JPS5988421A - Sebum spread reducing composition - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION Sebum or oil of the skin Ii'f is produced in the sebaceous glands located in the sebaceous apparatus of the skin and reaches the skin surface through the ducts of the hair follicles. When there is excess sebum on the skin surface, it usually results in oily skin.
It becomes a state of attractive makeup known as 1j. Sebum also plays an important role in the pathogenesis of acne scars. The activity of the sebaceous glands in perinatal patients is markedly increased, and the rate of sebum secretion is also greatest in those with the most severe forms of acne.

Thus, the spread of sebum on the skin surface is an important cosmetic parameter. This is because the distribution of sebum on the skin surface determines whether the skin becomes greasy or not, and it also depends on the degree of acne.

Therefore, taking into account the affected skin areas of patients with acne scars and skin lesions characterized by excessive sebum secretion or the presence of sebum,
It would be advantageous to have a means of reducing the flow of sebum to human skin.

It has now been discovered that quaternary halide salts of N,N,1J-1 realkylaminoalkylene gluconamides can be used to effectively reduce the extent of sebum spread.

The quaternary halide salts of N,N,N-)realkylaminoalkylene gluconamides used in the present invention are disclosed in U.S. Pat.
No. 290 describes its use as a topical and cosmetic emollient. However, its use as a drug that can effectively reduce the spread of sebum on 1η of human skin is
hitherto unknown.

The present invention provides treatments by reducing the spread of sebum on human skin (including the scalp); 11. N,
The present invention relates to methods and compositions for topical application of quaternary halides of N-trialkylaminoalkylene gluconamides.

Such methods provide a physiologically effective treatment of human skin, and cosmetics formulated specifically for use on oily skin,
It has useful uses such as pore-reducing lasers, scalp and hair summer shampoos and conditioners. Following this usage-C
1 It is felt that the skin becomes less oily, and in Kashishin's treatment, reducing the excessive spreading of the skin 11 is particularly desirable to help prevent the spread of raccoon hemorrhoid symptoms.

The active compounds used in the invention are N,N,N-)realkylaminoalkylene gluconamides of the formula: is a quaternary halide, and its quaternary chloride salt having the formula is most preferred.

A preferred quaternary chloride salt of formula ■, chemically known as α-gluconamidopropyldimethyl 2-hydroxyethylammonium chloride (0TIPA name = Quaternium 22), is manufactured by Nokun Dyke Company (
It is commercially available as a free-flowing 60% aqueous solution (60% active) under the trade name "Cerafil 60" by Van Dyk Company, Engineering, NC, ).

The quaternary nolides of Formula I and most preferably Formula H treat skin conditions characterized by excessive secretion or presence, or θ(1)m, of significantly reduced spread of sebum on human skin. The aim is to take advantage of this beneficial effect and thereby ameliorate the symptoms by topical application of suitable compositions containing this quaternary halide. Such topical compositions can be cosmetic formulations used for oily skin or anti-inflammatory formulations with therapeutic properties.

Specific types of topical cosmetic compositions include, for example, lotions and creams for the hands, face and body, scalp and hair conditioners, lotions, gels and shampoos. However, it is not definitive. Such forms of composition are readily prepared by skilled cosmetic chemical formulators. Similarly, the specific form of the composition is also determined. In that respect, the therapeutically active ingredients of anti-zatara, such as benzoyl peroxide,
Sulfur, resorcinol/l/, retin sensitive derivatives, chlorohydroxyquinoline, hormonal agents and antibacterial agents, etc. are also inconclusive.

The quaternary halides of formulas 1 and 2 above are non-toxic to human skin, are compatible with hydrophilic adjuvants, and can be easily incorporated into such topical compositions.

To create such a composition, the product is applied in such a way that the activity of the halides and H is substantially negated in reducing the extent of sebum spread on the surface of the skin when the product is applied topically. It should not be formulated or include such excipients or ingredients. In fact, the product should be physiologically compatible with the skin and cosmetically sophisticated.

For purposes of the present invention, an effective amount of a quaternary halide of Formulas 1 and most preferably 2 is included as an active ingredient in the topical compositions used herein to reduce the extent of sebum spread on the skin. generally at least about 0.05% by weight based on the total composition weight (i.e., %W/W
) is known to be appropriate, but about 0.3 to about 6%w/
w/w is preferred, and about 0.5 to about 3% w/w is most preferred.

