JP2008290951A - Emulsion composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To prepare a preparation that exhibits further stable emulsifiability and is widely used although a sphingoglycolipid or the like has an important role for the skin as an intercellular lipid and is used for a cosmetic. <P>SOLUTION: The emulsion composition is obtained by mixing one or more kinds of a sphingoglycolipid and a phospholipid with a polyhydric alcohol containing two or more hydroxy groups in the molecule, a polyhydric alcohol containing three or more hydroxy groups in the molecule selected from one or more kinds of a glycerin, a diglycerin and a polyglycerin, one or more kinds of saccharides and an oil. Namely, the emulsion having a fine particle diameter is obtained by mixing three or more kinds of polyhydric alcohols. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to an emulsion having very small particles and no surfactant.

  Various emulsified compositions used for cosmetics and pharmaceuticals have been prepared. In addition, glycosphingolipids have an important role in the skin as intercellular lipids, and have a role of increasing usefulness by blending in cosmetics and the like. Prior patents using glycosphingolipids (glycolipids) are “emulsified compositions comprising a glycolipid, a water-soluble polyhydric alcohol having two or more hydroxyl groups in the molecule, and an oil” ( Patent Document 1), “Gel with high-pressure dispersion of glycosphingolipid and glycerin and / or diglycerin” (see Patent Document 2), “High-pressure emulsification treatment of oil-soluble active ingredient, oil, polyhydric alcohol and surfactant. In addition, a skin external preparation characterized by mixing and stirring water and a water-soluble component ”(see Patent Document 3) is actually applied.

JP 59-39338 A JP 2000-128760 A JP 2002-338499 A

These emulsified compositions exhibit emulsifying properties to a certain degree of fine particles, but in order to effectively use the highly effective glycosphingolipid, it is possible to further reduce the size of the particles.
As a result, appearance and stability, which are important factors for cosmetics, are also improved, and transparent preparations are possible, and the range of choices for prescriptions is widened so that more people can use them. The

As a result of intensive studies, the present inventors have made it possible to use three or more kinds of polyhydric alcohols. That is,
One or more of glycosphingolipids and phospholipids, a polyhydric alcohol having two hydroxyl groups in the molecule, and a polyvalent alcohol having three or more hydroxyl groups in the molecule selected from one or more of glycerin, diglycerin and polyglycerin This problem has been solved by using an emulsified composition containing alcohol, sugar and oil.
Note that% is% by weight, and in the following explanation,% is all% by weight.
There are various types of glycosphingolipids and phospholipids, both of which achieve the gist of the present invention. However, in our study, considering the effectiveness on the skin, the size of the particles, etc. Lipids were the most ideal.
Glycosphingolipid is a general term for galactosylceramide, glucosylceramide, galactosylphytoceramide, glucosylphytoceramide, sphingomyelin, and the like. One or more of them are used, but a mixture obtained by extraction from animals and plants is not problematic. Furthermore, as a result of studies by the present inventors, the glycosphingolipids extracted from animal brains and medulla and the glycosphingolipids extracted from microorganisms showed the best effects. Although these contain some components other than glycosphingolipid, there is no problem. .
The amount of glycosphingolipid and phospholipid varies depending on the type of glycosphingolipid and phospholipid, the type, amount and mixing ratio of polyhydric alcohol, and the type and amount of oil.

There are various types of sugar, but there is no particular limitation, but particularly preferred are sorbitol, maltitol, glucosyl trehalose, maltosyl trehalose, maltotriitol, maltotetritol, maltotriosyl trehalose, maltopentitol One or more of monosaccharides such as erythritol, pentaerythritol, dipentaerythritol, threitol, arabitol, xylitol, ribitol, galactitol, mannitol, lactitol, cytilitol, laminitol, glucose, sucrose, oligosaccharide, and sugar alcohol are preferable. .
The polyhydric alcohol having two hydroxyl groups in the molecule is not particularly limited. For example, ethylene glycol, diethylene glycol, polyethylene glycol (average molecular weight 1000 or less), propylene glycol, 1,2-pentanediol, 1,3- Examples include butylene glycol, dipropylene glycol, 1,2-hexanediol, 1,2-octanediol, isoprene glycol, and hexylene glycol. Particularly preferred in the present invention include 1,3-butylene glycol and propylene glycol.
When a polyhydric alcohol having 3 or more hydroxyl groups in a molecule selected from at least one selected from glycerin, diglycerin and polyglycerin is described, polyglycerin is preferably decaglycerin or less, and polyglycerin is an emulsifying method. However, it may be used alone, but is preferably used in combination with glycerin or diglycerin.
Further, the sugar is preferably 5 to 90%, more preferably 10 to 80%, and the polyhydric alcohol having two hydroxyl groups in the molecule, preferably 5 to 70%, more preferably, in view of the total amount of the polyhydric alcohol. The polyhydric alcohol having 3 or more hydroxyl groups in the molecule selected from 10 to 60%, glycerin, diglycerin and polyglycerin is preferably 5 to 70%, more preferably 10 to 60%.
However, when dipropylene glycol, 1,2-pentanediol, or 1,2-octanediol is used, the upper limit is further limited, so the polyhydric alcohol having a smaller amount of use or having two hydroxyl groups in another molecule is used. It is preferable to use together.

