JPH0366286B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to hydrophilic poultices, which are external skin patches used for anti-inflammatory and analgesic treatments, and particularly to improvements in the base thereof. Poultices are used to treat lower back pain, neuralgia, rheumatism, stiff shoulders,
It has been used for a long time to treat bruises, sprains, etc. For these purposes, the base contains medicinal ingredients such as salicylic acid esters, camphor, and menthol.
and oil-based active ingredients such as emollient ingredients such as liquid paraffin and polybutene. The composition, manufacturing method, etc. of such poultices are disclosed in numerous documents, and include gelatin, polyvinyl alcohol, thickeners such as carboxymethyl cellulose and sodium polyacrylate, bulking agents such as kaolin, bentonite, and talc, and propylene glycol. ,
It is produced by kneading a humectant such as glycerin, sorbitol, or ethylene glycol and water, and then mixing the oil-based active ingredient with the mixture. Since the composition of this type of poultice is a simple mixed system, the aqueous and oily components tend to separate quickly over time after manufacture. Therefore, when the drug was applied, the efficacy of the drug was inconsistent and the duration of the drug's effect was short. In addition, the separated oily ingredients contain high concentrations of oil-soluble medicinal ingredients, which can cause excessive skin irritation.
It was also likely to cause undesirable side effects such as redness. As a result of extensive research, the present inventors improved these points and completed the present invention by increasing the water content and creating an oil-in-water type emulsified poultice. That is, the present invention contains oil-based active ingredients and 55% by weight.
The above water-containing base composition is emulsified using two or more nonionic surfactants having different HLBs and having an HLB in the range of 10 to 18 in an amount of 0.3 to 0.7% by weight, and The present invention provides an oil-in-water emulsion type poultice whose pH is adjusted to 5 to 6. The poultice of the present invention contains sodium polyacrylate, carboxyvinyl polymer,
One or more types of carboxymethylcellulose are used, light anhydrous silicic acid, hydrated silicon oxide or titanium oxide is used as a filler, and an organic substance such as propylene glycol, glycerin, sorbitol or ethylene glycol is used as a humectant.
The thickener is preferably thickened by adding an aluminum compound such as aluminum hydroxide or aluminum sulfate to form a crosslinked structure with aluminum.
Thereby, the moisture content can easily be increased to 55% or more. In particular, it is preferable to use aluminum hydroxide. As an example of the formulation of thickeners, fillers and humectants, a combination of sodium polyacrylate, hydrous silicon oxide and glycerin is preferred. In the present invention, examples of the nonionic surfactant include polyoxyethylene sorbitan fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, and polyoxyethylene glycerin fatty acid ester, particularly polyoxyethylene sorbitan fatty acid ester. Esters are preferred in terms of compatibility with thickeners and the like, and among these, polyoxyethylene sorbitan monooleate gives good results. In order to obtain a stable oil-in-water emulsion in the present invention, it is necessary to use two or more nonionic surfactants with different HLBs in combination. Typical examples are HLB10 and HLB15
combination of activators, i.e., NITSUKOL TO-
106 and Nitsukor TO-10 (manufactured by Nikko Chemicals Co., Ltd.)
can be mentioned. If the amount used is too small, emulsification will be insufficient, and if it is too large, too many bubbles will form, so a range of 0.3 to 0.7% is appropriate. The emulsification temperature should be 35 to 70℃ because if it is too high, it will cause coalescence and become unstable.
A range of is preferred. The emulsification time and stirring speed are related to temperature; when the temperature is relatively high, the stirring speed is short and the stirring speed is slow, and when the temperature is low, the emulsification time is long and the stirring speed is high. These conditions can be determined by ordinary researchers through experiments. In addition, poultices have a PH level that is similar to that of human skin.
It is desirable to reduce side effects by keeping the pH close to (4.5 to 6.5), and from the standpoint of stability of the main drug salicylate esters, the lower the pH, the better, and the most suitable pH for poultices is 5 to 6. I can do it. PH regulators include glycolic acid, malic acid,
It is preferable to adjust the pH to 5 to 6 using an organic acid such as lactic acid, tartaric acid, succinic acid, citric acid, etc., and inorganic acids are generally not preferable. The poultice of the present invention obtained as described above is in an oil-in-water emulsion state in which the oily component is formed into extremely fine droplets, so it gradually exerts a certain medicinal effect, has a long duration, and has no side effects. It is an excellent poultice with almost no expression. Further, since the water content is high, cooling can be performed effectively, which is advantageous, and moreover, the water content of 55% or more can be stably maintained. Furthermore, the PH is adjusted to 5 to 6, and the poultice of the present invention is excellent in terms of the stability of the main drug over time and its effect on the skin. The following examples and comparative test examples are shown. Example 1 Component A below was maintained at 60°C and stirred, while component B was gradually added and stirred for 30 minutes. Then while stirring 40
The mixture was cooled to 0.degree. C. and spread on flannel or nonwoven fabric to a thickness of about 1 mm to obtain a plaster. Component A: A solution obtained by dispersing 0.5 parts of titanium oxide and 0.5 parts of aluminum hydroxide in 3.4 parts of purified water is added to 22 parts of purified water at 60°C and stirred. While stirring, a solution prepared by dissolving 0.5 part of polyoxyethylene sorbitan monooleate (Nitsukor TO-106) in 5 parts of liquid paraffin is added. Next, a solution prepared by dispersing 3 parts of sodium polyacrylate in 20 parts of glycerin is added, and the mixture is sufficiently stirred while maintaining the temperature at 60°C until the mixture becomes uniform. Component B: Add 4 parts of hydrated silicon oxide (Carplex, manufactured by Shionogi & Co., Ltd.) and 0.5 parts of succinic acid to 37 parts of purified water at 60°C, and stir while maintaining the temperature at 60°C. Slowly add 2 parts of carboxyvinyl polymer with stirring. Next, 0.6 parts of dl-menthol, 0.4 parts of dl-camphor, 0.3 parts of methyl salicylate, 0.1 part of ethylene glycol salitate, and 0.2 parts of polyoxyethylene sorbitan monooleate (Nitsukol TO-10) were mixed into the previous solution. Add and stir thoroughly while heating to 60℃ until uniform. Example 2 2 parts of light anhydrous silicic acid is added to 57.1 parts of purified water at 60°C, and the mixture is stirred while being heated to 60°C. Add 0.5 parts of titanium oxide and 0.5 parts of aluminum hydroxide to 5 parts of purified water.
Add the dispersed liquid to the mixture and stir until it is homogeneous. While stirring, add 0.6 parts of dl-menthol, 0.4 parts of dl-camphor, 0.3 parts of methyl salicylate, 0.1 parts of ethylene glycol salicylate, 5 parts of polybutene,
0.2 parts of polyoxyethylene sorbitan monooleate (Nitsukor TO-10) and polyoxyethylene sorbitan monooleate (Nitsukor TO-10)
-106) Add a mixture of 0.3 parts. 60℃ for 30 minutes
After stirring while maintaining the temperature, cool to 40°C. Next, a solution obtained by dispersing 5 parts of sodium polyacrylate in 20 parts of glycerin is added and stirred until the mixture is sufficiently homogeneous. Further, 3 parts of lactic acid was added and stirred, and the mixture was uniformly spread on flannel or non-woven fabric to a thickness of 1 mm to obtain a poultice. Example 3 A poultice was obtained in the same manner as in Example 2, except that 1.4 parts of mepyrizole was used in place of menthol, camphor, methyl salicylate, and ethylene glycol salicylate. Comparative Example 1 Same as Example 1 except that 0.2 parts of polyoxyethylene sorbitan monooleate (Nitsukor TO-10), which was component B in Example 1, was replaced with 0.2 parts of polyoxyethylene sorbitan monooleate (Nitsukol TO-106). and obtained a poultice. Comparative Example 2 Polyoxyethylene sorbitan monooleate (Nitsukor TO-106) as component A of Example 1 0.5
A poultice was obtained in the same manner as in Example 1, except that 0.5 part of polyoxyethylene sorbitan monooleate (Nitsukor TO-10) was used. Comparative Test The following tests were conducted on the poultices obtained in Examples 1 and 2 and Comparative Examples 1 and 2 and five types of commercially available poultices. The active ingredients are shown in Table 1, and the test results are shown in Table 2.
Shown in the table. Test 1 Duration of stimulation The paste was applied to the shoulder, and the duration was defined as the time it took until no stimulation was felt (20 participants per group). Test 2 Side effects (redness) Remove the poultice after you no longer feel any irritation.
It was determined whether the skin where the patch was applied was red or not (20 people per group). Test 3 Identification of base, PH and determination of emulsification. Scrape off 0.5g of the paste of the plaster, mix it with 5ml of purified water in a mortar, measure the PH, and determine whether the paste is aqueous based or not. After determining whether it was an oil base, the paste was dispersed in water and the size of the oil droplets was observed with an optical microscope to determine whether emulsification occurred. Test 4 Moisture content Based on the general test method of the Japanese Pharmacopoeia, 10th edition, and the Karl-Fisscher method for determining moisture content.

