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Title: Topical oil-in-water emulsions containing retinoids
United States Patent: 5,976,555
Inventors: Liu; Jue-Chen (Neshanic, NJ); Wang; Jonas C. T.
(Robbinsville, NJ); Yusuf; Mohammed (Edison, NJ); Yamamoto; Norihiro (Koriyama,
JP); Kazama; Satoshi (Sukagawa, JP); Stahl; Christopher R. (Hawthorne,
CA); Holland; Jean P. (Doylestown, PA); Mather; Kamran (Agoura Hills, CA);
Aleles; Margaret A. (Gladstone, NJ); Hamada; Sachio (St-Germain-en-Laye,
FR); Cole; Curtis A. (Langhorne, PA)
Assignee: Johnson & Johnson Consumer Products, Inc.
(Skillman, NJ)
Appl. No.: 609588
Filed: March 1, 1996
Abstract
Skin care compositions comprising an oil-in-water emulsion base
containing retinoids and possessing good physical and chemical stability.
More particularly, said skin care compositions contain (a) an emulsifier
system selected from the group consisting of: (i) a mixture of glyceryl
stearate and polyethylene glycol 100 stearate; (ii) cetearyl alcohol and
cetearyl glucoside; (iii) a mixture of a polyethylene glycol ethers of
stearyl alcohol; and (iv) a mixture of sorbitan stearate and polysorbate
60; (b) a co-emulsifier selected from the group consisting of cetyl
alcohol, stearyl alcohol and mixtures thereof; (c) an oil phase present in
the amount of from about 5 to about 20 percent by weight of the total
emulsion composition which contains (i) a light, dry absorbable oil and
(ii) substantive, emollient oils or waxes, wherein the light, dry
absorbable oil and the substantive oil or wax are present in a ratio of
from about 1:3 for about 10:1.
SUMMARY OF THE INVENTION
In accordance with the present invention, it has now been
unexpectedly found that certain retinoids may be successfully stabilized
against chemical degradation by incorporating them into oil-in-water
emulsions comprising a specifically defined stabilizing system. In
addition, this invention relates to oil-in-water emulsion compositions
which are cosmetically elegant.
The retinoids which can be stabilized against chemical degradation in
accordance with the principles of the present invention are retinol
(Vitamin A alcohol), retinal (Vitamin A aldehyde), retinyl acetate,
retinyl palmitate and mixtures thereof. It is also theorized that other
retinoids, including synthetic retinoids and retinoid-like chemicals may
benefit from inclusion in the formulations of this invention.
As used herein, the "chemical stability" or
"stability" of a retinoid is defined in terms of the percentage
of the specified retinoid which is retained in its original chemical form
after the composition has been stored for a specified period of time at a
specified temperature. Thus, if the original concentration of all-trans
retinol in an absolute ethanol solution were 0.20% by weight and, after
two (2) weeks' storage at room temperature (21oC..+-.1oC.),
the concentration of all-trans retinol were 0.18% by weight, then the
original solution would be characterized as having a chemical stability of
90% after two weeks' storage at room temperature. In the same fashion, if
an emulsion comprising all-trans retinol had an initial concentration of
0.30% by weight and after storage for 13 weeks at 40o C. had a
concentration of all trans-retinol of 0.24% by weight, then the original
emulsion retinol of 80% after 13 weeks storage at 40oC.
Specifically, a commercially usable composition should exhibit a stability
of at least about 60% of the active retinoid(s) after 13 weeks storage at
40oC. Preferably, the compositions of this invention exhibit a
stability of at least about 70% after 13 weeks' storage at 40oC.
Accordingly, there is provided, in accordance with the teachings of this
invention, a skin care composition comprising an oil-in-water emulsion and
a retinoid selected from the group consisting of retinol, retinal, retinyl
acetate, retinyl palmitate and mixtures thereof, said composition having a
pH of between about 4 and about 10; said composition further comprising an
oil phase, said oil phase having a relatively low level of unsaturation;
said composition further comprising a stabilizing system selected from the
group consisting of:
a) at least one oil-soluble antioxidant;
b) a chelating agent and at least one oil-soluble antioxidant;
c) a chelating agent; and
d) a chelating agent and an antioxidant present in each of the oil and
water phases of said emulsion;
said composition retaining at least about 70% of said retinoids after 13
weeks' storage at 40oC.
Additionally, there are provided herein oil-in-water emulsions having
novel emulsification systems. The oil-in-water emulsion compositions of
this invention preferably contain:
a) an emulsifier system selected from the group consisting of:
i) a mixture of glyceryl stearate and polyethylene glycol 100 stearate;
ii) cetearyl alcohol and cetearyl glucoside;
iii) a mixture of a polyethylene glycol ether of stearyl alcohol of the
formula:
CH3 (CH2)16 CH2 (OCH2
CH2)n OH
wherein n is 21 and a polyethylene glycol ether of stearyl alcohol of the
formula:
CH3 (CH2)16 CH2 (OCH2
CH2)n OH
wherein n is 2; and
iv) a mixture of sorbitan stearate and polysorbate 60 (a mixture of
stearate esters of sorbitol and sorbitol anhydrides condensed with 20
moles of ethylene oxide);
b) a co-emulsifier selected from the group consisting of: cetyl alcohol,
stearyl alcohol and mixtures thereof;
c) an oil phase present in the amount of from about 2 to about 20 percent
by weight of the total emulsion composition comprising:
i) a light, dry absorbable oil and
ii) substantive, emollient oils or waxes
wherein such dry absorbable oil and such substantive emollient oil are
present in a ratio of from about 1:3 to about 10:1.
Claim 1 of 37 Claims
1. A topical oil-in-water emulsion composition comprising:
a) an emulsifier system selected from the group consisting of:
i) a mixture of glyceryl stearate and polyethylene glycol 100 stearate;
ii) cetearyl alcohol and cetearyl glucoside;
iii) a mixture of a polyethylene glycol ether of stearyl alcohol of the
formula:
CH3 (CH2)10 CH2 (OCH2
CH2)n OH
Wherein n is 21 and a polyethylene glycol ether of stearyl alcohol of the
formula:
CH3 (CH2)16 CH2 (OCH2 CH2)n
OH
Wherein n is 2; and
iv) a mixture of sorbitan stearate and polysorbate 60 (a mixture of
stearate esters of sorbitol and sorbitol anhydrides condensed with 20
moles of ethylene oxide);
b) a co-emulsifier selected from the group consisting of: cetyl alcohol,
stearyl alcohol and mixtures thereof;
c) an oil phase present in the amount of from about 2 to about 20 percent
by weight of the total emulsion composition comprising:
i) a light, dry absorbable oil and
ii) substantive, emollient oils or waxes
wherein said light dry absorbable oil and said substantive oil or wax are
present in a ratio of from about 1:3 to about 10:1;
d) a retinoid;
said composition having a pH of from about 4 to about 10.
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