JPS5869248A - Alcohol gel composition for external application - Google Patents

Abstract

PURPOSE:To provide the titled composition which has no offensive odor, is not irritating to skin and shows a high level satety, prepared by adding a carboxyvinyl polymer and alcohol soluble nylon to lower alcohol. CONSTITUTION:A carboxyvinyl polymer and alcohol-soluble nylon are added to a solvent consisting mainly of lower alcohol. The nylon should pref. be used in an amount at least three times that of the carboxyvinyl polymer and 0.1-20% of the total compsn. When the amount of the nylon is less than the above level, it sometimes leads to insufficient thickning, while when it exceeds 20%, the compsn. shown poor solubility and the gel tends to solidify during storage. The concentration of the lower alcohol in the solvent should pref. be 60-100%.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a topical alcohol glue composition containing xyvinyl f-rimer and alcohol-soluble nylon.
More specifically, the present invention relates to an alcohol glue composition for external use, which is made by neutralizing and thickening a system of carboxyvinyl polymer and a solvent mainly composed of lower alcohol with alcohol-soluble nylon.

Recently, Cal? has been used as a gelling agent for cosmetics and pharmaceuticals. Calgexivinyl, Je 17mer, known under the trade name Pall, is widely used. This calgexivinyl/I
J Mama Yoru Guru is less sticky, is not harmed by bacteria or mold, and contains a small amount of calxyvinyl. It has many advantages such as being able to obtain high viscosity and chicken tropism as a remer, being highly safe, and being applicable to a wide variety of solvents such as fragrant water, alcohol, and polyhydric alcohol.

In this case, K to obtain a carboxyvinyl polymer glue is carried out by dispersing or dissolving the carboxyvinyl polymer in a solvent and then adding an appropriate neutralizing agent to thicken and glue it. It is often used in Bieller.

However, when blending drugs such as fragrances and active ingredients into glue, lower alcohol It is preferable to use a solvent system mainly consisting of alcohol and alcohol.

Conventionally, when forming an alcoholic polymer using carboxyvinyl polymer, organic amine bases such as ammonia, triethanolamine, and triethylamine are used as neutralizing agents. It has been said that adding an excessive amount of 100% or more has been considered to be beneficial in stably improving the thickening and gluing effect.

However, these organic amine bases are highly irritating to the skin, have a strong odor, and are highly reactive with the drugs they are compounded with, often impairing the stability of the drugs, and may cause reactions and decomposition products. This lowers the viscosity of the glue and impairs the stability of the glue itself.

In addition, in general, when a compound having a phenol group is added to a glue containing xyvinyl polymer, the viscosity of the glue decreases significantly over time, so the addition or amount of this type of compound is limited, and furthermore, it is difficult to add an ester compound. Even when they are blended, they exhibit acidity due to decomposition and have the problem of lowering the viscosity of the glue.

The Ministry of the Invention and others improved the above situation and conducted intensive research on a good neutralizing thickener to replace the conventionally used organic amine bases, which are highly irritating to the skin, and found that alcohol-soluble nylon with low grade It has been found that a completely new and good neutralizing thickener for carboxyvinyl polymers in alcohol-based solvent systems. That is, by blending alcohol-soluble nylon with carboxyvinyl polymer into a solvent mainly composed of lower alcohols, this system is neutralized and thickened to form alcohol glue, and this alcohol glue has no off-odor and is gentle on the skin. It is non-irritating and highly safe, and has little reactivity with drugs, etc. Therefore, even if alcohol-soluble nylon is added in excess, it does not impair the stability of strips, etc., and reduces the viscosity of the glue. In addition, phenol groups and ester groups
The present inventors have discovered that it is possible to blend compounds that have the following properties, and that even when these compounds are blended, the viscosity of the glue does not decrease, and the present invention has been completed.

The present invention will be explained in detail below.

The present invention is an alcohol composition for external use, which is characterized by blending xyvinyl polymer and alcohol-soluble nylon in a solvent mainly composed of lower alcohol, and is used as a facial mask, trauma agent, and external anti-inflammatory analgesic agent. agent,
It is used for applications such as skin disease treatments, anti-itch agents, adhesive plasters, etc. that are applied to the skin.

In the present invention, the carboxyvinyl polymer is
Any of those conventionally used as gluing agents can be used, specifically B and F.

Carbopol 934, 940゜941 manufactured by Goodri@h, Hiviswako-103゜104 manufactured by Wako Tsumugi Co., Ltd.
．． 105. Jibanron PW110.11 manufactured by Nippon Tsumugi Pharmaceutical Co., Ltd.
1 etc. may be used. In addition, in the present invention, these cals may be used alone or in combination with 181 of Kishou Narima or 2& or more.

