JPH03106818A - External drug composition for skin - Google Patents

Abstract

PURPOSE:To obtain an external drug composition for skin giving warm stimulation to the skin and free from pain of the skin by compounding a skin- stimulating agent or a pungent crude drug to a composition containing cinnamaldehyde. CONSTITUTION:The objective composition can be produced by compounding 0.001-5wt.% of natural or synthetic cinnamaldehyde or a cinnamaldehyde- containing composition and a skin stimulation agent (e.g. salicylic acid or Guinea pepper) or a pungent crude drug such as SENKYU (rhizome of Cnidium officinale) and forming the mixture in the form of a drug by conventional method. The amount of the skin-stimulation agent is 0.001-10wt.% and that of the pungent crude drug is 0.01-10wt.%. Both agents may be used in combination. The composition can be used in the form of salve, poultice, liniment, lotion, ointment, gel, plaster, pack, spray, bathing agent, hair liquid, hair tonic, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an external preparation composition that provides thermal stimulation to the skin. It has been known for a long time that applying skin stimulants such as chili pepper powder, chili pepper extract, and capsaicin to the skin gives a warming sensation to the skin. Utilizing their effects, these are used in topical skin preparations for the purpose of anti-inflammatory and analgesic treatment for neuralgia, stiff shoulders, rheumatism, lumbar pain, etc.
However, the currently commonly applied concentrations produce a low thermal sensation on the skin, and when applied as a poultice for a long period of time, one often experiences pain rather than a thermal sensation. On the other hand, attempts have been made to give a warming sensation to the skin using pungent herbal medicines such as Kawakatsu, Nakumi, and Sanshu, but no actual results or sensations can be expected. The purpose of the present invention is to provide a composition for external use on the skin that provides a felt and actual thermal sensation and does not cause skin pain. The external skin preparation composition of the present invention is characterized by containing a natural or synthetic cinnamic aldehyde-containing substance and a skin irritant or pungent herbal medicine. The present invention will be explained in more detail below. As the cinnamaldehyde, both synthetic and naturally derived substances can be used, and two or more types of substances, such as synthetic aldehyde and cinnamon oil, may be used in combination.

As a natural product containing cinnamic aldehyde, Cinnam
osium cassia BLυME, C.
obtussifolium NEES,C.
zaylanicum NEES, C. inners
REINV ax BLLIMEpC. burman
ni BLUM*C, cliLawan BLU
ME*C. javanicum BLUMES, C.
pseudo-1oursirii HAYrC. s
There are barks of plants of the same genus in the Lauraceae family, such as L. ieboldii MEISN.

The essential oil obtained by steam distillation of these barks contains a large amount of cinnamaldehyde and is commercially available as cinnamon oil.
Cinnamon oil is easily available and is preferred as the natural-derived cinnamaldehyde-containing material of the present invention.

Skin irritants include salicylic acid derivatives, nicotinic acid derivatives, capsicum, camphor, menthol, mustard oil,
Turpentine oil can be used alone or in combination of two or more. As salicylic acid derivatives, salicylic acid, methyl salicylate, glycol salicylate, etc. are commercially available, and as nicotinic acid derivatives, nicotinic acid, nicotinic acid amide, etc. are commercially available and are preferred because they are easy to obtain. In addition, chili peppers include chili pepper powder,
In addition to chili pepper extract, it also contains compounds that are irritating to the skin, such as capsaicin. Camphor, currant oil, turpentine oil. Menthol has also been used as a skin irritant since ancient times, and is effective. Examples of the pungent herbal medicine of the present invention include Toki (Toki) and Kawakatsu (Kawakatsu).
Senkyu), Shokiyou, Xerophyll, Sansho, Kurecha 1JL (Goshuyu),
Bushi, gajutsu, safflower, clove, botanpi, kaigai, japonica, arnica, etc. are used singly or in combination of two or more. Pungent herbal medicines can be used as powders obtained by drying or pulverizing these plants, or as extracts. What is the extract here?
Plant or crude drug extracts, diluted solutions, concentrated extracts,
and its dry powder. The extract is obtained by extracting the above dried powder of the plant or herbal medicine using water or an organic solvent, for example, a water-containing hydrophilic organic solvent such as aqueous alcohol, as the extraction solvent. The extraction temperature is usually room temperature. The obtained extract can be used as it is, or after dilution, concentration, or freeze-drying, it can be used as a powder or paste. In addition, each extract used in the formulation examples described later was obtained by the above-mentioned extraction method.