There is no particular limitation on the oil content. Avocado oil, almond oil, olive oil, beef tallow, turtle oil, mink oil, squalene, and other animal and vegetable oils and their hydrogenated oils, cetanol, stearyl alcohol, oleyl alcohol, lanolyl alcohol, cholesterol, phytosterol and other higher alcohols, myristin Esters such as myristyl oleate, oleyl oleate, decyl oleate, octyldodecyl myristate, hexyldecyl dimethyloctanoate, oil-soluble vitamins such as vitamin E and vitamin A, silicone oil, oil-soluble animal and plant extracts, flavors, etc. Oil-soluble drugs such as ceramide can be blended. These are used singly or in combination of two or more, but squalane and esters having 20 or more carbon atoms are particularly preferred in the present invention, and formulated so that 50% or more of the oil is occupied by squalane or esters having 20 or more carbon atoms. It is more suitable for the purpose of the present invention.
The amount of oil varies depending on the type of oil, the type and amount of polyhydric alcohol, glycosphingolipid, and phospholipid, but the proportion of the total amount is preferably 0.1 to 40%, more preferably 1 to 30%. Good.
Although it is not an essential component with respect to water, it was also found that emulsifiability is further improved by adding a small amount.
In addition, depending on the purpose of the formulation and the type of raw material to be blended, water-soluble drugs, alcohol, water, etc. can be blended, but the types and amounts that can be blended are limited depending on the blending amount, type, etc. It goes without saying that there are things.

  Further, from various experimental studies, FIG. 1 and FIG. 2 show the ternary phase diagrams regarding the three components of the oil component, such as the amount of glycosphingolipid and phospholipid, polyhydric alcohol and the like. The gray portion varies depending on the type of the blend, but is a portion that roughly meets the spirit of the present application.

In the emulsification method, a necessary amount other than the oil is weighed, heated to a temperature or higher until the blended substance is dissolved and stirred, and then the oil is added and stirred.
In addition, a method may be employed in which all the blends are weighed in necessary amounts and heated to a temperature or higher until the blended substances are dissolved.
As a stirring method, a commonly used homomixer, homodisper, homogenizer, or ultrasonic emulsifier can be used, but since a so-called surfactant is not used, it is better to use an emulsifier having a certain emulsifying power. Good.
Furthermore, using high-pressure emulsifiers such as microfluidizer (trade name), nanomizer (trade name), and optimizer (trade name) makes the particles finer and allows more prescriptions to be selected. improves.
A high pressure emulsifier may be used for all stirring, but when emulsifying in two stages, it is more effective to use it in the latter stage.

Further, depending on the application, it is possible to prepare a preparation by adding an aqueous phase to the above emulsion.
Water, polyhydric alcohol, ethanol, water-soluble vitamins, preservatives, water-soluble animal and plant extracts, and other water-soluble drugs can be added to the aqueous phase. However, it goes without saying that the amount and type of substances that reduce the emulsion stability are limited.
In this case, the emulsification does not require particularly strong emulsifying power.

Examples and Comparative Examples are described below, but the Examples are not limited to these.
In addition, the number in a table | surface represents a weight part.

The notes in the table are as follows.
Note 1) Product name Bioceramide CH manufactured by LABORATOIRES SEROBIOLOGIQUES
Note 2) Trade name Torunale manufactured by Hayashibara Biochemical Laboratories Inc. 3) Product name Fermented Ceramide manufactured by Kibun Food Chemifa Inc. Note 4) Product name Basis LS-60HR manufactured by Nisshin Oilio Inc.
Note 5) Product name SLP-PC70HS manufactured by Sakai Oil Co., Ltd.
Note 6) Product name Hibiswako 103 manufactured by Wako Pure Chemical Industries, Ltd.
Note 7) An amount that gives a pH of 6.5 was added.

The preparation method of these emulsion compositions is:
Glycosphingolipid or / and phospholipid, polyhydric alcohol and water were predispersed at 85 ° C. (8,000 rpm, 2 minutes), added with oil and emulsified at 85 ° C., 8,000 rpm, 5 minutes (TKAUTO HOMO MIXER M made by Special Machine Industries). (This was treated as a homogenizer.)
This emulsion was processed once at 124 MPa with a high-pressure emulsifier (manufactured by Microfluidizer M-110 E / H Microfluidics Corp.).