The amount of carboxyvinyl polymer blended is 0 in the entire composition.
．． It is preferable to set it to 03 to 5%. If the blending amount is lower than ODs, the viscosity may be too low to become a glue.
Also, it dissolves when the amount is more than 5%.

The workability of dispersion is not necessarily easy, and the viscosity of the resulting glue is sometimes too high, resulting in poor usability.

As the alcohol-soluble nylon, copolymer type, modified nylon, copolymer-modified nylon, etc. can be used. As a copolymer type nylon, Nyon 6/
66/610. (oy6/66/12, nylon 6/
69/12, nylon 6/612. /12゜Nylon 6/66/69/12, Nylon 6/66/11/1
2. Nylon 6/66/612/12, Nylon 6/
Examples include ternary or higher copolymers such as 66/bis(4-aminocyclohexyl)methane-6, specifically CM-4000 and CM-4001゜CM manufactured by 311/Company.
-8000, Ditiru made by Jepon Co., Ltd.-61゜63, 6
9, BASF Ultraamide-IA, I
C.

5A, 6A, 10, Diazed manufactured by Daicel, etc. may be used. In addition, modified nylon is one in which the hydrogen of the amide group is replaced with an alkoxyal group, etc., and is manufactured by Teikoku Kagaku Sangyo Co., Ltd., such as Trezi yF30. F3'Oc, F30X, etc. can be used, and the copolymerized-modified nylon is a combination of a copolymerized type and a modified type, and the Diabad X series manufactured by Daicel Corporation can be used. . Note that the nylons exemplified above all have melting points in the range of 80 to 160°C.

In the present invention, the above nylon may be used alone or in combination of two or more.
In addition, the amount of alcohol-soluble nylon blended is at least 3 times the amount of carcinyl vinyl/IJmer, and is 0% of the total composition.
．． If the amount of alcohol-soluble nylon blended is preferably less than 3 times the amount of xyvinyl polymer, or less than 0.1 of the total composition, a sufficient thickening effect can be obtained. may not be obtained.

On the other hand, if the amount of alcohol-soluble nylon exceeds 20%, the solubility will be rapid and the glue may solidify during storage. A more preferable blending amount of alcohol-soluble nylon is carboxyvinyl/13mer 5
The amount is 1 to 20% of the total composition.

As mentioned above, the solvent used in the present invention is mainly composed of lower alcohol, but lower alcohol pale filtrate
It is preferably 60 to 100% in the solvent, and the lower alcohol is ethanol.

Isopropyl alcohol, Flobil alcohol, etc. are suitable Kg! can be used. In addition to the above-mentioned lower alcohols, water may be used in the solvent in an amount of 0 to 40% for the m agent, and polyhydric alcohols such as glycerin, nrubitol, ethylene glycol, and propylene glycol, as well as ethyl calpitol and ethyl cellosolve.

Other organic solvents such as chloroform, isoglobil myristate, isopropyl nogrumitate, etc.
0% can be used.

The alcoholic acid composition of the present invention includes materials and bactericidal agents depending on its type or purpose of use.

Local narcotics, antihistamines, anti-inflammatory analgesics, astringents.

Sulfa drugs, vitamin A, antifungal agents, peripheral nerve paralyzing agents,
111 or 21 of physiologically active drugs such as blood circulation promoters, S, renal cortical hormones, insect repellents, herbal medicine extracts, tinctures, herbal medicine powders, etc. [more than 00 to 30% of the entire composition]
Can be mixed to some extent.

In addition, specific examples of the above-mentioned drugs are as follows.

m) Disinfectants: pendelkonium chloride, pesozethonium chloride, cetylpyridinium chloride, domiphene bromide, dequalinium chloride, fradiomycin sulfate, homosulfamine, chlorhexidine, chlorhexidine talconate l) Local narcotics: didecaine hydrochloride, pyridoxine hydrochloride.

Ethyl aminobenzoate, hydrochloric acid! Locaine, dimethisoquine hydrochloride, hydrochloric acid! spideroxin. Lidocaine C) Antihistamines Nidiphenhydramine, Diphenhydramine Hydrochloride, Tripelenamine.

Tongjiryolumin, maleic acid chloride Lupheniramine 8 isocypendi lucremizole, diphenylimine Dazol D) Anti-inflammatory analgesics: salicylic acid, methyl salicylate.