The skin external preparation composition of the present invention can be obtained by blending a cinnamic aldehyde-containing substance with a skin stimulant or a pungent herbal medicine, and formulating the mixture as appropriate depending on the dosage form. A skin stimulant and a pungent herbal medicine can also be combined together.

The amount to be incorporated into the skin external preparation composition depends on the dosage form, etc.
Cinnamaldehyde-containing substances such as cinnamic aldehyde and cinnamon oil. A suitable amount is 0.001 to 5% by weight. Further, in the case of skin stimulants, 0.001 to 10% by weight is suitable, and in the case of pungent herbal medicines, 0.01 to 10% by weight is suitable. Forms of the skin external preparation composition of the present invention include plasters, poultices, liniments, lotions, ointments, gels, plasters, packs, sprays, bath salts, hair liquids, hair growth agents, etc. It can take any dosage form. According to the present invention, by blending cinnamic aldehyde with a skin stimulant or pungent herbal medicine to form a skin external preparation composition, the skin temperature can be lowered by promoting blood flow at the application site. It can give you a tangible and real effect, and it also relieves excessive skin irritation and does not cause pain to the skin. Example 1 (Confirmation of Skin Temperature Raising Effect) As representative examples of pungent herbal medicines and skin stimulants, Namemi and Chili pepper were selected, respectively, and the effects on skin surface temperature when used in combination with cinnamon oil or cinnamic aldehyde were evaluated. ．． (Left below) A bag is manufactured by mixing each component shown in Table 1 above,
Appropriate amounts were applied to the inner forearms of five subjects. The pack was removed 15 minutes after application, and the degree of warmth was measured immediately, 10 minutes, 20 minutes, 30 minutes, and 60 minutes later using an infrared thermograph (manufactured by NEC Sanei) and a deep body temperature monitor (Terumo II1). , evaluated by measuring skin surface temperature and deep skin temperature. The test results are shown in Table 1. In addition, Table 1
The skin surface temperature increase temperature and the deep skin temperature increase temperature are the maximum temperature change (20
minutes) and is the average value of 5 people. As shown in Table 1, Samples 1 and 2 had no effect on increasing skin surface temperature or deep skin temperature. In specimen 3, the skin surface temperature increased by approximately 1°C, but no increase in the deep skin temperature was observed. On the other hand, in products 1 and 2 of the present invention, which use ginger or chili pepper together with cinnamon oil, the skin surface temperature was about 1.3 to 1.5°C, and the deep skin temperature was about 0.5 to 0.
．． A significant increase of 8°C was observed.

