JPS59134717A - Tacky plaster base - Google Patents

Abstract

PURPOSE:The titled plaster base that is made by adding quercetin, a hydroxycarboxylic acid and tocopherol to a rubber tacky substance, thus keeping the active ingredients stably without their decomposition. CONSTITUTION:Quercetin or an extract from a plant containing the same such as buckwheat extract, a hydroxycarboxylic acid of 10 or less carbon atoms and tocopherol are added to a rubber tacky substance such as natural rubber, synthetic rubber or their mixture. The amount of quercetin is 0.005-2wt%, the hydroxycarboxylic acid, 0.001-0.02wt% and tocopherol, 0.01-2wt%. It is very useful, when the plaster contains, as active ingredients, compounds bearing phenolic hydroxyls such as salicylic acid derivatives and amines such as ethanolamine antihistamics, which are remarkably lowered in their contents in the conventional rubber plaster base.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a plaster for adhesive patch preparations and an adhesive patch preparation into which the plaster is sprayed. More specifically, the present invention relates to an improvement in a plaster made of an adhesive substance used for adhesive patch preparations, and an adhesive patch preparation in which a drug is further blended into the improved paste.

Conventionally, drugs administered to the integument have been intended to locally act on the integument and its underlying components, such as bactericides, disinfectants, and skin irritants. However, attempts have been made to administer drugs that have delayed systemic effects through the skin, and various methods of administering drugs through the skin have been proposed or attempted.

Dermal administration of drugs is carried out, for example, in the form of adhesive patches in which the drug is blended onto a bone body made of an adhesive substance. When stored at fC, the therapeutic effect of the preparation tends to decrease significantly due to decomposition, volatilization, etc. of the drug.

By the way, can volatilization and photodecomposition of drugs be prevented by sealing them with aluminum laminate packaging and shielding them from light?
However, for n'fc drugs, especially compounds containing phenolic hydroxyl groups, amine compounds, etc., that are mixed into adhesive plasters such as those mentioned above, the decomposition of the drug continues to progress even when packaged with aluminum laminate. However, there are many products that become unusable after being stored for two to three years. In particular, the content of salicylic acid derivatives such as methyl salicylate and monoglycol salicylate as anti-inflammatory analgesics, skin irritants such as capsaicin, nonylvanillylamide, and chili pepper extract, and ethanolamine antihistamines such as diphenhydramine decreases in content over time. Therefore, it is desired to develop a plaster or an adhesive patch made of an adhesive substance in which the decomposition of the drug does not proceed even if the drug is added thereto.

Under these circumstances, the present inventors have received various research awards and found that quercetin, oxyacid, and hycopherol are found in rubber-based sticky substances↓lina plaster. It has been found that when used in combination, the drug remains stable without decomposition even if the drug is mixed into the paste.

The present invention has been completed based on this new knowledge, and includes a paste for an adhesive patch preparation comprising a paste made of a rubber-based adhesive substance mixed with quercetin, an oxyacid, and a hydroxyacid. This invention relates to an adhesive patch preparation which is made by combining all the drugs in a paste.

Examples of rubber-based adhesive substances include diene-based polymer compounds that have traditionally been used as plasters for rubber-based adhesive patch preparations, specifically natural rubber, synthetic rubber, and mixtures thereof. ra. Synthetic rubbers include TEHA, styrene-isoprene-styrene block copolymer rubber, styrene-butadiene rubber, polybutene rubber, polyimprene rubber, butyl rubber, and silicone rubber. In addition, as a third component, tackifiers such as terpene resins and petroleum resins, liquid paraffin, animal and vegetable oils (for winter, olive oil, soybean oil, beef tallow, fat), polybutene, lower isoprene, wax, etc. Adhesion/retention force regulator, titanium oxide, zinc oxide,
Fillers such as aluminum metasilicate, calcium sulfate, calcium phosphate, water and emulsifiers (e.g., nrubitan monooleate, sodium lauryl sulfonate, emulsifiers (yc, magnesium stearate,
Aluminum stearate or the like may also be added.

Querceti/ is Querceti 7-containing Its substance-r-
It may also be used in the form of a kiss. Examples of such extracts include Kaika extract and Shichiba extract. Examples of such extracts include aqueous extracts and alcohol (e.g., methanol, ethanol, and globanol extracts).
E7C, the extract is preferably used as a dry powder with a size of 100 mesh or less.The amount of quercetin itself is usually 0.001 to 5% by weight based on the rubber adhesive substance. Kneading degree (preferably 0.005~
(approximately 2% by weight), and in the case of extracts, 0.0% by weight
01-10 weight kneading K (preferably about 0.005 to 2% by weight).