The present invention thus treats human skin characterized by excessive sebum secretion or sebum in order to ameliorate the symptoms of such a condition by reducing the degree of spread of sebum on the human skin. A method is provided, comprising a composition comprising an active amount of an N,N,Ii-trialkylaminoalkylene gluconamide of formula I or formula I as an active ingredient for reducing the extent of sebum spread. It consists of topical application to human skin with specific characteristics. The present invention discloses a novel anti-m4M for topical scar cloth consisting of an effective amount of this halide 1 or H as an active ingredient to reduce the spread of sebum.
Compositions are also provided.

The method of the present invention, the compositions used herein, and the quaternary halides reduce the degree of sebum spreading provided by C.
A further understanding will be obtained by referring to the following examples.

The procedure used in testing the reduction in sebum spread is as follows.

Test Procedure Place 2-4 vy/crfi of the material to be tested on the back of your hand and spread it evenly into a circle approximately 2 inches in diameter.

After application of the test material, it is left at room temperature for 1 hour to achieve equilibrium. After this time, a 4μ11 drop of artificial sebum supplemented with 213% by weight of Spare is measured using a micropipette and placed approximately in the center of the treated area. The prescription for artificial sebum is as follows.

Ingredients %-w
/w Squalene 18.0 Corn oil 7.0 Glyceryl dioleate: Olein 1 (1: 1) mixture 1.0 Oleic acid 27.0 Seraphyll 140 (Decyl oleate) 43
．． 5 Cholesterol Palmitate
1.0 cholesterol 2.
5iooo,.

After a 10 minute spreading period, diameter 1. Place an on glass cylinder in the center and extract the sebum in the recess of the cylinder. This extraction was carried out using hexane 2X in a glass cylinder.
This is done by pipetting a 0.57 fit for 30 seconds without stirring. Both extracts are pipetted into test tubes and evaporated to dryness using a nitrogen gas evaporator.

Redissolve the residue in 0.2 ml hexane and add 10 μl of tetracosane to the sample as an internal standard. The amount of sebum in the glass cylinder is determined by gas-liquid chromatography (G
LO).

From this data, the total area covered by the spread of artificial sebum is calculated as 1γ. The greater the amount of suhuarenes recovered from the extract, the greater the rate of reduction in the spread of sebum.

Example 1 A cosmetic product that can be applied to oily skin and deeply cleanses the pores is prepared according to the following recipe. Unless otherwise indicated, all amounts are parts by weight.

Table 1 7 Luco/l/ *49. l v/v salicylic acid
0.5 acetone
0.9 v/v Setiares-27 (Table [j
g+4E agent) 1.0 Propylene glycol 0.5 Menthol
0.05 tartaric acid
0.25 fragrance
0.05 water (purified) tene fk
100.00 v/v (43, *
Equivalent to 43.2% v/v of absolute alcohol.

Example 2 Compositions were prepared by mixing the pore cleanser of Example 1 with Serafil 60 at the percentage concentrations shown in Table 2, and the percentage reduction in sebum spread of each composition was recorded.

Table 2 3゜OO%/W Serafile 60 (control) Negligible 5 (Basic (2) b, o, v-% tt
12.3c, 0.
5% // 26
,4d, 1.0% tt
41.2e, 1.5% //
29.4**f. 2.
0% tt 〃u tt 3
8.8g, 25% //
33.8**h, 3.0%y
42.4j,, 5.
0% // 70
．． 4*) Average of readings from 6 studies **) Exceptionally low percentage due to inclusion of 1 patient who did not respond.

Example 3 This example shows the extent to which sebum spreads on human skin when Serafil 60 is added to two types of commercially available a-apparatus creams (each containing 10% penzoyl peroxide as an anti-swelling active ingredient). shows a significant decrease.

TABLE 3 A, 7i, j Color 0046 B, Vanishing 09 2 21 *) Sold by Richardson-Vicks, Wilton, CT Example 4 The following basic shampoo formulation, A is 1% (w/w) V and E were prepared without adding Serafil 60, and the rate of reduction in sebum spread was tested.

Table 4 Sulfate (30%) 40.0
4% Citric anhydride 0.3 Water 59.7B, Atriwaum lauryl ether sulfate (30%) 40.0
60% power! (Mizukuenbaku o3 Seraph Ill 60 l, Q Water 58.7 Example 5 A needle pack 71ζ for a hair moisture replenishing cleanser containing 3% W/'W SeraFil 6o and containing no oil is made. During the test, The reduction in sebum spread is 46%. In contrast, a similar formulation without Serafil 6o (ie, replaced with water) shows a reduction of 35%.

