JP2011088849A - Lotion for skin external application - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a lotion for skin external application which includes chlorpheniramine maleate, has good transparent stability, and also has good usability. <P>SOLUTION: The lotion for skin external application includes (a) 0.01-1 mass% of chlorpheniramine maleate, (b) 0.05-0.5 mass% of a glycyrrhizinate selected from among dipotassium glycyrrhizinate and monoammonium glycyrrhizinate, (c) 0.01-2 mass% of a polyoxyethylene alkyl ether selected from among POE(20) cetyl ether, POE(30) cetyl ether, POE(20) stearyl ether, POE(20) oleyl ether, POE(30) behenyl ether, and POE(20)-POP(4) cetyl ether, and (d) 1-30 mass% of a moisturizer selected from among concentrated glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol, and sodium hyaluronate. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention relates to an external skin lotion, and more particularly to an external skin lotion containing chlorpheniramine maleate.

Chlorpheniramine salts such as chlorpheniramine maleate and glycyrrhizinate salts such as dipotassium glycyrrhizinate are anti-histamine and anti-inflammatory properties, respectively, and are used externally for eczema and dermatitis. In addition to compositions, it is widely used in ophthalmic compositions such as eye drops and eye wash, nasal drops, pharmaceuticals, quasi drugs and the like.
However, when preparing an external skin lotion containing chlorpheniramine maleate and glycyrrhizinate at the same time, there is a problem of quality deterioration due to white turbidity over time, and this white turbidity was particularly noticeable at low temperatures. .

Here, as a technique which mix | blended chlorpheniramine maleate and glycyrrhizinate, there exist the following.
That is, in Patent Document 1, 0.0003 to 0.006% chlorpheniramine salts and / or 0.0025 to 0.05% glycyrrhizinate salts, polyoxyethylene (POE) -polyoxypropylene (POP) blocks An aqueous liquid composition containing a copolymer or a POE sorbitan fatty acid ester and a chelating agent and having an active ingredient stably maintained is known. However, this aqueous liquid composition has a drawback that the concentration of the active ingredient is low.
In addition, Patent Document 2 discloses an aerosol preparation with enhanced medicinal effects in which an antihistamine component, a glycyrrhizinate salt, an essential oil component, and a propellant are blended. However, this aerosol formulation requires essential oil components and a propellant.
Patent Document 3 discloses a stable eye drop containing chondroitin sulfates, glycyrrhizinates and edetates. However, chondroitin sulfates are essential for this eye drop.

  As a commercially available lotion agent, there is a tact lotion manufactured by Sato Pharmaceutical. This tact lotion contains 1% diphenhydramine hydrochloride, 0.5% dipotassium glycyrrhizinate, 1% tesitdecitine (POE lauryl ether), 0.2% allantoin, and 0.1% isopropylmethylphenol as active ingredients. However, this lotion does not have the problem of white turbidity over time because the antihistamine is not chlorpheniramine maleate, and cannot be solved by the same method. In addition, this lotion preparation was not very useful.

JP 2004-149526 A JP 2003-81812 A JP 2005-330271 A

  In view of the circumstances as described above, the present invention provides a skin external lotion having good transparency stability and good usability even when chlorpheniramine maleate and glycyrrhizinate are blended at a relatively high concentration as active ingredients. The purpose is to provide an agent.

  As a result of intensive research to achieve the above-mentioned problems, the present inventors have blended a specific surfactant and further a moisturizing agent, so that the usability is good, the stability is good, and there is no white turbidity. The inventors have found that it can be used as a skin external lotion, and have completed the present invention.

The present invention is a skin external lotion characterized by containing the following (a) to (d).
(A) 0.01-1% by mass of chlorpheniramine maleate
(B) 0.05 to 0.5% by mass of glycyrrhizinate selected from dipotassium glycyrrhizinate and monoammonium glycyrrhizinate
(C) selected from polyoxyethylene alkyl ether (wherein the alkyl group has 14 to 22 carbon atoms) and polyoxyethylene polyoxypropylene alkyl ether (wherein the alkyl group has 14 to 22 carbon atoms) 0.01 to 2 mass% of one kind or two or more kinds
(D) 1 to 30% by mass of a humectant selected from concentrated glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol and sodium hyaluronate

  The skin external lotion according to the present invention has good stability and good usability while compounding chlorpheniramine maleate and glycyrrhizinate as active ingredients.

