher than that of the WP compositions. On the basis of the obvious advantages of EC compositions, it could be expected that these formulations would play a predominant role on the market. Actually however, the number of WP compositions is somewhat higher than that of the EC-s. The reason for this is that an EC composition can be prepared only from an active ingredient which is liquid or, when a solvent can be found in which the active ingredient can be dissolved to give a solution of 10 to 85% concentration (depending on the usual concentrations of the application) without any risk of the interim alteration of the active ingredient. An other drawback of the EC compositions arises from their high solvent content whereby they are inflammable and explosive and the environment is polluted. The drawback of the EC compositions can be diminished by formulating the active ingredient in an emulsifiable microemulsion concentrate.
Microemulsion is a colloidal system which, in a first approach differs from a true emulsion in the dimension of its particles which are smaller by an order of magnitude than those of a true emulsion. According to the general definition, this system contains surface active agents and two immiscible liquids, one of them is usually water, though, in principle, it is also possible to prepare a water-free microemulsion by using an other solvent.
The surfactant may be the mixture of even 6 to 8 tensides and additionally, it may contain alcohols or amines of medium chain length as auxillary surfactants (co-surfactants). A peculiarity of this complicated system lies in its thermodynamical stability: it is formed spontaneously from the appropriate components without the input of an outer energy. The direct reason for this formation is that the interfacial tension between the two phases is very small, it approaches zero and transiently it even becomes negative.
In the outer appearance, a microemulsion is a transparent solution as a consequence of the very small size of the disperse particles. The size of the monodisperse spheres varies between 0.01 and 0.2 .mu.m. Although this system is transparent, all monochromatic lights such as electron or neutron radiation or X rays are scattered by the system whereby the determination of the particle size is also rendered possible.
Being a peculiar colloidal system, a microemulsion may prominently be used for formulating plant-protective agents on the basis of its above characteristics.
An additional advantage of the microemulsion consists in that it contains a lower amount of organic solvent than an EC composition which is preferably from the viewpoint of both environment protection and the danger of fire and explosion. Microemulsions are preferably used in the cases of ULV applications.
It is characteristic of the known microemulsion EC compositions that, in addition to the active ingredient they contain a combination of no
REFERENCES:
patent: 3880997 (1975-04-01), Schmidt et al.
patent: 4139616 (1978-02-01), Ducret et al.
patent: 4755311 (1988-07-01), Burjes et al.
Chem. Ab. 85,83569w, J. B. Brown et al.
Pioc. Int. Cort. Colloid Sortane Sci, Microemulsions Using Nonionic Emulsifiers, Brown, J. B. et al., p. 507 (1975) which is the underlying reference in Chem. Abstracts 85:83569W Cited by the Examiner as Chem. Abstracts (R).
Angyan Sandor
Detre Tamas
Kiss Eva
Marmarosi Tamasne
Pal Josefne
Chinoin Gyogyszer - es Vegyeszeti Termekek Gyara Rt.
Dubno Herbert
Kulkosky Peter F.
Myers Jonathan
Page Thurman K.
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