JPS6115845A - Shellac-containing composition for epidermis - Google Patents

Abstract

PURPOSE:To provide the titled composition resistant to water, having excellent adhesivity to the skin, and giving a coating film having high releasing rate of the drug contained therein, by compounding shellac to a solvent composed mainly of a lower alcohol. CONSTITUTION:The objective composition for epidermis can be prepared by compounding shellac to a solvent composed mainly of a lower alcohol. Shellac has been examined as a coating material of tablet or a raw material of a slow- releasing preparation. When shellac is used in a film-forming composition for epidermis, a composition having improved water-resistance, action of drug-retaining matrix, high safety and excellent adhesivity to the skin, and moisturizing effect to the skin can be obtained. The composition also has high activity to release the contained drugs such as disinfectant (e.g. benzalkonium chloride), anti-inflammatory and analgesic (e.g. salicylic acid), etc. The amounts of shellac, drug and the lower alcohol are preferably 1-50%, 0.01-30% and 95-40%, respectively.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention is generally applied to lower alcohols which are sprayed or applied onto the skin to form a film and whose medicinal ingredients are absorbed externally. This invention relates to a skin composition characterized by containing shellac as a main solvent.

Conventional technology Conventionally, known methods for treating wounds include disinfecting the affected area with a disinfectant solution and fixing and covering the wound with a bandage, or applying ointment, powder, etc. to the affected area and fixing it with a bandage or the like. ing. Additionally, a method of applying or spraying a hydrophobic polymer solution onto the skin has also been used. However, these use acetone and ethyl acetate as solvents and contain polymers that dissolve in them, so: 1. The film forming agent becomes sticky when dried.

2. There is a safety problem.

3. When removing the film from the skin, it must be wiped off with the same solvent, and it is difficult to remove it without damaging the skin.

It has the following drawbacks. (Unexamined Japanese Patent Publication No. 50-4914,
(Refer to Japanese Unexamined Patent Publications No. 50-25725) Also, there are known examples in which water is used as a solvent and a water-soluble polymer is blended, but these 1. do not form a transparent film; 2. are sticky even after the film is formed. 3. The coating has poor adhesion to the skin; 4. The drying time of the coating is long.

Furthermore, examples in which polyvinyl butyral and PVA partially saponified polymers are blended using ethanol or water-ethanol as a solvent (JP-A-58-78633, JP-A-59-
47269) are also known, but these have the problem that the adhesion of the coating to the skin is poor. It is also known to use an ethanol-water system as a solvent and blend an alcohol-soluble polyamide (see JP-A-57-112323 and JP-A-58-69811); however, the alcohol composition becomes thicker over time. It has the problem of gelation.

As mentioned above, conventional therapeutic film-forming compositions have various problems7, and the current situation is that a film-forming composition with sufficient effects has not yet been obtained.

Next, the conventional technology for shellac, which is contained in the composition of the present invention and is also a feature of the present invention, will be explained.

Sheratsku has traditionally been used as a finishing paint for wooden furniture, as a base for synthetic resin paints, as a binder paint for wood, as a surface and base paint for metals, as metal foil paints, as a finishing agent for paper, as a finishing agent for paper surfaces, and as a rubber gloss paint. It is used in printing ink materials, electrical insulation materials, polishing waxes, tape release agents, etc.

It is also being considered as a coating agent for tablets and as a raw material for sustained-release preparations. (Refer to Japanese Unexamined Patent Application Publication No. 55-23152.) However, its use as an external preparation for the skin is completely unknown, and there are no examples of external skin compositions aimed at forming a film. There are no documents, etc.

That is, the use of shellac as a skin composition for film formation is a novel finding first made by the inventor of the present invention.

Problems to be Solved by the Invention The object of the present invention is to obtain a film-forming composition that solves the problems listed below.

1. To obtain a sufficiently stable composition in which a film-forming substance is dissolved in a solvent mainly composed of a lower alcohol, and there is no thickening, gelling, or precipitation caused by the film-forming substance.

2. To obtain a highly safe composition.

3. To obtain a composition with sufficient quick drying properties.

4. To obtain a composition having sufficient skin adhesion.

5. To obtain a composition that is not sticky after film formation.

6. To obtain a composition that has a strong film and does not stain clothes, etc.

7. To obtain a composition that has sufficient flexibility against skin movement.

8. To obtain a composition with sufficient drug release properties.

9. To obtain a composition that does not cause stuffiness or feel due to inhibition of physiological functions such as sweating and breathing when applied for a long time.

Means for Solving the Problem In view of the above situation, the present inventors conducted intensive research and found that a lower alcohol composition of shellac, which is a purified product from a natural product, has a remarkable effect as an agent for the skin. Heading: The present invention has been completed.