Embodiments of the present invention will be described below.
(A) Chlorpheniramine maleate used for the external skin lotion of the present invention has an antihistamine action, and its blending amount is 0.01 to 1% by mass, preferably 0.1 to 0.1% by mass. 1% by mass.

  The (b) glycyrrhizinate which is an anti-inflammatory agent used in the external skin lotion of the present invention is dipotassium glycyrrhizinate or monoammonium glycyrrhizinate.

  The amount of glycyrrhizinate is 0.05 to 0.5% by mass, preferably 0.1 to 0.5% by mass.

Component (c) used in the present invention includes polyoxyethylene (POE) alkyl ether (wherein the alkyl group has 14 to 22 carbon atoms) and polyoxyethylene polyoxypropylene (POE · POP) alkyl ether (provided that And the alkyl group has 14 to 22 carbon atoms).
Component (c) is preferably one or more selected from POE cetyl ether, POE stearyl ether, POE oleyl ether, POE behenyl ether, and POE · POP cetyl ether. These surfactants may be blended singly or in combination of two or more. The total number of added moles of POE and POP is preferably 20-30.
Particularly preferred as component (c) are POE (20) cetyl ether, POE (30) cetyl ether, POE (20) stearyl ether, POE (20) oleyl ether, POE (30) behenyl ether, POE (20). One or more selected from POP (4) cetyl ether.
Among the surfactants, by using the above surfactants, while blending chlorpheniramine maleate and glycyrrhizinate, it not only has good transparency stability, but also has a penetrating feeling and is not sticky. In addition, it is possible to make an excellent skin lotion.

  The amount of the component (c) in the external skin lotion of the present invention is 0.01 to 2% by mass, preferably 0.1 to 0.8% by mass, based on the total amount of the external skin lotion. . If the amount of the component (c) is too small, the stability is poor, and if the amount of the component (c) is too large, foaming occurs and the safety is not good.

  The humectant of component (d) used in the present invention is one or more selected from concentrated glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol, and sodium hyaluronate.

  The blending amount of the component (d) in the external skin lotion of the present invention is 1 to 30% by mass, preferably 10 to 20% by mass, based on the total amount of the external skin lotion. If the blending amount of the component (d) is too small, there is no moistness and the usability deteriorates. If the blending amount of the component (d) is too large, the component becomes sticky.

  The external preparation for skin lotion of the present invention is prepared by appropriately blending other optional components usually used in external preparations for skin, such as cosmetics and pharmaceuticals, as necessary, in addition to the above-described essential components. I can do it. For example, the skin external lotion of the present invention can be prepared by blending the above essential ingredients and one or more of the following ingredients.

  Other active ingredients used in the external skin lotion of the present invention are not particularly limited on the condition that they are pharmacologically or physiologically acceptable, and for example, allantoin and isopropylmethylphenol can be used. .

  As the preservative, for example, parabens, sorbic acid or a salt thereof, salicylic acid or a salt thereof, or phenoxyethanol can be used. Of these, methyl paraoxybenzoate is preferred.

  As the chelating agent, for example, ethylenediaminetetraacetic acid (hereinafter referred to as “edetic acid”) or a salt thereof, citric acid or a salt thereof can be used. Of these, edetic acid or a salt thereof is preferable.

  Others include lower alcohols such as ethanol and isopropanol; pH adjusters such as citric acid or salts thereof, lactic acid or salts thereof; antioxidants such as butylhydroxytoluene and tocopherol; sugar alcohols such as sorbitol; hydroxypropylcellulose, carboxy Water-soluble polymers such as vinyl polymer and xanthan gum; vitamin A and its derivatives, vitamin B6 hydrochloride, vitamin B2 and its derivatives, vitamin B such as vitamin B12, vitamins such as ascorbic acid and ascorbic acid phosphate (salt) Vitamin E such as C, α-tocopherol, δ-tocopherol, tocopherol acetate, vitamin D, vitamin H, pantothenic acid, pantethine, etc .; nicotinamide, benzyl nicotinate, γ-oryzanol, glycine Luretic acid and its derivatives, pantothenyl ethyl ether, ethinyl estradiol, tranexamic acid, arbutin, placenta extract, l-menthol and other drugs; pigments, fragrances; sorbitan monostearate, sorbitan sesquioleate, polyethylene glycol monooleate, poly Nonionic surfactants such as oxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, sugar ester, cations such as benzalkonium chloride and laurylamine oxide Surfactants, anionic surfactants such as sodium lauryl sulfate and sodium cetyl sulfate, and amphoteric surfactants.