  The particles of the above Examples and Comparative Examples were appropriately diluted with purified water, and the particle size was measured with a particle size distribution meter. (SALD-2000 manufactured by Shimadzu Corporation)

The results in Table 1 show that the polyhydric alcohol as in Example 1, a polyhydric alcohol having two hydroxyl groups in the molecule, a polyhydric alcohol having three or more hydroxyl groups in the molecule, and a sugar. When blended, the particle size is very large even if the emulsification method is different as compared with one having one polyhydric alcohol as in Comparative Examples 1 to 3, and two polyhydric alcohols as in Comparative Examples 4 to 7. Is small. (See FIGS. 3 to 16)
In Comparative Example 7, the homogenizer-treated product and the high-pressure emulsifier were separated from the once-treated product at 124 MPa, so the particle distribution was not measured.

  The results shown in Table 2 show that the balance between the polyhydric alcohol having two hydroxyl groups in the molecule and the polyhydric alcohol having three or more hydroxyl groups in the molecule and the sugar is within the range of Examples 2-7. It was found that the objective of making the target particle diameter fine was achieved. (See FIGS. 17 to 28)

Moreover, although the kind was changed about the saccharide | sugar which is one component of this invention, the object of this invention can also be achieved even if maltitol and sorbitol are used for the sugar mixture as in Examples 8 and 9 in Table 3. all right. (See FIGS. 29 to 32)
It was also found that good results could be obtained by replacing glycerin with diglycerin, 1.3 butylene glycol with propylene glycol, and the sugar mixture with sorbitol. (See Examples 10 and 11, FIGS. 33 to 36)
However, when experimenting with polyhydric alcohols other than sugar instead of sugar (Comparative Examples 8 to 10), good results were not obtained. (See FIGS. 37 to 42)

Table 4 will be described below.
I also experimented with glycosphingolipids and phospholipids. (Examples 12 to 14)
Glycosphingolipids derived from horses as well as those derived from microorganisms could be carried out without problems. When the phospholipid is treated with a homogenizer, the distribution of the particles becomes wide. In this case, the high-pressure emulsification treatment is consistent with the gist of the present invention. (See FIGS. 43 to 48)
In addition, other oils were also tested for the oil content (Examples 15 to 16). The results of the present invention were achieved without any problem. (See FIGS. 49 to 52)

Experiments were conducted in Table 5 with respect to the amount of oil. (Examples 17 to 18) (See FIGS. 53 to 56)
When the oil content was 45% as in Comparative Example 11, the processed product was separated once at 124 MPa with a high-pressure emulsifier. (Particle distribution was not measured)

Table 6 varied the amount of glycosphingolipid. (See FIGS. 57 to 64)
Within this range, the effect of the present invention was exhibited without any problem.

  Examples 23 to 26 in Table 7 are applications to dosage forms, Examples 1 to 22 are gels, and can be used as massage gels as they are, but lotions like Example 23, Example 24 It is possible to apply to a gel like this, a cream like Example 25, a whitening cream like Example 26, etc. In this case, stirring was performed with an anchor blade at 100 rpm for 10 minutes (emulsification tester ET-3A type, manufactured by Nikko Chemicals Co., Ltd.). In addition, Example 1 used what was processed once by 124 MPa with the high-pressure emulsifier. (Microfluidizer M-110 E / H manufactured by Microfluidics Corp.)

  Summarizing the above results, the emulsified state changes depending on the type and blending amount of oil, glycosphingolipid and phospholipid, but it is 1 more than polyhydric alcohol with two hydroxyl groups in the molecule, glycerin, diglycerin and polyglycerin. By blending polyhydric alcohols with 3 or more hydroxyl groups in the molecule selected from more than one species and three types of sugars, the emulsified state is significantly greater than when one or two polyhydric alcohols are blended. I found it to improve.

