JPS63222113A - Plaster composition - Google Patents

Abstract

PURPOSE:To obtain a plaster composition having high cooling effects and raised releasability and percutaneous absorption of active ingredient, containing a water-soluble high polymer substance, an oil component, water, an oily gelatinizing agent and an active ingredient. CONSTITUTION:(A) 1-30wt.% preferably 2-15wt.% water-soluble high polymer substance (e.g. gelatin, PVA or xanthan gum) is blended with (B) 2-20wt.%, preferably 2.5-10wt.% oil component (preferably primary alcohol fatty acid) except an active ingredient, (C) >=30wt.%, preferably 40-75wt.% water content, (D) 1-15wt.%, preferably 2-10wt.% oily gelatinizing agent, preferably anhydrous light silica having 5-100mum average particle diameter of primary particles and (E) 0.01-20wt.% active ingredient such as methyl salicylate, indomethacin or peppermint oil). Although the composition contains the oil composition, the composition has no oozing of the oil component, no sag and no reduction in adhesivity by the action of the oily gelatinizing agent and shown excellent effects by application to the affected part.

Description

DETAILED DESCRIPTION OF THE INVENTION [Field of Industrial Application] The present invention relates to a patch composition, and more particularly to a patch composition in which the release of active ingredients from a plaster and the percutaneous absorption thereof are improved.

[Conventional technology]

Hydrophilic patches such as patches, poultices, and 79 Tsude preparations are:
It is an external preparation that is applied to areas affected by stiff shoulders, lower back pain, bruises, sprains, muscle pain, etc. In addition to the effect of the active ingredients, this effect is thought to be due to the water and oil contained in Toku, which promotes transdermal absorption of the active ingredients, the cooling effect of water, and the protective effect of plasters, etc. .

Conventionally, patches have generally used inorganic powders such as kaolin, Merck, bentonite, titanium dioxide, and zinc oxide as excipients, and water-soluble polymeric substances such as glycerin, sorbitol, etc. Humectants such as lyethylene glycol; prepared by adding and kneading water and active ingredients and applying a paste-like paste to a support (backing) such as paper, woven fabric, non-woven fabric, or plastic film.

[Problem that the invention seeks to solve]

By the way, the water and oil content in the paste has a cooling effect as described above, and also has the effect of increasing transdermal absorption of the active ingredient.

However, in the past, there was a limit to the amount of oil that could be stably contained in a patch with a high water content (because it could cause oozing and sagging), it was difficult to use oil other than the active ingredient. Oil content was excluded as much as possible.As a result, the release of the active ingredient from the plaster and its transdermal absorption were insufficient, and conventional patches often lacked quick-acting and long-lasting effects.

[Means for solving problems]

Under such circumstances, the present inventor conducted intensive research and found that water-soluble polymer substances and oil components other than active ingredients (hereinafter referred to as "
The patch-side composition prepared by blending an oil-based gluing agent (sometimes referred to as "oil component"), and 30% or more water of the total composition has the ability to release the active ingredient from the paste without oozing or blurring. We discovered that it has excellent transdermal absorption.
The invention has been completed.

That is, in the present invention, 1 to 30% by weight of a water-soluble polymer substance
, oil components other than active ingredients 2 to 20% by weight, moisture 307E
[This invention provides a patch-side composition characterized by containing 1 to 15% by weight of an oil-based gelling agent and an active ingredient.

In the present invention, water-soluble polymeric substances include, for example, gelatin, vector, etc. Lyacrylic acid? Sodium acrylate, sodium alginate? Lipinyl alcohol, polyvinylpyrrolid/? Lipinircal 4? xy copolymer,
? Lipinyl pyrrolidone Φ vinyl acetate copolymer,?
Liethylene oxide, carboxin methylcellulose,
Hydroquine methylcellulose, hydroxyethylcellulose, methylcellulose, ethylcellulose, xanthan gum, gum arabic, gum tragacanth, gum karaya,
Examples include methoxyethylene and maleic anhydride co-heavy metals, and these may be used alone or in combination of two or more. These water-soluble polymer substances account for 1 to 30% of the total composition.
%, preferably 2 to 15%.

Examples of oil components include -grade alcohol fatty acid ester; squalene, squalane, desu;
Examples include higher hydrocarbons such as rough-in; silicon-containing compounds such as silicone oil; and fatty acid glycerin esters such as monoglyceride, diglyceride, and triglyceride. Among them, the following general formula % formula % (in the formula, R1 has 2 to 18 carbon atoms, and the island has 1 to 18 carbon atoms)
Primary alcohol fatty acid esters represented by (representing a straight chain or branched alkyl group) are preferred, and among these, isopropyl myristate and octyldodecyl myristate have a high effect of improving release properties and percutaneous absorption, and are less irritating to the skin. Therefore, it is particularly preferable. The blending amount of these is 2 to 20%, preferably 2.5 to 10% of the total composition.

Examples of oil-based gelling agents include zopenzolidenesorpitol, 12-hydroxystearic acid, stearic acid metal salts, acylated amino acids, silica agents, ethylene vinyl acetate copolymers, and styrene-ethylene-phthylene-styrene hooks. Examples include copolymers, styrene-isoprene-styrene block copolymers, styrene-ptazoene-styrene block copolymers, and the like. Among these,
Considering the high water content in the patch composition, 7 silica agents are preferred, and among these silica agents, anhydrous light silica,
In particular, it is preferable that the average diameter of the secondary particles is 1 to 500 mμ, more preferably 5 to 100 mμ. This oil-based gluing agent is used to disperse the oil component in the patch-side composition,
Since it has the effect of stabilizing the uniformity and suppressing the seepage of oil components, a good patch-side composition that is not sticky to the skin can be obtained. The amount of this oil-based gelling agent is 1% of the total composition.
~15%, especially 2-10% is preferred.