Hereinafter, the present invention will be described in more detail with reference to examples. The present invention is not limited to these examples. Unless otherwise specified, the blending amount indicates mass%.
Prior to the examples, the evaluation method used in the present invention will be described.

(1) Stability evaluation method Immediately after production, the transparency of the appearance when the sample was allowed to stand at 50 ° C. for 1 month and at 0 ° C. for 1 month was visually evaluated and evaluated according to the following criteria.

(Evaluation criteria)
○: Transparent.
X: It is cloudy.

(2) Evaluation method of feeling of use (2-1) Penetration feeling Penetration feeling at the time of application was evaluated based on the following evaluation point criteria by a questionnaire survey of five panels. Subsequently, the evaluation points given by each person were averaged and evaluated based on the following evaluation criteria.

(Evaluation criteria)
5 points: Feels penetrating.
4 points: Feels slightly penetrating.
3 points: Neither can be said.
2 points: Slightly permeation is not felt.
1 point: There is no sense of penetration.

(Evaluation criteria)
○: The average score is 3.5 or more.
(Triangle | delta): An average point is 2.5 or more and less than 3.5.
X: The average score is less than 2.5.

(2-2) Moistness Based on a questionnaire survey of five panelists, the moistness at the time of application was evaluated based on the following evaluation criteria. Subsequently, the evaluation points given by each person were averaged and evaluated based on the following evaluation criteria.

(Evaluation criteria)
5 points: Moist.
4 points: Slightly moist.
3 points: Neither can be said.
2 points: Not moist.
1 point: Not moist.

(Evaluation criteria)
○: The average score is 3.5 or more.
(Triangle | delta): An average point is 2.5 or more and less than 3.5.
X: The average score is less than 2.5.

(2-3) Stickiness Based on a questionnaire survey of five panelists, the stickiness at the time of application was evaluated based on the following evaluation criteria. Subsequently, the evaluation points given by each person were averaged and evaluated based on the following evaluation criteria.

(Evaluation criteria)
5 points: Not sticky.
4 points: Not sticky.
3 points: Neither can be said.
2 points: Slightly sticky.
1 point: Sticky.

(Evaluation criteria)
○: The average score is 3.5 or more.
(Triangle | delta): An average point is 2.5 or more and less than 3.5.
X: The average score is less than 2.5.

Examples 1-8, Comparative Examples 1-3
A lotion preparation for external use comprising the respective formulation components shown in Tables 1 and 2 below was prepared by the following method.
About the obtained skin external lotion, stability and usability were evaluated according to the above criteria. The results are also shown in Tables 1 and 2.

(1) Manufacturing method After melt | dissolving surfactant component, it melt | dissolves in a part of moisturizer, and is set as surfactant part. Next, a surfactant part is added to the aqueous phase part in which the aqueous component is dissolved. Finally, the active ingredient is added and dissolved by stirring to obtain a lotion.

  Below, the formulation example of the skin external lotion of this invention is given. Needless to say, the present invention is not limited by these formulation examples and is specified by the scope of claims.

Formulation Example 1
(1) Chlorpheniramine maleate 1.0% by mass
(2) Allantoin 0.2
(3) Dipotassium glycyrrhizinate 0.1
(4) Concentrated glycerin 5.0
(5) 1,3-butylene glycol 5.0
(6) Macrogoal 1500 1.0
(7) Sodium hyaluronate 0.01
(8) Polyoxyethylene (20) cetyl ether 0.5
(9) Sodium edetate 0.1
(10) Methyl paraoxybenzoate 0.1
(11) Purified water balance

Claims (2)

A skin external lotion comprising the following (a) to (d):
(A) 0.01-1% by mass of chlorpheniramine maleate
(B) 0.05 to 0.5% by mass of glycyrrhizinate selected from dipotassium glycyrrhizinate and monoammonium glycyrrhizinate
(C) selected from polyoxyethylene alkyl ether (wherein the alkyl group has 14 to 22 carbon atoms) and polyoxyethylene polyoxypropylene alkyl ether (wherein the alkyl group has 14 to 22 carbon atoms) 0.01 to 2 mass% of one kind or two or more kinds
(D) 1 to 30% by mass of a humectant selected from concentrated glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol and sodium hyaluronate   The (c) is selected from polyoxyethylene cetyl ether, polyoxyethylene stearyl ether, polyoxyethylene oleyl ether, polyoxyethylene behenyl ether and polyoxyethylene polyoxypropylene cetyl ether. Skin lotion.