KR100402576B1 - Cosmetic composition containing retinol by multiple stabilization - Google Patents

Abstract

The present invention relates to a technique and a prescription for improving the stability of retinol and maintaining its activity in cosmetics containing retinol, which is an unstable active substance, and in particular, because it is oxidized and unstable by contact with air or moisture. Retinol, a fat-soluble active ingredient that was limited in use in oil-in-water cosmetics, was encapsulated in a matrix mixed with phospholipids, a wall, and encapsulated in cyclodextrins with tocopherols as an antioxidant. The stabilized raw material is dispersed in a mixture of propylene glycol and hydrogenated lecithin, and then dispersed in an oil-in-water (O / W) cosmetic containing tocopherol, dibutyl hydroxytoluene, and an appropriate amount of antioxidant at 20 ° C to 50 ° C. Multiple stabilization avoids the maintenance of active ingredients according to the improvement of retinol stability. It relates to a cosmetic composition having improved affinity and feeling.

Description

Cosmetic composition containing multiple stabilization of retinol {Cosmetic composition containing retinol by multiple stabilization}

The present invention relates to techniques and prescriptions for improving the stability of retinol in cosmetics containing retinol, which is an unstable fat-soluble active substance.

Retinoid-based raw materials, including retinol, which have been widely used in medicine because of excellent cell regeneration, anti-wrinkle and improvement effects, have been limited in use in cosmetics because they are easily oxidized by air or moisture and temperature-sensitive instability. Therefore, in order to improve the stability, cosmetic encapsulation and its advanced form of double encapsulation and stabilization as a raw material using liquid crystal, etc., take a water-in-oil (W / O) type of emulsion or contain various antioxidants Although stabilization through prescription has been studied, in particular, since stability over time is difficult to be considered sufficient, the inventors of the present invention plan to stabilize both as a raw material and a cosmetic composition containing the raw material at the same time. Under the proposition of long-term stability and continuation of activity, studies on the development of cosmetics containing multiple stabilization of retinol were conducted.

For encapsulation used in cosmetics, a general encapsulation in which an inner phase is used as an active ingredient and an outer phase wall material is wrapped in a film form, and a matrix in which an effective ingredient and a wall material are mixed in a continuous phase. The encapsulation can be divided into two methods. In general encapsulation, the dissolution of the active ingredient due to the swelling of the wall, the penetration of water into the inner phase, and the encapsulation of the matrix are difficult to stabilize completely due to the dissolution of the active ingredient through the capillary of the capsule particles.

In addition, water-in-oil (W / O) type emulsions have been generally used for the stabilization of formulations, but they are not considered to be complete stabilization, and they are not satisfactory.

Therefore, the present inventors conducted a study to solve the above problems, as a result of encapsulating the retinol, an active ingredient for cosmetics, in the inner phase (phosphoridide) as a wall to form a continuous phase encapsulated in a matrix form of antioxidant and tocopherol It is then enclosed in cyclodextrin and dispersed in a mixture of propylene glycol and hydrogenated lecithin, which is then added to an oil-in-water (O / W) cosmetic containing tocopherol and dibutyl hydroxytoluene as an antioxidant, The present invention has been completed by multiple stabilization of the active ingredient, which is susceptible to oxidation, by primary encapsulation after the stable encapsulation with an antioxidant, and then further dispersed to be more stabilized, and then secondarily dispersed in a cosmetic having a proper antioxidant prescription.

The specific objects and applications of the present invention are clearly presented to those skilled in the art from the following detailed description of the invention.

Next, the present invention will be described in more detail.

Stabilization of the retinol in the cosmetics stabilized by retinol according to the present invention is achieved by the following method.