Furthermore, it is essential that the patch composition of the present invention contains 30% or more of water; if it is less than this, the effects of the present invention will not be achieved. In particular, it is preferable to mix water in an amount of 40 to 75% of the total composition.

In addition, as active ingredients, commonly used in such cases, for example, methyl salicylate, glycol salicylate, indomethacin, etc. - One or more of menthol, pepper oil, eucalyptus oil, dl-camphor capsicum extract, vanillylamide nonylate, tocopherol acetate, sophenhydramine, alpha maleic acid, thymol, etc. are blended. This amount is generally 0.
01-20% is preferred.

In addition to the above-mentioned essential ingredients, the patch composition of the present invention may optionally contain ingredients commonly used in patches, such as:
Propylene glycol, glycerin, lupitor, -
One or more types of humectants such as Lietere/glycol, lactic acid) +3um (the amount added is usually 5 to 50% of the total composition)
30%); one or more inorganic powders such as kaolin, Merck, bentonite, titanium dioxide, and zinc oxide (the blending amount is usually 0 to 30%); Polymeric substances such as lipten, acrylic resin emulsion, vinyl acetate emulsion, etc. can be blended for the purpose of adjusting moldability, etc.).

The patch composition of the present invention is prepared by mixing the above components in a conventional manner. This patch composition is applied to a support such as paper, woven fabric, non-woven fabric, plastic film, etc., and then applied as needed. Apply 7A coating such as polyethylene film to make a patch.

〔Effect of the invention〕

Since the patch composition of the present invention contains a large amount of water and oil components, it has a higher cooling effect than conventional plasters, and also has improved release of active ingredients from the plaster and transdermal absorption. Are better. Furthermore, although the adhesive patch composition of the present invention contains an oil component, it can be applied to diseased areas and exhibits excellent effects without any oozing of the F oil component or decrease in sagging tackiness due to the action of the oil-based gelling agent.

〔Example〕

Next, the present invention will be described in more detail with reference to Examples.0 Example 1 An F patch composition was prepared in a conventional manner according to the following formulation, and this was applied as a poultice on a nonwoven fabric or lint cloth. death,
A poultice was further coated with an ethylene film.

Example 1 ■? Sodium lyacrylate 4.0 (70 mp SS9 Nippon Pure Chemical Industries ■) ■? Lyacrylic acid 1.5 (Zoyurimer AC-10H, Nippon Cotton Pharmaceutical Co., Ltd.) ■Glycerin
10.0■Medicinal ingredients Glycol salicylate 1. Oj-menthol
1.0■ Octyldodecyl myristate
3.0■? resolvate 80
2.0 ■ Aluminum sulfate
0.5■ Anhydrous light silica 4.0
■Water balance total
The poultice obtained at 100.0% had excellent release properties of the active ingredient, transdermal absorbability, and adhesiveness.

Examples 2 and 3 A patch composition was prepared in a conventional manner according to the formulation shown in Table 1 below, and this was applied as a poultice on a nonwoven fabric or lint cloth, and then... A poultice was prepared by applying a polyethylene film.

The release properties of the active ingredient, transdermal absorption, and adhesiveness of the poultice obtained above were examined below. As a comparative example, nine samples were prepared from Example 2.3 except for octyldodecyl myristate (comparative P1).
1) and Example 2.3 from which anhydrous light silica was removed (Comparative Example 2.3).

Release properties, transdermal absorption properties, and adhesion were measured as follows: Drug holding tank, squalane-treated Nitrocell a
- A diffusion cell device consisting of a gas membrane and a receptacle with a sample collection tube was used.

Fill the container with υnoic acid raw salt buffer. After that, fill each paste into the drug holding tank. and pass through the membrane while stirring the inside of the receiver. The concentration of drug released into the receiver Measured over time.

Transdermal absorption: The abdomens of white rabbits (15 rabbits, 5 in each group) were placed in a separate house, each No9tsuzo drug was applied, and blood was collected over time to measure the drug concentration in the blood.

Adhesion: Measured by JIS tack test method (ball rolling method).

The results are shown in FIG. 1, FIG. 2, and Table 2.

Table 2

[Brief explanation of drawings]

Figure 1 shows the release properties of the active ingredient (glycol salicylate) of the adhesive composition of the present invention, and Figure 2 shows the transdermal absorption of the same active ingredient. Also Tosai Q-1'l! 5 ÷ standard procedural amendment (
Spontaneous) April 1982 138 1. Indication of the case 1988 Patent Application No. 56047 2. Name of the invention Patch composition 3. Relationship with the person making the amendment Applicant's address name (091) Kao Stocks Company 4, agent name (6870) Patent attorney Miko Ariga, -1
1 Address Same as above Koji Ryo. Name (7756) Patent Attorney Toshio Takano'::
l'i・1 Address Same as above 1--2J6
, Column 7 of "Detailed Description of the Invention" of the specification to be amended, contents of the amendment (1) In the specification, page 6, line 12, "dj-kanfurt" toraru is changed to "dl-kanfur, to". correct. (2) Same, page 7, line 3, "5-30%" is corrected to "5-50%."

Claims (1)

[Claims] 1. Contains 1 to 30% by weight of a water-soluble polymeric substance, 2 to 20% by weight of an oil component other than the active ingredient, 30% by weight or more of water, 1 to 15% of an oil-based gelling agent, and an active ingredient. Patch composition.