Utilization of ethoxylated fatty acid esters as self-emulsifiabl

Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Carboxylic acid ester

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514552, 514937, 554227, A61K 4700

Patent

active

061037702

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

1. Field of the Invention
The present invention generally relates to the use of ethoxylated fatty acid esters as self-emulsifiable compounds, particularly useful for preparing phytosanitary treatment products or medicines for veterinary or human use.
2. Description of the Related Art
It is known that an emulsion is a mixture of water and oil stabilised by surfactants.
The dispersion of oil in water (or water in oil) in the form of droplets sufficiently fine for obtaining a stable emulsion necessitates bringing about energy which is often considerable.
Furthermore, any oily preparation is called self-emulsifiable which is capable of forming a stable emulsion with an aqueous phase, practically without bringing about energy, by dispersion in the aqueous phase by slow mechanical stirring for example.
Self-emulsifiable compositions are particularly appreciated each time that mixtures with an aqueous phase, generally water, must be prepared without the need for efficient means of stirring.
Thus, it is notably a matter of:
within the context of domestic uses, e.g. for the preparation of household cleaning materials or gardening products;
within the context of agricultural uses, e.g. for the preparation of phytosanitary products intended for storage in tanks or other containers;
in the pharmaceutical field, e.g. for the preparation of extemporaneously made medicines.
Self-emulsifiable preparations have been described for a long time in the state of the art, especially in the agrochemical field.
These preparations are generally constituted of mineral oils or petroleum fractions to which not very harmful surfactants such as ethoxylated alkyl phenols in particular have been added.
Such preparations are however weakly biodegradable and therefore represent a potential danger to the environment, which has limited the development of them over the last years.
Recently, research has been orientated towards substitute products for petroleum oils and the use has been recommended to this end of biodegradable oils such as triglycerides or methyl esters of fatty acids in particular.
However, these oils are much more difficult to emulsify than mineral oils.
Furthermore, it has also been envisaged to replace ethoxylated alkyl phenols by biodegradable surfactants, but this has proved to be extremely difficult for cost and efficiency reasons.


SUMMARY OF THE INVENTION

Within this context, the aim of the present invention is to solve the technical problem which consists in providing a novel self-emulsifiable composition which is particularly useful for preparing phytosanitary treatment products or medicines for veterinary or human use, whose implementation is easy and which has a sufficient biodegradable character to fulfill the concerns of respect of the environment.
It has been discovered, and this constitutes the basis of the present invention, that certain esters obtained by reaction between fatty acids, low molecular weight alcohols or polyols and ethylene oxide constitute self-emulsifiable components without the aid of any other surfactant, and are biodegradable and capable of dissolving active principles which are little or not soluble in water.
Thus, according to a first aspect, the present application aims at covering the use of ethoxylated fatty acid esters having one of the following formulae: ##STR1##
in which:
R.sub.1, R.sub.3, R.sub.5, R.sub.6, R.sub.8 and R.sub.10 represent a linear or branched, saturated or unsaturated hydrocarbon chain having from 5 to 30 carbon atoms;
R.sub.2, R.sub.4, R.sub.7 and Rg represent a linear or branched, saturated or unsaturated hydrocarbon chain having from 1 to 5 carbon atoms;
the total number of ethylene oxide molecules represented in the above-mentioned formulae I, II and III by k, l+m, n+p+q respectively being an integer such that the HLB value (hydrophilic-lipophilic balance) of said compounds be between about 4 and about 10, preferably between about 5 and about 9 ; and, preferably still, neighboring 5.
as self-emulsifiable compounds which are particu

REFERENCES:
patent: 5676970 (1997-10-01), Okuyama et al.

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