First, the hydrophilic and lipophilic groups of phospholipid, which are relatively easy to encapsulate, have excellent skin affinity, and have a good feeling when encapsulating, form a fat-soluble active ingredient, retinol, and a matrix. The capsules have 60.0 to 80.0% by weight (preferably 65.0 to 75.0%) and tocopherol 20.0 to 40.0% by weight (preferably 25.0 to 35.0%). To the cyclodextrin in a weight ratio of 0.5: 1 to 2: 1. (0.8: 1 to 1.5: 1 is preferred.) This entrapped state is regarded as a raw material, and it is kept sealed in refrigeration and used in the manufacture of cosmetics.

60.0 to 66.7% (weight) of the raw material in the inclusion state is first dispersed with sufficient stirring at room temperature so as to be completely dispersed in 30.0 to 33.3% (weight) of the propylene glycol and 1.6 to 2.4% (weight) mixture of hydrogenated lecithin. Oil-in-water containing 0.1 to 2.0% (by weight) (preferably 0.8 to 1.5%) of tocopherol and 0.01% to 0.5% (by weight) (preferably 0.05 to 0.2%) of dibutylhydroxytoluene as an antioxidant. When the mixture is stirred and dispersed at about 20 ° C. to 50 ° C. (preferably about 30 ° C. to 40 ° C.), the cosmetic having the object of the present invention can be obtained.

The cosmetics prepared by the above method encapsulate the retinol as a fat soluble active ingredient in the form of a matrix, and then encapsulate in cyclodextrin with tocopherol as an antioxidant to significantly reduce instability due to elution of the inner phase. This encapsulated raw material not only has better dispersibility than capsules when dispersed in cosmetics, but also has a sustained release delivery system that protects the active ingredient until it is applied to the skin so that the active ingredient is gradually released to have continuous activity. In addition, this encapsulated raw material is dispersed in a mixture of propylene glycol and hydrogenated lecithin, which has excellent moisturizing and skin-friendly properties, which improves skin penetration of the active ingredient, improves the feeling of use, and reinforces the sustained release delivery system, and at the same time, stabilizes the active ingredient. It has a synergistic effect. The mixed solution obtained by dispersing the cladding material at room temperature is effective to be produced by high temperature process by dispersing it in water-in-oil (O / W) type cosmetics using an appropriate amount of tocopherol and dibutyl hydroxytoluene as antioxidants at 20 ° C to 50 ° C. Minimizes the inactivation of retinol as an ingredient and prevents oxidation due to contact with moisture obtained when applied to water-in-oil (O / W) type cosmetics. You can get it.

Next, the constitutional and working effects of the present invention will be described in more detail as examples and experimental examples.

Preparation Example 1 and Comparative Example 1-3 Cosmetics

Furtherance Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Retinol Matrix Capsules 2.10 2.10 2.10 2.10 2. Tocopherol 0.90 - 0.90 0.90 3. cyclodextrin 3.00 - 3.00 3.00 4. Propylene Glycol 3.00 - - 3.00 5. Hydrogenated Lecithin 0.20 - - 0.20 6. Tocopherol 1.00 - - - 7. Dibutylhydroxytoluene 0.10 - - - 8. Glyceryl Stearate 0.50 0.50 0.50 0.50 9. Cetostearyl Alcohol 0.80 0.80 0.80 0.80 10. Squalane 8.00 8.00 8.00 8.00 11.Tri (capryl, caprylic acid) glycerin 3.00 3.00 3.00 3.00 12. Methylpolysiloxane 1.00 1.00 1.00 1.00 13.Glyceryl Stearate / Pig-100 Stearate 1.50 1.50 1.50 1.50 14. Concentrated glycerin 10.00 10.00 10.00 10.00 15. Lysolecithin 2.50 2.50 2.50 2.50 16. Xanthan Gum 0.20 0.20 0.20 0.20 17. Polyacrylamide / C 13-14 Isoparaffin / Laures 7 0.80 0.80 0.80 0.80 18. Allantoin 0.20 0.20 0.20 0.20 19. Preservatives Quantity Quantity Quantity Quantity 20. Purified water to 100 to 100 to 100 to 100 21. Spices Quantity Quantity Quantity Quantity

Manufacturing Method:

The raw materials 6-13 and the raw materials 14-20 were heated to about 80 ° C., respectively, mixed, emulsified (3000 rpm, 5 minutes), cooled to about 45 ° C., and then the raw material 21 was added. The raw material 21 was sufficiently stirred and cooled again. 1 was mixed with the raw material 2 and included in the raw material 3, dispersed in a mixed solution of the raw material 4 and the raw material 5, stirred and cooled to room temperature to prepare a cosmetic. The content of the first retinol of the preparation and comparative examples corresponds to 1200 IU.