Glycol salicylate, indomethacin, glycyrrhizin, glycyrrhetinic acid, azulene E) Astringent dichloroaluminum diaminoacetate, aluminum phenol sulfonate F) Sulfa drugs rufisoxazole, sulfamethogisazole, sulfanilamide, sulfapyridine, Sulfamethoxypyridazine, sulfamethoxine, sulfadiazine G) Vitamins: Vitamins E, A, D H) Antifungal agents: Pentachlorophenol, salicylic acid,
Trichlorophenol (trichlorophenol), ) IJ bromophenol caproate, lauryl triphenylphosphonium bromide, diantazole hydrochloride, acetyl inophenyl rhodan, thimerosal, tolnaftate, clotrimazole ■) Palpitis nerve paralytics: t- Menthol, camphor.

Thymol, Tessit J) m Row accelerator dinonylic acid panillylamide, nicotinic acid β-butoxyethyl ester.

Nicotinic acid benzyl ester, capsaicin, zinglone, lecithin, chloral hydrate, cantharis tincture K) Adrenal cortex, lumon: prednisolone, dexamethasone, fluoromesolone, triamcinolone acetonide.

Guiclolysin L>Insect 31 Agent II: N,N-diethylamide, bisethylenetetrahydrofurfural.

Butoxide, di-n-propyl incincoronate, herbal medicine extracts, tinctures: sea urchin chinensis, chinensis tincture, cuckoo extract.

Rot extract, Seimetsu Tochino Mi Extract, Capsicum Extract.

capsicum tincture N) Herbal medicine powders: Powdered medicinal herbs, Prunus elegans powder, Prunus elegans powder.

In addition, the composition of the present invention has physical properties such as viscosity and chicken tropism, as well as adhesion of a naive film formed after application of the composition, washability, releasability, etc. for,
Polyvinylpyrrolidone, polyvinylpyrrolidone/vinyl tate copolymer, IJ resin, methyl vinyl ether/maleic anhydride copolymer, vinyl acetate resin, and other lower alcohol- or water-soluble polymer compounds are used as a whole. It is possible to blend about θ to 5 cycles, and a hydrophilic tangle polymer can also be blended.

Add inorganic insoluble substances such as Naomatomo, kaolin, bentonite, Shichilight Co., Ltd. aluminum hydroxide, zinc oxide, cellulose powder, etc. to about 50% for the purpose of adjusting physical properties, increasing volume, or as a drug retention agent. You can also do that.

There are no particular limitations on the method for producing the alcohol glue composition of the present invention, and after dispersing and dissolving the carboxyvinyl polymer in a predetermined solvent, alcohol-soluble nylon may be added and dissolved by heating, or conversely, it may be dissolved in a solvent. After dissolving the alcohol-soluble nylon, the divinyl polymer may be added and dissolved. Furthermore, the cal-xyvinyl 4-rimer and the alcohol-soluble nylon may be immersed in a solvent at the same time, sufficiently swollen, and then heated. Any method such as dissolving may be used. In this case, if it is necessary to incorporate drugs into the fragrance, it is desirable to add them at the final stage.

As mentioned above, the alcohol dal composition of the present invention is neutralized and thickened with alcohol-soluble nylon, so there is no off-odor that occurs when conventional organic amine-based neutralizers are used, and there is no unpleasant smell. It has no skin irritation and is highly safe. Furthermore, since it has little reactivity with drugs, etc., it does not impair the stability of these components and does not cause a decrease in the viscosity of the 4R, and it is possible to improve the 4R by blending compounds with phenol groups and ester groups. , and the viscosity does not decrease.

Next, experimental examples will be shown to specifically explain the effects of the present invention. [Experimental Example 1] Carboxyvinyl polymer (Wako Tsumugi) was added to a solvent made by mixing ethanol and water at a ratio of 80:20. 0.25% of Hypiswako-105 (manufactured by Yakusha) was dissolved, and alcohol-soluble nylon (Ultraamide IC, manufactured by BASF) was added thereto in the amounts shown in Table 1, and its viscosity was measured using a viscometer. . In addition, the measurement uses an A2 or flat 3 rotor depending on the viscosity, and is performed at 6 to 60 rp.
The test was carried out at room temperature.

The results are shown in Table 1.

[Experimental Example 2] Methyl salicylate was selected as a representative of both phenolic compounds and ester compounds, which were conventionally considered difficult to blend as drugs, and the following formulations 46 and A7 were blended with methyl salicylate.
After storing these bottles at 50°C for 1 month and at room temperature for 3 months, their viscosity was measured using a B-type viscometer in the same manner as in Experimental Example 1. Shown in the table.