The present invention contains shellac and lower alcohol,
Polyhydric alcohol or its derivatives, essential oil components, as necessary.
Crotamiton, alcohol-soluble cellulose derivative, polyvinylpyrrolidone, polyvinylpyrrolidone copolymer,
The present invention relates to a shellac-containing skin composition characterized by blending a polyvinyl methyl ether copolymer, nitrified cotton, vinyl acetate, polyvinyl butyral resin, as well as drugs, additives, and the like.

Each component to be incorporated into the composition of the present invention will be sequentially explained below.

First, shellac, which is a feature of the present invention, will be explained in detail. The shellack used in the present invention is Japanese Shellac ■
Although the product name is "Shellac" manufactured by the company, it is not limited to this as long as it is generally a shellac that is soluble in ethyl alcohol.

Incidentally, "shellac" is made up of approximately 95% shellac resin and approximately 5% shellac wax, but "dewaxed shellac" in which the wax content is completely removed is also commercially available, and this is also fully applicable.

By the way, sheratsk is a leguminous plant (dilmanem).

American blackberry, Chinese lentil, giant bean tree, and pigeon pea.

It refers to the rank resin secreted by male and female larvae and female lac scale insects that parasitize plants in the mulberry family (such as acacia, intrapodium, etc.).

Normally, Sheratsuku is made by grinding and washing the raw materials, including the shells of dead parent insects, insect food, water-soluble pigments, proteins, sugars, earth and sand, and fibers, to remove impurities, and then removing the water-soluble substances. is eluted and then dissolved in a solvent to remove the solid residue. Depending on the variety, there are also products that have been dewaxed or have their pigments decomposed and removed. Shellac resin is thought to be a natural condensation product formed by chemically bonding organocarboxylic acids to each other as lactones, and although its chemical composition has not yet been completely elucidated, the following structural formula is accepted.

+1.1 Aleuritic Ac
1d): C,6If320,Oll 011 +10- (CH2>6-CH-C11-(CH2)
7-COOII (1972-, Nagel's formula) % Formula % Derivatives thereof In addition, shellac resin is said to contain up to 2% of butolic acid, myristic acid, and others.

In addition, Schluck wax is a warm alcohol soluble wax (
Raksha diacero) L which is 85% of total wax
t (C25H510H) and cyasseric acid (02585
It is said to contain esters of 1COOH) and warm alcohol-insoluble waxes, lasocerol (c32■65oH) and lasogalic acid (C3, 63COO■), as well as small amounts of other unsaponifiable waxes.

m1 Shellac used in the present invention is usually manufactured by Nippon Shellac Co., Ltd., NSC, C5,551, SSJ.

SST, NST, GN, I, dry transparent rack, dry milky white rank, etc. are used, but it is of course possible to use other alcohol-soluble shellacs.

In the present invention, the shellacs detailed above may be used alone or in combination of two or more.

Next, alcohols as solvents will be explained. The lower alcohol used in the present invention is particularly preferably ethanol or isopropyl alcohol, and polyhydric alcohol or its derivatives, as well as ginkgo oil and olive oil, may be used as necessary for plasticizing the film and dissolving or suspending the medicinal ingredients described below. , orange oil, cod liver oil, cinnamon oil, hydrogenated oil, sesame oil, soybean oil, castor oil, rapeseed oil, corn oil, turpentine oil, camellia oil, tincture oil, clove oil, or crotamiton.

More specifically, polyhydric alcohols and derivatives thereof include polyhydric alcohols, polyhydric alcohol alkyl ethers,
It means polyhydric alcohol alkyl esters, etc. In addition, polyhydric alcohols include ethylene glycol, diethylene glycol, triethylene glycol,
Polyethylene glycols such as PEG-200 and PEG-400, propylene glycol, polyethylene glycol-polyprohylene block copolymer, glycerin,
Examples include sugar alcohols such as toilette, erythresotho, and arabite. Examples of polyhydric alcohol alkyl ethers include cellosolves such as ethylene cellosolve and butyl cellosolve, polyoxyethylene octyl alkyl ethers such as polyoxyethylene lauryl ether, polyoxyethylene cetyl ether, polyoxyethylene stearyl ether, and polyoxyethylene oleyl ether; Examples include polyoxyethylene alkylphenol ethers such as polyoxyethylene octylphenol, polyoxyethylene nonylphenyl ether, and the like. Examples of polyhydric alcohol alkyl esters include glycerin fatty acid esters such as glycerin stearate and glycerin oleate; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate and polyoxyethylene sorbitan monostearate; Examples include oxyethylene monolaurate and polyoxyethylene monostearate. Incidentally, these alcohols can be used alone or in combination of two or more, if necessary.