As the oxyacid, an oxycarboxylic acid having carbon and IO or less is usually used. Specific examples of oxyacids include citric acid, malic acid, tartaric acid, nilinlupic acid, azcolhinic acid, and lactic acid.

Oxyacid is usually 0.000% for rubber adhesive substances.
1-0. l w/w%, preferably 0.001 w/
w%-0.02w/w% blended salel.

At least 0.001w/w%, preferably 0.001~
5w/wL especially good case I/'i0.01~2 w/
wfb.

The plaster of the present invention can be formulated into an adhesive patch by incorporating a drug that can be overused into the outer skin. Therefore, the adhesive patch preparation using the plaster according to the present invention is as follows:
What is the effect of the drug being kept stable without being degraded?

There are no particular restrictions on the drug that can be incorporated into the plaster of the present invention, as long as it can be administered through a sticky patch. Examples include drugs for treating skin diseases, drugs for skin irritation, and drugs for treating indefinite complaints. In particular, phenolic hydroxyl group-containing compounds and amine compounds are not included in conventional adhesive plasters.
Since the content in No. 1 is significantly reduced, it is of particular significance when formulating a drug according to the present invention.

Examples of compounds containing phenolic hydroxyl groups include salicylic acid derivatives (monoglycol salicylate, methyl salicylate, etc.) and kabsaicin, and examples of amine compounds include ethanolamine antihistamines such as diphenhydramine, and chlorpheniramine. Examples include ethylenediamine-based antihistamine drugs such as Lidokai 7. Other medicinal ingredients include, for example, 1-menthol, dt-kaffir, thymol, d
- Cold-sensitive skin irritating drugs such as borneol, non-steroidal anti-inflammatory drugs such as ittomedadino, cyclofenac sodium, steroidal anti-inflammatory drugs such as dexamethacin and bekmetazono, sterilization such as talolhexidine diglyconate, acrinol, etc. Examples include warm-sensitive skin irritating drugs such as chili pepper extract, nonylic acid panillylamide, kabsaicin, ginger extract, cattalis tincture, and cantharidino, and crude drugs such as chicon and cantaloupe.

It goes without saying that in preparing the uninvented viscous patch preparation, the drug may be added to the adhesive substance first, and then quercetin, tocopherol, and oxyacid may be added thereto.

Alternatively, the adhesive patch preparation of the present invention is used by being spread on a support such as an oil layer, cloth, or plastic film.

EXAMPLES The present invention will be explained in more detail with reference to Examples and Experimental Examples below, but the invention is not limited thereto.

In addition, in the following description, "to" means "1 part by weight".

Example 1 43 m5 of styrene-butadiene-styrene rubber and 25 parts of natural rosin were mixed in a kneader maintained at 150°C for 20 minutes.
After kneading for 1 minute, 1 m of chlorine, 1 ffl of dt-α-tocopherol, and 1 ml of quench were added and mixed using a fel, and the mixture was kneaded for 100 minutes. Next, 5 parts of Volipden, 7 parts of liquid paraffin, 6 parts of titanium oxide powder, and 5 parts of talc.
Add all parts and knead for io minutes to obtain a paste for adhesive patch preparation.

Example 2 To the paste obtained in Example 1, at 90''C, 5 units of monoglycol salicylate, 5 units of methyl bricylate, 0.02 units of panillylamide nonylate, and 0.8 units of diphenhydramine were added for 5 minutes. The material obtained by kneading is spread on cloth to a thickness of 0.2 aa to obtain an adhesive patch preparation.

Example 3 In the formulation of Example 1, dt-α-tocopherol was replaced with 90% natural vitamin E oil, and citric acid was replaced with malic acid. Obtain a patch preparation.

Comparative Example 1 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2 except that quercetin, dt-α-tocopherol, and citric acid were removed from the formulation of Example 1.

Js bottom margin Table 1 Drug degradation rate (%)

Claims (1)

[Claims] A plaster for adhesive patch preparations comprising a plaster made of a rubber thread adhesive substance mixed with quercetin, oxyacid, and tocopherol.