【table】

[Table] All bases were water-based. As shown in Table 2, the plasters obtained in Examples 1 and 2 were emulsified in oil-in-water (O/W). The stimulation duration of these poultices is 6 to 7 hours, which is clearly longer than the 4 to 5 hours of commercial products. Furthermore, the pH was below 6, and none of the 20 patients developed redness. On the other hand, with the commercially available product, redness was observed in 1 to 3 patients, confirming that the poultice according to the present invention is superior. The moisture content of the poultices shown in Examples 1 and 2 of the present invention was 55% or more, and actual measurements were obtained that supported the excellent cooling effect as an anti-inflammatory agent. In addition, the poultices of Examples 1 and 2, which were stored in aluminum bags at 40°C for two months, showed no separation of water or oil, and there was almost no difference from the time at the start of storage, and they were sufficiently durable for use. In contrast to Atsuta,
Separation of oil was observed in the plasters of Comparative Examples 1 and 2 after one day at 40°C, and the nonwoven fabric became sticky and wet from the separated oil after one month at 40°C.

Claims (1)

[Claims] 1. A base composition containing an oil-based active ingredient and a water content of 55% by weight or more is mixed with a base composition having a different HLB from 10 to 10.
emulsify using two or more nonionic surfactants in the range of 18 in an amount of 0.3 to 0.7% by weight, and
An oil-in-water emulsion type poultice with a concentration of 5 to 6.