In addition to the above-mentioned shellac, alcohols, essential oil components, crotamiton, etc., the shellac-containing skin composition of the present invention may also include bactericides, topical narcotics, antihistamines, anti-inflammatory analgesics, astringents, vitamins, etc. One or more physiologically active agents such as antifungal agents, coronary vasodilators, antihypertensive agents, peripheral nerve paralyzing agents, adrenocortical hormones, insect repellents, and crude drug extracts may be added. Further, when blending these, they may be dissolved or suspended in a polyhydric alcohol or its derivative, the above-mentioned essential oil component, crotamiton, or the like.

Here, the above-mentioned drugs will be specifically illustrated.

Examples of the disinfectant include benzalkonium chloride, betocetonilam chloride, cetylpyridinium chloride, domiphene bromide, dequalinium chloride, fradiomycin sulfate, homosulfamine, chlorhexidine, chlorhexidine glumanate, and the like.

Local narcotics include dypcaine hydrochloride, pyridoxine hydrochloride,
Examples include ethyl aminobenzoate, propylene hydrochloride, dimethysoquine hydrochloride, pramoosine hydrochloride, and lidocaine.

Antihistamines include diphencitramine, diphenhydramine hydrochloride, tripelenamine, tonsialsin,
Examples include chlorpheniramine isocypenzyl oleate, clemizole, diphenylimidazole, and the like. Anti-inflammatory analgesics include salicylic acid, methyl salicylate, glycol salicylate, indomethacin, ketophenene,
Examples include ibuprofen, ibuprofen piconol, piroxicam, glycyrrhizin, glycyrrhetinic acid, azulene, and the like. Examples of the astringent include dichloroaluminum aminoacetate, aluminum phenolsulfonate, and the like. Examples of sulfa drugs include sulfisoxazole, sulfapyridine, sulfamethoxypyridine, sulfamethoxine, and sulfadiazine. Examples of vitamin preparations include vitamins E, A, and D. Antifungal agents include pentachlorophenol, salicylic acid, trichlorophenol caproate, tribromophenol caproate, lauryltriphenylphosphonium bromide, diantazole chloride, paraacetylaminophenyl rhodan, thimerosal, tolnaftate, clotrimazole, etc. Can be mentioned. Coronary vasodilators include nitroglycerin, inosorbide nitrate, and the like. Examples of antihypertensive agents include clonidine, and examples of peripheral nerve paralyzing agents include β-menthol, camphor, thymol, and tesit. Examples of the blood circulation promoter include nonylic acid vanillylamide, nicotinic acid β-butoxyethyl ester, nicotinic acid benzyl ester, and the like. Examples of adrenal corticosteroids include prednisolone, dexamethasone, fluoromesolone, triamcinolone acetonide dycline, and the like. Insect repellents include N,N-diethylamide, bisethylenetetrahydrofurfural, butoxide, di-T-propylisocincoronate, diethyltoluamide, and the like. Examples of crude drug extracts include tinctures, ginger extracts, ginger tinctures, cacao extracts, and the like. Incidentally, the above-mentioned drugs are merely examples, and the present invention is not limited thereto, and of course, various other known drugs can be used as desired.

As mentioned above, the shellac-containing skin composition of the present invention contains shellac, a lower alcohol, if necessary a polyhydric alcohol or a derivative thereof, an essential oil component, crotamiton, and a drug, and further contains hydroxypropyl. One or more of alcohol-soluble cellulose m-conductors such as cellulose, polyvinylpyrrolidone, polyvinylpyrrolidone copolymer, polyvinyl methyl ether copolymer, nitrified cotton, vinyl acetate, and polyvinyl butyral resin may be used.

Furthermore, in addition to this, conventionally known additives such as transdermal absorption enhancers, stabilizers, anti-aging agents, fragrances, mineral oils, antioxidants, ultraviolet absorbers, and reinforcing fillers may be added as necessary. Also good.

Next, let's talk about the amount. Shellac blending amount is 1
-50% is preferable, and eel is also preferably 15-45%. The amount of the aforementioned drug is preferably 0.01 to 30%, most preferably 0.01 to 20%. Next, the amount of lower alcohol blended is preferably 95% to 40%, most preferably 80% to 40%. Next, the amount of polyhydric alcohol or its derivative, essential oil component, crotamiton, alcohol-soluble cellulose derivative, polyvinylpyrrolidone, polyvinylpyrrolidone copolymer, polyvinyl methyl ether copolymer, nitrified cotton, vinyl acetate, and polyvinyl brachyl resin is determined. 0.1-30% is preferable, 0.1-30%
20% is most preferred.

Next, a method for producing the skin composition of the present invention will be explained.

First, shellac is dissolved in alcohol in a closed container at room temperature. The skin composition of the present invention can be obtained by dissolving or suspending the above-mentioned components such as drugs, solubilizers, antioxidants, absorption enhancers, plasticizers, etc. in this.

