JPH10158186A - Antiinflammatory analgesic patch - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject patch by percutaneously administering indomethacin and an extracted solution and/or its essence of Iris germancia Lam, exhibiting more excellent analgesic action than separative use of each component. SOLUTION: This patch is obtained by formulating (A) indomethacin with (B) one or more selected from the group consisting of an extracted solution of Iris germancia Lam and its essence. For example, an extract (with water, a mixed solution of water/an alcohol or an alcohol) of rhizome of Iris germancia Lam, a plant of the genus Iris of the family Iridaceae is preferably used as the component A. A patch is formulated with 0.01-5.0wt.% of the component A and 1 pt.wt. of the component A is formulated with 0.001-10 pts.wt. of the component B (calculated as raw crude medicine).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to bruises, sprains, joint pain,
The present invention relates to a patch used for anti-inflammatory analgesia such as stiff shoulders and back pain.

[0002]

2. Description of the Prior Art Indomethacin is a non-steroidal anti-inflammatory analgesic having the chemical name of 1- (p-chlorobenzodiyl) -5-methoxy-2-methylindole-3-acetic acid. Although indomethacin has an excellent anti-inflammatory and analgesic effect, side effects such as gastrointestinal disorders have been observed when administered orally. In order to reduce these side effects, external preparations such as anti-inflammatory analgesic ointment and aqueous cataplasm have been studied. On the other hand, iris root contains an aromatic component and has been used as a raw material of perfume in Europe and the like.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to develop an anti-inflammatory analgesic external preparation having sufficient efficacy.

[0004]

Means for Solving the Problems As a result of intense research, the present inventors have found that if indomethacin and iris root extract and / or its extract are transdermally administered in combination, each of them is more effective than using each alone. The present inventors have found that they exhibit an excellent analgesic effect, and have completed the present invention. That is, the present invention provides (a)
An anti-inflammatory analgesic patch comprising one or two selected from the group consisting of indomethacin and (b) iris root extract and extract thereof.

[0005] In the present invention, the iris root is an iris (Iri
daceae) Purple iris, a plant of the genus Iris
(I.germancia Lam.), Smelt Iris (I.florentia L.),
And the extract from the rhizome of Ivory iris (I. pallida L.) or other congener plants (water, a mixture of water and alcohol,
(Alcohol) or an extract (dry extract or soft extract) produced using the extract thereof.
Indomethacin is preferably incorporated in the patch in an amount of 0.01 to 5.0% by weight, and more preferably 0.2 to 2.0% by weight. The mixing ratio of the iris root extract or extract used is 0.001 to 10 parts by weight based on 1 part by weight of indomethacin in terms of a crude drug. If the amount of the iris root extract is more than 10 parts by weight, coloring of the preparation and skin irritation occur, which is not preferable. Also, 0.00
If the amount is less than 1 part by weight, no effective action is observed, which is not desirable.

In the anti-inflammatory analgesic patch of the present invention, an adhesive, a filler, a plasticizer, a humectant, an excipient, a surfactant, a preservative, a solubilizer, an absorption enhancer, a crosslinking agent, a pH adjuster ,
Components normally used as external preparations, such as stabilizers, can be blended within a range that does not impair the effects of the present invention.

Examples of the adhesive include water-soluble polymer compounds such as polyacrylic acid, sodium polyacrylate, gelatin, gum arabic, polyvinyl alcohol, polyvinyl pyrrolidone, sodium carboxymethyl cellulose, carboxyvinyl polymer, hydroxymethyl cellulose, sodium alginate, xanthan gum and the like. , Natural rubber, hydrogenated rosin, SBR (styrene butadiene rubber),
SIS (styrene isoprene block copolymer rubber) Synthetic rubbers such as polyisobutylene rubber and polyisoprene rubber, acrylic pressure-sensitive adhesives such as acrylic acid ester and methacrylic acid ester, and silicone pressure-sensitive adhesives such as silicone rubber and resin can be used.

[0008] Examples of the filler include silicic anhydride, titanium oxide, aluminum silicate, zinc oxide and kaolin. As the plasticizer, fatty acids such as myristic acid, lauric acid and oleic acid, fatty acid esters such as isopropyl myristate, diisopropyl adipate and diethyl sebacate, lanolin, liquid paraffin, polybutylene and the like are used. As a cross-linking agent, aluminum hydroxide, aluminum glycinate, dihydroxyaluminum acetate, magnesium aluminate silicate, or the like is used.

