Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2000-07-05
2002-12-31
Dees, Jose′ G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C424S045000, C516S058000, C554S001000, C554S002000, C562S606000
Reexamination Certificate
active
06500862
ABSTRACT:
The present invention relates to stable microemulsions for the administration of fatty acids to humans or to animals. These microemulsions, with a pH of less than 6.5, have a very high fatty acid concentration since they contain from 5 to 30% by weight of fatty acids.
The influence of fatty acids and of mixtures thereof on the behaviour of animals has been described and commented on in the literature. By way of illustration, there may be mentioned pheromones which may contain or constitute such mixtures of fatty acids.
Compositions based on fatty acids are more particularly known which have a soothing and relaxing effect on certain mammals. These compositions are capable of combating anxiety in an animal experiencing a particular stress situation caused for example by a change in its environment which is too sudden. U.S. Pat. No. 5,709,863 describes in particular fatty acid compositions which, simply upon bringing into contact with the olfactory organs of the respiratory tract, facilitate the adaptation of cats to an unknown environment by limiting their anxiety.
The emulsions described in U.S. Pat. No. 5,709,863 have, nevertheless, a number of disadvantages.
They are not easily dispersible in the environment because of their high viscosity.
Furthermore, they exhibit inadequate heat stability; it has been possible to observe crystallization of the fatty acids at low temperature and sometimes even at room temperature.
One way of reducing the viscosity of fatty acid compositions is to formulate these fatty acids in a microemulsion.
However, the formulation of microemulsions with high fatty acid concentrations, which are both chemically and heat stable, is problematic.
In fact, because of the high fatty acid concentrations (greater than 5% by weight), the use of cosurfactants such as alcohols is necessary. However, the simultaneous presence of alcohols and fatty acids in the microemulsions is a priori not desirable given the high risks of esterification. The chemical stability of such microemulsions appears compromised.
Surprisingly, the inventors have been able to develop a stable composition, in microemulsion form, comprising a high concentration of fatty acids and which may include up to 30% by weight of alcohol.
More precisely, the invention relates to a stable, nondetergent composition, in microemulsion form, for administration to humans or animals, comprising:
from 5 to 30% by weight of one or more fatty acids with a free carboxylic acid function, as active ingredient;
from 5 to 35% by weight of one or more surfactants;
from 5 to 30% by weight of one or more C
1
-C
12
alcohols, as cosurfactant;
from 5 to 35% by weight of one or more water-soluble compounds with a carbonyl or hydroxyl function; and
from 0 to 35% by weight of one or more water-immiscible compounds; the said composition having a pH of less than 6.5.
Fatty acid is understood to mean, according to the invention, saturated or unsaturated, linear or branched hydrocarbon chain-containing monocarboxylic acids which are active in humans or animals when administered thereto, this being regardless of the route of administration. More precisely, these fatty acids are chemical substances capable of modifying the behaviour or the physiological responses of humans or animals.
Usually, the fatty acids are in the form of C
4
-C
22
. Examples thereof are capric, lauric, myristic, palmitic, palmitoleic, oleic, linoleic, stearic, arachidonic, n-butyric, isobutyric, &agr;-methylbutyric, caproic, pivalic, gamma-linoleic, eicosapentanoic and docosahexanoic acids.
At room temperature, these fatty acids are present either in liquid form or in solid form, depending on the length and structure of the carbon chain.
Examples of mixtures of fatty acids which can be used as active ingredient in the context of the invention are pheromones.