Prescription 46 A7 Methyl salicylate 5.89 5.09
Triethylamine -0,49
From the results in Table 1.2, by blending alcohol-soluble nylon with carboxyvinyl polymer,
A thickening effect has been observed, and even when phenol and ester compounds, which were traditionally considered difficult to blend into systems thickened with alcohol-soluble nylon, or whose amounts were limited, the viscosity of the product did not decrease at all. It has been found that it is stable and stable.

Examples will be shown below, but the present invention is not limited to the following examples.

(Example 1) Facial Back Ultraamide IC (manufactured by BASF)
10.0.9 Flavorings
0.11i solvent
89.6Ii [1 is! 01, which is a mixture of tanol, water, and propylene glycol in a weight ratio of 70:22:3, was used.

Cal 4 Pole 940f: After solving 8, Ultra Aty
was added and heated to dissolve, and after cooling, fragrance was added to create a facial powder. This thing is che.

- Fill it into a tube and make it into a product.

The crystal spreads well when used, does not run off, dries quickly, and can be completely peeled off as a single film after use.

[Example 2] Trauma agent pendelkonium chloride 0.0
1g Chlorhexidine gluconate 0
．． 01,9 Nahuazoline hydrochloride
0.1g maleic acid chlorpheniline
0.1.9 Hibis! Co 105 (manufactured by Wako Tsumugi Pharmaceutical Co., Ltd.) 0.25p Ultraamide TC
12.1 Ultraamide IC in solvent
was added and heated to dissolve, Hipiswoko 105 was dissolved therein, and other ingredients were added to the final fireworks to prepare a trauma agent. This is filled into a chip and made into a product. When applied to the affected area, the crystal does not run off or stickiness, and dries quickly to form a nylon coating, which helps to clean the wound surface. It showed high resistance against bacteria, etc. In addition, after use, it can be easily swelled and peeled off by washing with water, or it can be peeled off as a single film. [Example 3] External anti-inflammatory analgesic agent methyl salicylate 3.
5g glycol salicylate
1.591-menthol
5.0g nonylic acid panillylamide
0.01,9 Hipi 2'7: f-1050,25I
iUltra Acid IC 12.0 g Hipis Wako-105 and Ultra Amide IC were added to a solvent, heated and dissolved, and after cooling, other ingredients were added to obtain an external anti-inflammatory analgesic.

Quartz crystal is a highly transparent jelly, and when applied to the affected area, it did not run off like a liquid, and the drug was retained by the dry film formation, resulting in sustained medicinal efficacy. Maku,
The viscosity of the crystal did not decrease even after long-term storage, and it maintained its glue-like form. [Example 4] Skin disease treatment agent Glycyrrhetinic acid 0.5g Indomethacin 1. OIi Cal is Paul 940
0.3p ultra electrode
10. OJ solvent 88
．． The 2II solvent used was a mixture of ethanol, water, and propylene glycol in a weight ratio of 80:10:10.

The manufacturing method was the same as in Example 1.

Quartz is jelly-like and has excellent transdermal absorption.In addition, when conventional organic amine neutralizers are used, there is a high possibility that an acid-base reaction will occur with the active ingredient. However,
With crystal, there is no such concern, and the stability of the active ingredients is maintained over a long period of time4.

[Example 5] Anti-itch agent Diphenhydramine 0.5I Didecaine hydrochloride 0.3.9 Glycyrrhetinic acid 0.1g Nomenthol 3.0g Hibis! K-105 0.39 Ultraami IC 1.5g I-Livinylpyrroli-P (K-90) 0.5
．． 9 An anti-itch agent was produced according to Example IK.

The crystal is transparent and jelly-like, making it easy to use. Also, when this product was applied to the affected area, a film was formed after drying, but this film was extremely thin and completely unnoticeable, and could be easily removed by washing with water after use. Furthermore, the viscosity of the quartz crystal did not decrease after being stored for a long period of time.

Applicant: Lion Corporation Agent: Patent Attorney Takashi Kojima l Patent attorney Hanyo Takahata

Claims (1)

[Scope of Claims] 1. An alcohol glue composition for external use, characterized in that it is made by blending carboxyvinyl I remer and alcohol-soluble nylon in a solvent mainly composed of lower alcohols. 2. The composition according to claim 1, wherein the concentration of lower alcohol in the solvent is 60% by weight or more. 3. The composition according to claim 1 or 2, wherein the amount of alcohol-soluble nylon is at least three times the amount of xyvinyl polymer.