As humectants, glycerin, propylene glycol, butylene glycol, macrogol, sorbitol, sodium lactate and the like are used. As the excipient, kaolin, bentonite, zinc oxide, titanium oxide, silicic anhydride and the like are used. As a surfactant,
Polyoxyethylene sorbitan fatty acid ester (for example, polysorbate 80, polysorbate 60, etc.), polyoxyethylene hydrogenated castor oil, polyoxyethylene glycerin fatty acid ester, polyoxyethylene glycol fatty acid ester, polyoxyethylene polyoxypropyl alkyl ether, polyoxyethylene glycol Ether, sorbitan fatty acid ester, glycerin fatty acid ester and the like can be mentioned.

Examples of the preservative include paraoxybenzoic acid esters (for example, methyl paraoxybenzoate). Examples of the pH adjuster include citric acid, malic acid, tartaric acid, lactic acid and the like. As stabilizers, dibutylhydroxytoluene (BHT), butylhydroxyanisole, disodium ethylenediaminetetraacetate (ED
TA-2Na), sodium sulfite, and the like.

Further, in addition to the above components, salicylic esters such as methyl salicylate and glycol salicylate;
Capsicum powder, capsicum extract, vanillyl amide nonylate, camphor, menthol, peppermint oil, tocopherol acetate, azulene, glycyrrhetinic acid and the like as various adjuvants can be blended.

[0012]

According to the anti-inflammatory analgesic patch obtained by the present invention, a patch having an excellent analgesic effect on the target diseases such as bruise, sprain, muscle pain, stiff shoulder and low back pain can be provided.

[0013]

The following examples, comparative examples and test examples are given.
The present invention will be described in more detail. Example 1 After adding 0.5 parts by weight of silicic anhydride to 6.0 parts by weight of polyacrylic acid and 5.0 parts by weight of sodium polyacrylate, 7.0 parts by weight of propylene glycol was added and dispersed uniformly. Then, 0.03 parts by weight of EDTA-2Na was added to 65 parts by weight of purified water previously dissolved, and uniformly dissolved.
After heating and dissolving 0.3 parts by weight of polyoxyethylene sorbitan monostearate, 2.0 parts by weight of iris root extract, 1.0 parts by weight of indomethacin, and 0.3 parts by weight of aluminum glycinate are uniformly dispersed. Was added and mixed uniformly to obtain a patch. After applying this plaster to the nonwoven fabric to a uniform thickness, the liner is attached and cut,
It was a patch.

Example 2 30.0 parts by weight of natural rubber, 30.0 parts by weight of polyisobutylene, 10.0 parts by weight of polybutylene, 6.0 parts by weight of titanium oxide, 35.0 parts by weight of hydrogenated rosin, lanolin 4 0.0 parts by weight were uniformly mixed. Separately, B
After heat dissolving 3.0 parts by weight of HT, Iris root extract 8.
A solution in which 5 parts by weight and indomethacin 8.5 parts by weight were uniformly dispersed was added and mixed to obtain a plaster. After this plaster was applied to a cloth to a uniform thickness, a liner was attached and cut to obtain a plaster.

Comparative Example 1 A patch was prepared in the same manner as in Example 1 except that the iris root extract was omitted from the formulation of Example 1. (Comparative Example 2) A patch was produced in the same manner as in Example 1 except that indomethacin was omitted from the formulation of Example 1. Comparative Example 3 A plaster was produced in the same manner as in Example 2 except that the iris root extract was omitted from the formulation of Example 2. Tables 1 and 2 show the formulations of the preparations produced in these Examples and Comparative Examples.
Shown in

[0016]

[Table 1]

[0017]

[Table 2]

(Test Example) A pressure stimulation test was performed on the preparations produced in Examples and Comparative Examples, and the analgesic action of the preparations was examined.
The test method was as follows: 1 male Wister rat (120-150 g)
It was used as a group of 6 animals. 0.1 ml of a 20% yeast suspension was subcutaneously administered to the rat's left hind footpad. The headache threshold was measured using an analgesy meter (manufactured by Ugo basile) before and 3 hours after the injection of the proinflammatory agent, using the postcard-like reaction as an index. Grouping was performed so that the pain threshold at this time was substantially the same between the groups. Immediately after grouping, 2.5cm x 3.5
The test substance previously cut into cm was administered, and fixed with an elastic bandage. The pain threshold was measured 3, 5 hours after the administration of the test substance. From the pain threshold value after injection of the proinflammatory drug, the rate of increase of the pain threshold value was determined by the following calculation method.

[0019]

(Equation 1)

The results are shown in Tables 3 and 4.

[0021]

[Table 3]

[0022]

[Table 4]

Claims (1)

[Claims] 1. An anti-inflammatory analgesic patch comprising (a) indomethacin and (b) one or two selected from the group consisting of an iris root extract and an extract thereof.