Table 5 Carhomer 934 (gel) 0.2 (
1 Methylparaben 0.18"
"L Deionized water 2.00 Thorium lauryl amino acid pione) 2.
00 Amphotericu 2 3.00C
Zeng 1 (1,000 legs water)
2.00 water 11 sodium calcide)
0.08D? Jj Purified Water 1.00 Cerafil 60
3.00℃ part vinegar made myristyl 100 cetostearyl alcohol 1.00 myristic acid
1.50 silacrine 1'glyceryl 1.50 myristyl alcohol
0.25 Pu I Covil Puff Hen
0.10℃ part imidazolidinyl urea 030 purified water 1.00 meter
ioo, o.

Dissolve methylhalabane in water, add Carbomer 934, and heat to 70°C to produce Ag. Separately prepare Part B and Part D, and heat each to 75-80°C. Mix parts B and D together with part A. Make part E, heat to 80°C, and add to the previous mixture while stirring. Make 0 parts and add to the previous mixture while stirring. Allow the mixture to cool. At about 45°C the emulsion passes through an inversion phase and changes color to white.

Make part F and mix into the previous mixture at about 40°C.

Allow the mixture to cool to room temperature.

It will be understood by those skilled in the art that this invention is not limited to the specific embodiments provided, but that modifications may be made without departing from the spirit of the invention.

Agent: Patent Attorney Yatabe Sasai (1 person)

Claims (1)

[Scope of Claims] 1. A drug for treating human skin in order to improve the skin condition of human skin characterized by excessive secretion or productivity of sebum by reducing the degree of spread of sebum on the skin surface. As an ingredient to reduce the spread of sebum,
Formula [: In the formula,
A composition for topical dermal application comprising a quaternary halide active substance of N,N,N-)realkylaminoalkylene gluconamide having the following properties: 2. The composition of claim 1, wherein in the formula given, X is chloro and n is the integer 3. 3. A drug for treating human skin characterized by excessive sebum secretion in order to improve the skin condition by reducing the spread of sebum on the skin surface. , a non-toxic cosmetic carrier suitable for topical skin application and as an active ingredient without reducing the spread of sebum, N, N having the formula: where X is chloro or bromo and is an integer from nu2 to 4 , N −) Effective Nx of quaternary halide of IJ alkylaminoalkylene gluconamide
The composition of paragraph 1 comprising: 4. The composition of claim 3, wherein in the given formula n is an integer 3. 5. A drug for treating human skin characterized by excessive sebum secretion in order to improve the skin condition by reducing the spread of sebum on the skin surface. , a non-toxic cosmetic carrier suitable for topical skin application and an effective ffi of a quaternary chloride of a N,N,N-)realkylaminoalkylene gluconamide with the formula as an active ingredient that reduces sebum spread. 1st
composition of the term. 6. The amount of quaternary chloride in the composition is at least 0.
．． The composition of claim 5, wherein the composition is 0.5% by weight. 7. The composition of claim 5, wherein the quaternary chloride content in the composition is from about 0.3 to about 6% by weight. 8. The grade of quaternary chloride in this composition is about 0.5.
6. The composition of claim 5, wherein the composition is from about 3% to about 3%. 9. As an active ingredient for reducing the spread of sebum, N,N,N-)realkylaminoalkylene gluconamides of the formula: An effective amount of a topical anti-acne composition comprising an effective amount of a quaternary halide is applied to the affected area to reduce the extent of acne spread on the skin surface of a person suffering from 4M. Composition. 10. The composition of claim 9, wherein n is an integer 3 in the formula given. 11. A topical anti-seizure composition comprising an effective amount of a quaternary chloride of N,N,N-)realkylaminoalkylene gluconamide having the formula as an active ingredient for reducing sebum spread; By applying it to the affected area, it can be applied to the skin surface of the person suffering from the disease.
9. The composition of item 9 for reducing the degree of spread of J fat. 12. The composition of claim 11, wherein the amount of quaternary chloride in the composition is at least 0.05%. 13. The amount of quaternary chloride in this composition is about 0.3
12. The composition of claim 11, wherein the composition is from about 6% to about 6%. 14. The amount of quaternary chloride in the composition is about 0.5
12. The composition of claim 11, wherein the composition is from about 3% to about 3%.