JPS61260015A - External preparation - Google Patents

Abstract

PURPOSE:An external preparation useful for remedying an abnormal disease of skin keratinization, containing urea, a phospholipid, water and a fat and oil component. CONSTITUTION:2-30wt%, preferably 5-20wt% urea is blended with 0.2-30wt%, preferably 1-20wt% phospholipid (e.g., extracted from soybean, corn or colza), 5-80wt% water (purified water) (preferably 30-80wt% in the case of O/W type or 5-15wt% in the case of W/O type), 5-60wt% fat and oil component (e.g., hydrocarbon such as liquid paraffin, solid paraffin, etc., aliphatic higher alcohol such as cetyl alcohol, etc., ester such as bees wax, etc.) in the case of O/W type or 70-92wt% fat and oil component in the case of W/O type, and, if necessary, a gelatinizing agent, etc., or antibiotic, etc., to give an external preparation. EFFECT:Having much more increased remedying effect on an abnormal disease of skin keratinization than an external preparation using a synthetic surface active agent as a dispersant.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Application Field) The present invention relates to an external preparation, and more particularly to an external preparation used for the treatment of skin dyskeratosis.

(Prior technology) Fish scale, senile xeroderma, atopic skin, progressive digital palmar endotheliosis (dry type of housewife's eczema) 1. Forefoot cleft dermatitis, palmar and hoof keratosis 9. Lichen pilaris External preparations containing urea are effective for the treatment of skin dyskeratosis such as. Since urea is water-soluble, it has conventionally been used in emulsion ointments, creams, and lotions in which an aqueous urea solution is dispersed in oil and fat components using a synthetic surfactant.

(Problems to be Solved by the Invention) However, the synthetic surfactants contained in these preparations promote water evaporation from the skin, significantly reducing the therapeutic effect of urea-containing external preparations.

(Means for Solving the Problems) As a result of extensive research in order to eliminate the drawbacks of conventional urea-containing external preparations, the present inventors have found that by using phospholipids as a dispersant, they can treat skin dyskeratosis. The present invention has been completed based on the discovery that the therapeutic effect of urea-containing external preparations on urea is significantly increased.

The object of the present invention is an external preparation consisting of urea, phospholipids, water, and fat and oil components.

In the present invention, urea is contained in an amount of 2 to 30% by weight of the total amount.

Preferably, it is blended in an amount of 5 to 20% by weight. If the amount is less than this range, no therapeutic effect can be expected, and if the amount is more than this range, the irritation to the skin will be too strong to be practical.

The phospholipid is one extracted from egg yolk, soybean, corn, or rapeseed, preferably commercially available soybean phospholipid (phos-7 atidylcholine content of about 25 to 35% by weight) or egg yolk phospholipid (phosphatidylcholine content of about 25 to 60% by weight). α2 of total amount
~50% by weight, preferably 1~20% by weight.

Purified water is used, and the amount is 5 to 80% by weight of the total amount, preferably 30 to 80% by weight for 0/W type formulations.

Si0. In this type of preparation, 5 to 15% by weight is added.

Oil and fat components are liquid to solid hydrocarbons (e.g. liquid paraffin, white petrolatum, solid paraffin).

microcrystalline wax, squalane, squalene, etc.), aliphatic higher alcohols (e.g., cetyl alcohol, hexadecyl alcohol, stearyl alcohol, oleyl alcohol), esters of higher fatty acids and higher alcohols (e.g., beeswax, spermaceti),
Esters of higher fatty acids and lower alcohols (e.g., inglovir myristate, isopropyl palmitate, etc.) and vegetable oils (e.g., olive oil, almond oil).

peanut oil, etc.), modified vegetable oils (e.g., hydrogenated and mustard oil, medium-chain fatty acid glycerides, etc.), esters of fatty acids and glycerin (e.g., glycerol, esters of fatty acids and propylene glycol (e.g., palmitic acid, stearic acid, etc.), ) in Hetaib formulations, 5 to 60% by weight, preferably 10 to 30% by weight, and in '10 type formulations, 70 to 92% by weight.

Preferably, it is blended in an amount of 80 to 91% by weight.

In addition, if necessary, a gelling agent (increases storage stability of the preparation; 0.01 to 2% by weight of the total amount, preferably 0.02 to 2% by weight)
For example, carboxymethylcellulose, carboxyvinyl polymer (Hipis Wako: trade name, manufactured by Wako Pure Chemical Industries, Ltd.).

polyvinyl alcohol, etc.], wetting agent (increases the wetting effect of the preparation; α1-20% by weight of the total amount, preferably 0.5-20% by weight)
10% by weight; for example, propylene glycol,
glycerin, sorbitol, etc.), chelating agents (increases the storage stability of the formulation; e.g., disodium ethylenediaminetetraacetate, etc.), preservatives (e.g., methyl, ethyl, propyl, butyl, dehydroacetic acid and its like). salts, etc.), - conditioning agents (e.g.
Citric acid, lactic acid, tartaric acid and its salts, diisopropanolamine, etc.; the amount to be adjusted is determined based on the stability of the formulation, and it is generally preferred that the formulation be kept weakly acidic to weakly alkaline. ), antioxidants (for example, butylated hydroxytoluene, butylated hydroxyanisole, etc.) can be added.

