JPH09309813A - Preparation for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject preparation formulated with a specific ester which is useful for incorporating the preparation with e.g. α-tocopherol, a kind of vitamin E, having high antioxidant ability but being oily and hard to homogeneously formulate in e.g. an aqueous solution, in high stability and safety. SOLUTION: This preparation for external use for skin contains 0.01-10wt.% of α-tocopherol phosphoric ester and/or its sodium salt and/or its disodium salt, but contains no nonionic surfactant. This preparation is obtained by homogeneously dispersing and dissolving α-tocopherol phosphoric ester and the other ingredients together by making use of the solubilizing and emulsifying ability of the α-tocopherol phosphoric ester, etc., followed by agitating the system.

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for skin characterized by containing α-tocopherol phosphate ester. [0002] α-Tocopherol is a kind of vitamin E and has a high antioxidative ability and a pharmacological action such as a blood circulation promoting action, and has been compounded for a long time in medicines, cosmetics, feeds and the like. In addition, its utility value is expected to increase in the future. However, conventionally, α-
Tocopherol and / or α-tocopherol derivatives are oil-soluble and it was difficult to uniformly mix them in an aqueous solution or emulsion. In addition, when prepared as a solubilized state or an emulsion in pharmaceuticals, cosmetics, etc., it is generally possible to disperse evenly by using a nonionic surfactant together, but some nonionic surfactants are irritating. Some of them are highly prone to cause environmental pollution, and are considered unfavorable in terms of safety. On the other hand, the α-tocopherol phosphate and / or its salts have a certain degree of water solubility, but in order to disperse them uniformly, as disclosed in JP-A-59-44375, a nonionic surfactant is used. .Alpha.-tocopherol and / or .alpha.-
It has the same problem as the tocopherol derivative. An object of the present invention is to solve such problems and provide a composition having high stability and safety. Means for Solving the Problems As a result of studying means for solving these problems, the present inventors have found that α-
The inventors have found that tocopherol phosphate ester and / or its salts have useful solubilizing ability and emulsifying ability, and completed the present invention. That is, the present invention makes it possible to uniformly disperse the α-tocopherol phosphate ester and / or its salts and the oil-soluble component in a solubilized state or an emulsified state by blending the oil-soluble component in the same system. is there. Further, a highly safe preparation can be obtained by preparing a skin external preparation using a highly safe amphoteric surfactant such as lecithin in combination with α-tocopherol phosphate and / or a salt thereof. The α-tocopherol phosphate ester and / or its salt used in the present invention may be any,
Preferably, the monoester or salt is a metal salt such as sodium salt, disodium salt, potassium salt or dipotassium salt and / or
Alternatively, an organic salt such as monoethanolamine or triethanolamine may be used. The blending amount of the α-tocopherol phosphate ester and / or its salt is preferably 0.01 to 20% by weight, more preferably 0.05 to 10% by weight. The oil-soluble component used in the present invention may be anything that can be used as a skin external preparation, including fat-soluble vitamins such as α-tocopherol and / or α-tocopherol derivative, avocado oil, castor oil, beef tallow, mink. Fats and oils such as oil, waxes such as lanolin, beeswax, jojoba oil, hydrocarbons such as liquid paraffin, squalane, vaseline and paraffin, fatty acids such as myristic acid, stearic acid, isostearic acid and linoleic acid, ethanol,
Alcohols such as cetanol, stearyl alcohol and cholesterol, polyhydric alcohols such as propylene glycol, butylene glycol, glycerin and polyethylene glycol, diethylhexanoic acid triglyceride, isononyl isononanoate, neopentyl glycol dicaprate, octyldodecyl myristate, etc. Examples thereof include esters, dimethylpolysiloxane, methylphenylpolysiloxane, and silicone oil such as volatile cyclic silicone. The compounding amount of the oil-soluble component can be applied in a wide range of 0.01 to 99% by weight. The amphoteric surfactant used in the present invention may be any, but is preferably a phosphate ester type, a carboxylic acid type or the like, and more preferably a hydrogenated phospholipid. The amount of amphoteric surfactant is 0.1 to 3
0% by weight is preferred, more preferably 0.5-5.0% by weight
It is. Further, the external preparation for skin of the present invention may contain components generally used in the external preparation for skin, as long as the effects of the present invention are not impaired. The present invention will be described in detail with reference to examples, but the present invention is not limited to the examples. The compounding amount in the examples is% by weight. The safety test was conducted by the closed patch method using experimental animals. (Below margin) (Production Method of Comparative Example 1 and Example 1) 1 to 6 are uniformly dispersed and dissolved, and added to 7 with stirring to obtain the desired lotion 1
Get. (Results) Lotion 1 obtained in Example 1 had excellent transparency, low irritation, and good stability over time. On the other hand, in Comparative Example 1, it was not possible to uniformly dissolve or disperse, and it was not possible to obtain a lotion having excellent transparency. (Below margin) (Manufacturing method of Comparative Example 2 and Example 2) 1 to 5 are uniformly dispersed and dissolved, and added to 6 while stirring to obtain the intended lotion 2