The skin composition of the present invention has water resistance by containing shellac, has the action of a drug-retaining matrix, is safe, has good skin adhesion, and has a tough and flexible coating. It has a formative effect.

It also has a moisturizing effect on the skin and has a high release effect on the drug it contains.

Next, examples will be shown.

Example 1 (Anti-inflammatory analgesic for external use) 20 g of shellac resin (transparent mortar rack: manufactured by Nihon Shellac Kogyo Co., Ltd.) and 80 g of ethanol were dissolved in a flask at room temperature. This solution was mixed with a solution of 1 g of indomethacin dissolved in 3 g of crotamiton to prepare a topical anti-inflammatory analgesic.

Example 2 (Anti-inflammatory analgesic for external use) 20 g of shellac resin (transparent Mortarak 2, manufactured by Nippon Shellac Kogyo Co., Ltd.) and 80 g of ethanol were dissolved in a beaker at room temperature. This solution was mixed with a solution prepared by heating and dissolving 3 g of ketoprofen and 1 g of hydroxybenzophenone in 5 g of crotamiton to prepare an anti-inflammatory analgesic for external use.

Example 3 (trauma agent) Benzalkonium chloride 0.02 g □ Chlorhexidine gluconate 0.02 g Nafarison hydrochloride 0.1 gl6 Marein Schlafuku 49.7 g Ethanol 50.0 g Example 1
Shellac was added and dissolved in accordance with 2 and 2, and other ingredients were added to prepare a wound agent.

Example 4 (Anti-itch agent) Diphenhydramine 0.5 g Dipcaine hydrochloride 0.3 g Glycyrrhetinic acid 3.0 g Menthol 3.0 g Shellac
20.0 g polyvinylpyrrolidone 4.0 g ethanol
72.0 g An anti-itch agent was produced according to Examples 1 and 2.

Example 5 (External anti-inflammatory analgesic) Methyl salicylate 3.5 g Glycol salicylate 1.5 g l-menthol 5.0 g Nonylic acid vanillylamide 0. old g glycerin
10.0 g shellac
40.0 g ethanol
40.0 g An external anti-inflammatory analgesic was produced according to Examples 1 and 2.

Example 6 (coronary vasodilator) Isosorbitol nitrate 0.1 g Isopropyl myristate 0.3 g Glycerin 10.0 g Shellac
40.0 g polyvinylpyrrolidone-vinyl acetate copolymer 3.0 g ethanol
46.0 g Examples 1 and 2
A coronary vasodilator was manufactured according to the method.

Example 7 (Antibacterial agent) Clotrimazole 1.0 g Ethanol 60.0 g Shellac 30.0 g Polyvinylpyrrolidone-vinyl acetate copolymer 5.0 g Glycerin
4.0gAn antibacterial agent was produced according to Examples 1 and 2.

Effects The shellac-containing skin composition of the present invention has the remarkable effects listed below.

1. It is sufficiently safe as a pharmaceutical composition.

2. Has sufficient quick drying properties.

3. The film of the composition has high skin adhesion, is strong, is not sticky, and does not stain clothes.

4. It has sufficient flexibility and has a moisture-permeable effect even when applied for a long time, and can prevent dryness due to inhibition of physiological functions such as sweating and breathing.

5. Has sufficient sustained release properties.

6. This composition can be easily prepared at room temperature,
It is possible to prepare thermolabile drugs.

, Proceedings (Spontaneous) September 24, 1985 1, Indication of the case 1988 Patent Separate Section No. 136381 2, Name of the invention Shellac-containing skin composition 3, Patent applicant (contact information: ffi 0942B -3-2101 Hideki Yamakawa) 6. Contents of amendment The following corrections will be made to the specification of this application.

(1) In the specification, the first column of “3. Detailed description of the invention”
In lines 8 to 7 from the bottom of the page, the words ``absorbed by external application'' are corrected to ``transdermal absorption.

(2) In the same book, the phrase ``precipitation'' in the second line from the bottom of page 4 is corrected to read ``r phenomenon''.

(3) In the same book, from the fourth line to the third line from the bottom of page 7, “
"Natural condensation products" should be corrected to "Natural condensation products."

(4) In the same book, insert ``1,3-butylene gellicol, j'' next to ``polyethylene glycols'' in the 8th line from just above the 10th line.

(5) In the same book, the word ``toilet'' in lines 10 to 11 from just above No. 10 is corrected to read ``r tray soto''.

(6) In the same book, in the third line from the bottom of page 12, after "diphenylimidazole", insert "ketotifen j".

(7) In the same book, the first line on page 13: “Ibuprofen.”
Next, insert "Flurbiprofen, Pranoprofen".

Claims (1)

[Claims] 1. A skin composition characterized by blending shellac with a solvent mainly composed of lower alcohols.