In the ternary phase diagram (homogenizer-treated product) for the three components of the oil component, including the amount of glycosphingolipid and phospholipid, polyhydric alcohol, etc., ○ is the average particle size is less than 1 micron, □ is the particle size The average is 1 micron or more, ▪ indicates that secondary particles are formed or peaks are broad, and x indicates that separation or preparation is impossible. In addition, a gray part is a part with the effect of this invention. In the three-component phase diagram (the product processed once at 124 MPa with a high-pressure emulsifier) regarding the three components of oil component, including the amount of glycosphingolipid and phospholipid, polyhydric alcohol, etc., the average particle size is less than 1 micron □ indicates that the average particle size is 1 micron or more, □ indicates that secondary particles are formed or the peak is broad, and × indicates that separation or preparation is not possible. In addition, a gray part is a part with the effect of this invention. Particle distribution of homogenizer treated product of Example 1 Particle distribution of the product processed once at 124 MPa in the high-pressure emulsifier of Example 1 Particle distribution of the homogenizer treated product of Comparative Example 1 Particle distribution of product processed once at 124 MPa with high pressure emulsifier of Comparative Example 1 Particle distribution of the homogenizer treated product of Comparative Example 2 Particle distribution of the product processed once at 124 MPa in the high pressure emulsifier of Comparative Example 2 Particle distribution of the homogenizer treated product of Comparative Example 3 Particle distribution of product processed once at 124 MPa with high pressure emulsifier of Comparative Example 3 Particle distribution of the homogenizer treated product of Comparative Example 4 Particle distribution of product processed once at 124 MPa with high pressure emulsifier of Comparative Example 4 Particle distribution of the homogenizer treated product of Comparative Example 5 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Comparative Example 5 Particle distribution of the homogenizer treated product of Comparative Example 6 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Comparative Example 6 Particle distribution of homogenizer treated product of Example 2 Particle distribution of processed product once at 124 MPa with the high-pressure emulsifier of Example 2 Particle distribution of homogenizer treated product of Example 3 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 3 Particle distribution of homogenizer treated product of Example 4 Particle distribution of processed product once at 124 MPa in high pressure emulsifier of Example 4 Particle distribution of homogenizer treated product of Example 5 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Example 5 Particle distribution of homogenizer treated product of Example 6 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Example 6 Particle distribution of homogenizer treated product of Example 7 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 7 Particle distribution of homogenizer treated product of Example 8 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 8 Particle distribution of homogenizer treated product of Example 9 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 9 Particle distribution of homogenizer treated product of Example 10 Particle distribution of processed product once at 124 MPa with the high-pressure emulsifier of Example 10 Particle distribution of homogenizer treated product of Example 11 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 11 Comparative Example 8 Particle distribution of homogenizer treated product Particle distribution of product processed once at 124 MPa with high pressure emulsifier of Comparative Example 8 Particle distribution of the homogenizer treated product of Comparative Example 9 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Comparative Example 9 Particle distribution of the homogenizer treated product of Comparative Example 10 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Comparative Example 10 Particle distribution of homogenizer treated product of Example 12 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 12 Particle distribution of homogenizer treated product of Example 13 Particle distribution of processed product once at 124 MPa with the high-pressure emulsifier of Example 13 Particle distribution of homogenizer treated product of Example 14 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Example 14 Particle distribution of homogenizer treated product of Example 15 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Example 15 Particle distribution of homogenizer treated product of Example 16 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 16 Particle distribution of homogenizer treated product of Example 17 Particle distribution of product processed once at 124 MPa in high pressure emulsifier of Example 17 Particle distribution of homogenizer treated product of Example 18 Particle distribution of product processed once at 124 MPa with the high-pressure emulsifier of Example 18 Particle distribution of homogenizer treated product of Example 19 Particle distribution of the product processed once at 124 MPa in the high-pressure emulsifier of Example 19 Particle distribution of homogenizer treated product of Example 20 Particle distribution of processed product once at 124 MPa with the high-pressure emulsifier of Example 20 Particle distribution of homogenizer treated product of Example 21 Particle distribution of product processed once at 124 MPa in the high-pressure emulsifier of Example 21 Particle distribution of homogenizer treated product of Example 22 Particle distribution of product processed once at 124 MPa in the high-pressure emulsifier of Example 22

Claims (6)

  One or more of glycosphingolipids and phospholipids, one or more polyhydric alcohols having two hydroxyl groups in the molecule, and three hydroxyl groups in the molecule selected from one or more of glycerin, diglycerin and polyglycerin An emulsified composition comprising the above-described polyhydric alcohol, one or more sugars, and an oil.   The emulsified composition according to claim 1, wherein the sugar is one or more of sorbitol, maltitol, glycosyl trehalose, and a mixture of hydrolyzed starch degradation products.   The emulsion composition according to claim 1 or 2, wherein the polyhydric alcohol having two hydroxyl groups in the molecule is at least one of 1,3 butylene glycol and propylene glycol.     One or more types of glycosphingolipids and phospholipids, one or more types of polyhydric alcohols having two hydroxyl groups in the molecule, and many having three or more hydroxyl groups in the molecule selected from one or more types selected from glycerin and diglycerin An emulsion composition comprising a monohydric alcohol, one or more sugars, and an oil.   An emulsified composition emulsified at 50 MPa or more when emulsifying the emulsified composition according to claim 1.   An emulsified composition obtained by emulsifying a water phase in the emulsified composition according to claim 1.