Preferably, the compositions of the invention comprise one of the following fatty acid mixtures:
i—a mixture of oleic acid and palmitic acid;
ii—a mixture of oleic acid and n-butyric acid;
iii—a mixture of oleic acid, palmitic acid and linoleic acid;
iv—a mixture of oleic acid, palmitic acid, linoleic acid and palmitoleic acid;
v—a mixture of capric acid, lauric acid, myristic acid, palmitoleic acid, palmitic acid, linoleic acid and oleic acid;
vi—a mixture of oleic acid, palmitic acid, linoleic acid and myristic acid;
vii—a mixture of oleic acid, palmitic acid, linoleic acid , lauric acid and myristic acid;
viii—a mixture of oleic acid, palmitic acid, linoleic acid, myristic acid and pentadecanoic acid;
ix—a mixture of oleic acid, palmitic acid, linoleic acid, myristic acid, pentadecanoic acid and stearic acid;
x—a mixture of oleic acid, palmitic acid, linoleic acid, myristic acid, lauric acid and pentadecanoic acid;
xi—one of the C
4
-C
22
fatty acid mixtures described in U.S. Pat. No. 5,709,863.
The composition of the invention preferably comprises from 10 to 30% by weight of one or more fatty acids, better still from 15 to 25% by weight, for example from 17 to 23% by weight.
According to the invention, it is essential that pH of the composition is less than 6.5. Preferably, the pH of this composition is between 3 and 6.
According to the invention, the composition in microemulsion form may comprise one or more surfactants chosen from an anionic, cationic, zwitterionic or nonionic surfactant as long as its nature is not incompatible with its use.
Preferably, the compositions of the invention comprise exclusively pharmaceutically acceptable constituents.
Thus, the preferred surfactants are anionic, and better still nonionic, surfactants.
Examples of anionic surfactants which may be suitable are alkyl sulphates in which the alkyl chain is C
6
-C
18
, such as sodium lauryl sulphate, alkyl benzenesulphonates in which the alkyl chain is C
6
-C
18
and dialkyl sulphosuccinates in which the alkyl chain is C
6
-C
18
, such as sodium dioctyl sulphosuccinate.
The counter-ion for the alkyl sulphates, for the alkyl benzenesulphonates and for the dialkyl sulphosuccinates is preferably the cation of an alkali metal such as sodium or potassium, or alternatively an ammonium cation.
Examples of nonionic surfactants are:
a) the product of condensation of an aliphatic fatty alcohol, preferably a C
8
-C
22
, with a C
2
-C
3
alkylene oxide. The C
2
-C
3
alkylene oxide may be ethylene oxide, propylene oxide or alternatively a mixture of ethylene oxide and propylene oxide in any proportions. An example of such surfactants is the product of condensation of lauryl alcohol (or n-dodecyl alcohol) with 30 mol of ethylene oxide;
b) the product of condensation of an alkylphenol in which the alkyl chain is C
8
-C
22
with a C
2
-C
3
alkylene oxide. Here again, the products of condensation with ethylene oxide, propylene oxide or alternatively a mixture of ethylene oxide and propylene oxide in any proportions are also advantageous. By way of example of such surfactants, there may be mentioned the product of condensation of n-nonylphenol with 10 mol of ethylene oxide;
c) the product of condensation of a fatty acid, preferably a C
8
-C
22,
with a C
2
-C
3
alkylene oxide, for example ethylene oxide or propylene oxide or a mixture of ethylene oxide and propylene oxide in any proportions. These condensation products contain a chain alkoxylated at the level of the hydroxyl function of the carboxyl group. Preferred surfactants of this group are the condensation products obtained from oleic acid, palmitic acid and stearic acid;
d) the product of condensation of a C
8
-C
22
fatty acid glyceride with a C
2
-C
3
alkylene oxide such as ethylene oxide and/or propylene oxide. Among these, ethoxylated glyceryl palmitate is preferred;
e) the product of condensation of a C
8
-C
22
fatty acid ester of sorbitol with a C
2
-C
3
alkylene oxide which may be ethylene oxide, propylene oxide or mixtures thereof. These compounds are polysorbates. A preferred example is sold under the name Tween 80;
f) the product of condensation of sorbitol with a C
8
-C
22
fatty acid.
As surfactant, it is preferred to use either an alkali metal alkyl sulphate or
Ceva Sante Animale
Dees Jose′ G.
Haghighatian Mina
Jacobson & Holman PLLC
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