Get. (Results) Lotion 2 obtained in Example 2 had excellent transparency, low irritation and good stability over time. On the other hand, in Comparative Example 2, it was not possible to uniformly dissolve or disperse the oil particles, and it was confirmed that oil droplets floated, and it was not possible to obtain a lotion having excellent transparency. (Below margin) (Manufacturing method of Comparative Example 3 and Example 3) 1 to 6 are uniformly dispersed and dissolved, and added to 7 with stirring to obtain the desired lotion 3.
Get. (Results) Lotion 3 obtained in Example 3 had excellent transparency, low irritation and good stability over time. On the other hand, in Comparative Example 3, it was not possible to uniformly dissolve or disperse, and it was not possible to obtain a lotion having excellent transparency. (Below margin) (Manufacturing method of Comparative Example 4 and Example 4) 1 to 5 are uniformly dispersed and dissolved, and added to 6 with stirring to obtain the intended lotion 4
Get. (Results) The non-ethanol type lotion 4 obtained in Comparative Example 4 was excellent in transparency and showed good stability over time. In addition, the non-ethanol type lotion 4 obtained in Example 3 also showed excellent transparency and good stability over time, even though it did not contain a nonionic surfactant. And showed low irritation. (Below margin) (Production method of Comparative Example 5 and Example 5) 1 to 3 are uniformly dispersed and dissolved, and 4 is added with stirring to obtain the intended gel external preparation 1. (Results) The gel-type external preparation 1 obtained in Example 5 had a transparent gel-like appearance, and showed low irritation and good stability over time. On the other hand, in Comparative Example 5, gel formation was not performed. (Below margin) (Production Method of Comparative Example 6 and Example 6) 1 to 3 are uniformly dispersed and dissolved, and 4 is added with stirring to obtain the desired gel external preparation 2. (Results) The gel-type external preparation 2 obtained in Example 6 had a transparent gel-like appearance, and exhibited low irritation and good stability over time. On the other hand, in Comparative Example 6, gel formation was not performed. (Below margin) (Manufacturing method of Comparative Example 7 and Example 7) 1 to 4 are uniformly dispersed and dissolved, and 5 is added with stirring to obtain the intended gel external preparation 3. (Results) The gel external preparation 3 obtained in Comparative Example 7 had a transparent gel appearance and exhibited good stability over time. On the other hand, the gel external preparation obtained in Example 7 also had a transparent gel-like appearance even though it did not contain a nonionic surfactant, and showed good stability over time. It showed better safety than Example 7. (Below margin) (Production method of Comparative Example 8 and Example 8) 1 to 4 are uniformly dispersed and dissolved, and 5 is added with stirring to obtain a target emulsion 1. (Results) Emulsion 1 obtained in Example 8 had a refreshing feel on use, showed low irritation and good stability over time. On the other hand, in Comparative Example 8, an emulsion was not formed and an emulsion could not be obtained. (Below margin) (Production method of Comparative Example 9 and Example 9) 1 to 4 are uniformly dispersed and dissolved, and 5 is added with stirring to obtain a target emulsion 2. (Results) Emulsion 2 obtained in Example 9 had a refreshing feeling to use, showed low irritation and good stability over time. On the other hand, in Comparative Example 9, although an emulsion was obtained, phase separation was observed after several days, and good stability over time could not be obtained. (Below margin) (Production Method of Comparative Example 10 and Example 10) 1 to 4 are uniformly dispersed and dissolved, and 5 is added with stirring to obtain a target emulsion 3. (Results) Emulsion 3 obtained in Example 10 had a refreshing feeling to use, showed low irritation and good stability over time. On the other hand, in Comparative Example 10, although an emulsion was obtained, phase separation was observed after several days, and good stability over time could not be obtained. (Below margin) (Production Method of Comparative Example 11 and Example 11) 1 to 4 are uniformly dispersed and dissolved, and 5 is added with stirring to obtain the objective Emulsion 4. (Results) Emulsion 4 obtained in Example 11 had a refreshing feel on use, showed low irritation and good stability over time. On the other hand, in Comparative Example 11, although an emulsion was obtained, phase separation was observed after several days, and good stability over time could not be obtained. (Below margin) (Production method of Comparative Example 12 and Example 12) 1 to 5 are uniformly dispersed and dissolved, and 6 to 10 that are uniformly dispersed and dissolved while stirring are added to obtain a target cream. (Results) The cream obtained in Example 12 had a moisturizing feeling to use, showed low irritation and good stability over time. On the other hand, in Comparative Example 12, no emulsion was formed and a cream could not be obtained.

   ────────────────────────────────────────────────── ─── Continuation of front page    (72) Inventor Satoru Nakata             2-7 Torimicho, Nishi-ku, Nagoya-shi             Nard Cosmetics Co., Ltd.

Claims (1)

Claims: 1. An external preparation for skin, which comprises an α-tocopherol phosphate ester and / or a salt thereof and does not include a nonionic surfactant. 2. An external preparation for skin according to claim 1, which further comprises an amphoteric surfactant. 3. The external preparation for skin according to claim 1, wherein the blending amount of the α-tocopherol phosphate ester and / or its salt is 0.01 to 10%. 4. The external preparation for skin according to claim 1, wherein the α-tocopherol phosphate ester and / or its salt is a sodium salt and / or a disodium salt.