Test Example 1

The stability of the cosmetics obtained in Preparation Example 1 and Comparative Examples 1 to 3 was tested by measuring the titer of retinol. The test method was performed according to the Korean Pharmacopeia Vitamin A quantitative method. The results are shown in the following Tables 2-6.

Comparison of stability when left at room temperature for 4 weeks sample Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Potency (IU) 1175 922 1097 1152 efficiency (%) 97.9 76.8 91.4 96.0

Comparison of stability when left at 50 ℃ for 1 week sample Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Potency (IU) 1148 785 1066 1099 efficiency (%) 95.7 65.4 88.8 91.6

Comparison of stability when left at 50 ℃ for 2 weeks sample Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Potency (IU) 1092 535 799 1026 efficiency (%) 91.0 44.6 66.6 85.5

Comparison of stability when left at 50 ℃ for 3 weeks sample Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Potency (IU) 960 259 728 904 efficiency (%) 80.0 21.6 60.7 75.3

Comparison of stability when left at 50 ℃ for 4 weeks sample Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Potency (IU) 936 130 692 820 efficiency (%) 78.0 10.8 57.7 68.3

As can be seen in Tables 2 to 6, the stability of the cosmetics obtained in Preparation Example 1 is a matrix-encapsulated raw material, Comparative Example 1, which is dispersed in oil-in-water (O / W) type cosmetics without using an antioxidant, after matrix encapsulation. Comparative Example 2, a raw material enclosed in cyclodextrin with tocopherol and dispersed in oil-in-water (O / W) cosmetics without using an antioxidant, propylene glycol and hydrogenei Compared with Comparative Example 3, which was dispersed in Tied Lecithin and then dispersed in oil-in-water (O / W) type cosmetics without using an antioxidant, its stability was significantly improved, and especially when it was left at a high temperature for a long time, the stability was improved very well.

Test Example 2

Formulation stability of Preparation Example 1 and Comparative Examples 1-3 cosmetics

In order to compare the formulation stability of the cosmetics obtained in Preparation Examples and Comparative Examples 1 to 3 after storage for each of the following conditions and evaluated the results are shown in Table 7 below.

division Preparation Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 2 months at room temperature stability Instability stability stability 50 ℃ 2 months stability Instability Instability Instability 2 months cycling stability Instability Instability stability Color change after 2 months storage at 50 ℃ Good Severe discoloration discoloration Slightly discoloration Change in flavor after 2 months storage at 50 ℃ Good A bad smell Deodorant Slightly deranged

As confirmed in Table 7, the cosmetic composition of Preparation Example 1 of the present invention shows remarkable formulation stability compared to Comparative Examples 1 to 3.

Test Example 3

Preparation Example 1 and Retinol Matrix Capsules were combined with tocopherol in cyclodextrin and then dispersed in propylene glycol and hydrogenated lecithin to compare the usability of cosmetics dispersed in water-in-oil (W / O) cosmetics.

Usability of the cosmetics dispersed in the water-in-oil (W / O) cosmetics by preparing the preparation example 1 and the retinol matrix capsule with tocopherol in cyclodextrin and then dispersed in propylene glycol and hydrogenated lecithin (the same raw material as Preparation Example 1) To compare the results, the average scores were obtained by comparing the feelings during and after application with a four-point evaluation method by 60 inspectors consisting of men and women between 20 and 40 years of age.

※ Evaluation standard

1: dull and oily when applied, sticky after application

2: It feels light and smooth when applied, but sticky after application

3: dull and oily when applied, but fresh after application

4: It feels light and smooth when applied, and it is fresh after application.