Example 2 (Confirmation of skin pain) The degree of pain when the chili pepper or chili pepper and cinnamon oil used in Example 1 were used together in the form of a poultice was investigated. (containing 0.2%). Furthermore, the concentrations of quince, chili pepper, and cinnamon oil used here were sufficiently effective against increases in skin temperature. *2) For example, 1
/5 indicates that 1 out of 5 people felt pain *3) Vap-based glycerin 22. Owt% titanium oxide l. Ovt% gelatin
6.5wt% dialdehyde starch
0.5vt% carboxyvinyl polymer 2. O
vt% citric acid 0.5vt% The ingredients shown in Table 2 above were mixed and applied to cloth to produce a warming poultice, which was applied to both arms of five subjects and the pain was measured 3 hours later. The presence or absence of
It was shown to. As shown in Table 2, it can be seen that the present invention, which uses Namemi extract or chili pepper extract in combination with cinnamon oil, causes almost no pain compared to commercially available products, even though the temperature rises significantly. Example 3 (Preparation of external preparation composition) External preparation compositions having the following formulations and dosage forms were prepared. Formulation example 1 (lotion) Cinnamic aldehyde 0.5vt% Cinnamon extract 0.5wt% di-tocopherol monoacetate 0.2wt% Stearic acid
10, Ovt% cocoa butter
2, Ovt% purified lanolin
2. Owt% triethanolamine
4. Owt% glycerin
16. Owt% amount total 100. Owt% (blank space below) Formulation example 2 (liquid) Cinnamon oil Angelica extract di-camphor L-menthol Eucalyptus oil turpentine oil Ethanol Ice-making formulation example 3 (back) Cinnamon aldehyde Ginger tint l-Menthol polyvinyl alcohol Ethanol Glycerin Kaolin Fragrance 0. 5 glances t% 1, Owt% 5. Owt% 3. Ovt% 1. Ovt% 2.5vt% 80. Owt% Total amount 100. Ovt% 0.5wt% 1, Ovt% 0.5wt% 20. Ovt% 20, Ovt% 5.0%It% 6. Owt% 0.5wt% Total amount 100, Out% Formulation example 4 (basis) Cinnamon oil Glycol salicylate di Monocamphoracetic acid Tocopherol Capsicum extract 1-Menthol Glycerol Titanium oxide Gelatin Dialdehyde Starch Carboxyvinyl polymer Citric acid 0.2vt% 1 ．． OIIIt% 0.5vt% 0.3vt% 0.2vt% 0.1wt% 22. Owt% 1. Ovt% 6.5wt% 0.5vt% 2. Owt% 0.5vt% Total amount 100. Owt% (blank below) Formulation Example 5 (Basic agent) Cinnamon oil Dry extract Extract Auricularis extract Mentha oil Clove oil Eucalyptus oil Glycerin Oxide Titanium Gelatin Dialdehyde Starch Carboxyvinyl polymer Citric acid Formulation example 6 (Oil-based ointment) Cinnamon oil Goshuyu extract Purification Lanolin and beeswax total of 0.1vt% 1. Owt% 1. Owt% 0.5vt% O a 5 vt% 0.5%+1% 22. Ovt% LOent% 6.5wt% 0.5%+i% 2. Qwt% 0.5wt% 1. Owt% 1. Ovt% 5. Owt% 5, Owt% amount 100. Ovt% Formulation example 7 (w/o emulsion) Cinnamon aldehyde Botanica extract Sarashimitsu Stearyl alcohol Cholesterol Vaseline Total formulation example 8 (O/W emulsion) Cinnabar oil Calamus extract White petrolatum Stearyl alcohol Propylene glycol Polyoxyethylene curing Castor oil Monostearate Glycerin Rose Methyl benzoate Provil paraoxybenzoate Total 0.59t% 1. Owt% 8. Owt% 3. Owt% 3.0t% Amount 100. Owt% 0 5vt% 0 5wt% 25 0wt% 20 0ut% 12 0wt% 4 0wt% 1 0ut% 0 1wt% 0 1wt% Amount 100. On% Formulation example 9 (hair tonic) Cinnamic aldehyde senbritin quinicotinic acid amide 1-menthol ethanol fragrance formulation example 10 (gel) Cinnamon oil arnica tincture 1-menthol dl-camphorsalicylate Methyl salicylate glycol carboxyvinyl polymer Propylene glycol ethanol tri Ethanolamine 0.1vt% 0.5wt% 0.lwt% 0.3wt% 65. Owt% 0.2vt% 1. Ovt% 1. Owt% 3, Ovt% 3. Ovt% 5. Ovt% 5. Ovt% 1. Owt% 28. Ovt% 28. Ovt% 0. lvt% total 100. Ovt% Formulation Example 11 (Lotion) Cinnamon Oil Salamander Extract Turpentine Stearic Acid Cocoa Butter Refined Lanolin Triethanolamine Glycerin Formulation Example 12 (Massage Cream) Cinnamon Aldehyde Gajutsu Extract Canole Boxy Vinyl Polymer Glycerin Dibrobylene Glycol Hardened Castor Oil Paraben potassium hydroxide fragrance total 0.5vt% 1. Owt% 0.1wt% 10. Ovt% 2. Owt% 2. Owt% 4, Owt% 16. Ovt% 0.2vt% 1. Ovt% 0.4wt% 40. Owt% 20. Ovt% 0.3vt% 0, lwt% 0.12wt% 0.08vt% Amount 100. Owt% Formulation example 13 (basis) Cinnamon oil powder di-camphor 1-menthol glycerol titanium oxide gelatin dialdehyde starch carboxyvinyl bolimar citric acid 0.2 vt% 0.8 vt% 0.5 vt% 0.5 vt% 22. Ovt% 1. Ovt% 6.5vt% 0.5vt% 2. Ovt% 0.5vt% Formulation example 14 (liquid) Cinnamon oil mustard oil di-camphor 1-menthol Keigai extract ethanol 0.5wt% 0.1wt% 5. Ovt% 3. Owt% 1. Owt% 80. Owt% Total 100. Owt%

Claims (1)

[Claims] 1. A skin external preparation composition characterized by blending natural or synthetic cinnamaldehyde or a cinnamic aldehyde-containing substance with a skin irritant or a pungent herbal medicine.