Also, if necessary, antibiotics (e.g., gentamicin sulfate, 7-radiomycin sulfate, etc.), antihistamines (e.g., diphenhydramine).

bactericidal agents (e.g. dequalinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, sulfisomidine), anti-inflammatory agents (e.g. glycyrrhetinic acid, indomethacin, dexamethacin acetate, Betamethacin grass acid, hydrocortisone propionate butyrate, etc.)
, medicinal ingredients such as vitamins (e.g., vitamin A, vitamin D, vitamin E, etc.) and fragrances (e.g.,
Lavender, neroli, strawberry, heliotrope.

rose, amyl acetate, etc.) may also be blended in appropriate combinations.

Furthermore, if necessary, nonionic surfactants that are less irritating to the skin (for example, fatty acid monoglycerides, sorbitan fatty acid esters, polyoxyethylene higher fatty acid esters, etc.) may be added to increase the storage stability of the formulation. It can be added in a small amount to the extent that the effect of urea is not reduced.

The external preparation of the present invention can be produced, for example, by the method described below.

That is, phospholipids are dissolved in heated oil and fat components, and a heated urea aqueous solution is added thereto and cooled while stirring, or all components are mixed together, heated and stirred, and then cooled.

Although there are no particular precautions to be taken during production, an external preparation with high storage stability can be obtained by making the emulsion particles finer using a homomixer or the like during stirring during heating.

(Function) By using a phospholipid as a dispersant, the external preparation of the present invention has a significantly increased therapeutic effect on skin dyskeratosis compared to a urea-containing external preparation using a synthetic surfactant as a dispersant.

Hereinafter, the effects of the external preparation of the present invention will be illustrated by giving test examples.

Test Examples Samples 1 to 3 having the formulations shown in Table 1 were prepared according to Example 1 described below.

Housewife with progressive digital palmar endotheliopathy showing moderate symptoms (23-3
Three groups of 10 children (5 years old) were prepared, and an appropriate amount of each sample was applied to the affected areas of the housewives in the separate groups every day before washing and going to bed. We investigated the degree of improvement and expressed it in terms of the number of people affected.

The results are shown in Table 2.

Table 1 Table 2 (Effects of the Invention) The external preparation of the present invention has a high therapeutic effect on skin dyskeratosis and can be used as a medicine.

(Example) The present invention will be specifically described below with reference to Examples.

Example 1 Commercially available soybean phospholipid 1002 was mixed with liquid paraffin 300f
Ethyl paraoxybenzoate 22
and butylated hydroxytoluene 12 were added and dissolved to prepare an oil phase liquid.

In addition, urea 1002 was dissolved in purified water 595.5f, and lactic acid 2 and sodium lactate 1f were added to this.

After adding and dissolving ethylenediaminetetraacetic acid disodium Q, 52, add glycerin 100? was added, heated, and dissolved to prepare an aqueous phase liquid.

The aqueous phase liquid heated to approximately the same temperature was added to the oil phase liquid heated to 75°C, and the mixture was mixed at 5000 rpm using a homomixer.
The mixture was stirred for 0 minutes, and then cooled to room temperature while stirring to obtain a cream-like external preparation 1000F.

The crystal was stored at room temperature for one year and its condition was examined, but no change was observed in its condition.

Example 2 10 f of commercially available soybean phospholipid, 10 f of white petrolatum, 100 t of liquid paraffin, 2 of butylated hydroxytoluene, and 42 of methyl paraoxybenzoate were dissolved by heating,
An oil phase liquid was prepared.

In addition, after dissolving urea 100f in purified water 771.89 and adding and dispersing Hipiswako-22,
An aqueous phase liquid was prepared by adding 10.2 t of diisopropanolamide.

The aqueous phase liquid heated to approximately the same temperature was added to the oil phase liquid heated to 70°C, and the mixture was heated at 5000 rp using a homomixer.
The mixture was stirred for 15 minutes at m, and then cooled to room temperature while stirring to obtain a lotion-like external preparation 10002.

The crystal was stored at room temperature for one year and its condition was examined, but no change was observed in its condition.

Example 3 According to Example 1, a cream-like external preparation having the following formulation was prepared.

(Prescription) Urea 10
Part by weight Soy phospholipid
20 Isopropyl myristate
10 Stearyl alcohol
10 Butylated hydroxytoluene
0.5 Disodium ethylenediaminetetraacetate 0.1 Ethyl paraoxybenzoate α2N citric acid
α1〃Purified water
49.1//Total 100 Example 4 According to Example 1, an oil-based ointment-like external preparation with the following formulation was prepared.

(Prescription) Urea 5
Weight part soybean paste/fat
4 Purified water 10 Liquid paraffin 10
〃White petrolatum
7Q, 75 If phthyl hydroxytoluene
α05 〃Ethylenediaminetetraacetic acid disodium Q, 2〃Total
100 Example 5 According to Example 1, an oil-based liquid exfoliant having the following formulation was prepared.

(Formulation) Urea 2 parts by weight Soybean phospholipid 2 Olive oil 30 Liquid paraffin 6α05 Purified water 5
〃

Claims (1)

[Claims] 1) External preparation containing urea, phospholipids, water and oil components.