※ Evaluation results

Preparation Example 1 Cosmetic: 3.72

Cyclodextrins with Retinol Matrix Capsules with Tocopherols

After entrapment in propylene glycol and hydrogenated lecithin

Cosmetics dispersed in water-in-oil (W / O) cosmetics: 1.98

As can be seen from the above results, the oil-in-water (O / W) type cosmetics of the present invention are oils using the same raw material as the retinol matrix capsules, which are contained in a cyclodextrin with tocopherol and then dispersed in propylene glycol and hydrogenated lecithin. Compared to heavy water (W / O) cosmetics, it has a very light and fresh feeling.

As shown through the above test examples, encapsulated retinol in an inner phase (phosphoride) as a wall and encapsulated in a matrix form into a continuous phase was encapsulated in cyclodextrin with an antioxidant tocopherol and then propylene glycol and hydrogenase. The cosmetics (Preparation Example 1) obtained by dispersing in a mixed solution of tide lecithin and dispersing it in an oil-in-water (O / W) type cosmetic having an appropriate amount of tocopherol and dibutylhydroxytoluene as an antioxidant (Preparation Example 1) were used as a matrix encapsulated raw Cosmetics (Comparative Example 1) obtained by dispersing in an unused oil-in-water cosmetic (O / W) or oil-in-water (O / W) type without the use of antioxidants as a raw material encapsulated in cyclodextrin with tocopherol after matrix encapsulation Cosmetics obtained by dispersing in cosmetics (Comparative Example 2), cyclodex with tocopherol after matrix encapsulation The stability was significantly improved compared to the cosmetics (Comparative Example 3) obtained by dispersing the raw material entrapped in trine in propylene glycol and hydrogenated lecithin and then dispersing it in oil-in-water (O / W) cosmetics without using antioxidants. In terms of the feeling of use, it was found that the raw material encapsulated in cyclodextrin with tocopherol after dispersing the matrix in propylene glycol and hydrogenated lecithin was superior to the cosmetics obtained by dispersing it in water-in-oil (W / O) cosmetics. Can be.

As can be seen from the above detailed description, the encapsulation of retinol, a fat-soluble effective ingredient that has been extremely limited in use in oil-in-water (O / W) cosmetics because it is oxidized by air or moisture and is unstable, is an antioxidant. Encapsulated in cyclodextrin together with intocopherol, and then dispersed in a mixture of propylene glycol and hydrogenated lecithin, this dispersion is dispersed in an oil-in-water (O / W) cosmetic containing tocopherol and dibutylhydroxytoluene as an antioxidant. The cosmetics obtained by dispersing at from -50 占 폚 bring about an improvement in stability of retinol and usability as a cosmetic.

Claims (2)

60.0 to 66.7% of the raw material in which retinol, a fat-soluble active ingredient for cosmetics, was encapsulated in an inner phase, phospholipid as a wall, and encapsulated in a cyclodextrin by mixing together the tocopherol as an antioxidant. ) Is dispersed in a mixture of propylene glycol 30.0 to 33.3% (weight), hydrogenated lecithin 1.6 to 2.4% (weight) by stirring sufficiently at room temperature 60.0 to 66.7% of the raw material in which retinol, a fat-soluble active ingredient for cosmetics, was encapsulated in an inner phase, phospholipid as a wall, and encapsulated in a cyclodextrin by mixing together the tocopherol as an antioxidant. ) To a dispersion of 30.0 to 33.3% (weight) of propylene glycol and 1.6 to 2.4% (weight) of hydrogenated lecithin with sufficient stirring at room temperature, and 0.1 to 2.0% (weight) of tocopherol as an antioxidant. And a cosmetic prepared by stirring and dispersing in an oil-in-water (O / W) type cosmetic containing 0.01% to 0.5% (weight) of dibutylhydroxytoluene at 20 ° C to 50 ° C.