JPS5936611A - Adhesive application pharmaceutical - Google Patents

Abstract

PURPOSE:An adhesive application pharmaceutical, prepared by incorporating a rubber type adhesive material with a drug active constituent and a flavonoid, and having improved stability of the drug active constituent. CONSTITUTION:An adhesive application pharmaceutical prepared by incorporating a rubber type adhesive material, e.g. a natural rubber, synthetic rubber or a mixture thereof and further the third constituent, e.g. a tackifier or an adhesion and holding powder adjusting agent, etc., a drug active constituent and a flavonoid, e.g. preferably quercetin, gossypetin or herbacetin, or an extract obtained from a plant containing the flavonoid, e.g. an extract of Sophora japonica L. or buckwheat flour extract. The amount of the flavonoid to be incorporated is about 0.002-5% based on the weight of the adhesive material, and that of the plant extract is about 0.005-3%. A compound containing a phenolic hydroxyl group, e.g. salicylic acid derivative, or an amine type compound, e.g. ethylenediamine type antihistaminic agent, used as the drug active constituent is particularly effective.

Description

[Detailed description of the invention] The present invention relates to adhesive patch preparations.

Conventionally, medicinal ingredients administered to the integument have been intended to act locally on the integument and its underlying tissues, such as sterilization, disinfection, and analgesia. However, in recent years, attempts have been made to administer medicinal ingredients that have systemic effects to the skin, and the administration of various medicinal ingredients to the skin has been proposed or attempted. The administration of such medicinal ingredients to the skin is usually carried out by converting them into adhesive patch preparations, but if the medicinal ingredients are blended into a rubber-based adhesive and stored for a long period of time, the medicinal ingredients may volatilize or decompose. For example, the therapeutic effect of the preparation tends to be significantly reduced.

By the way, volatilization and photodecomposition of medicinal ingredients can be prevented by sealing them with aluminum laminate packaging and shielding them from light. Even with such aluminum laminated packaging, the decomposition of drugs continues to progress, resulting in 2 to 8
Many items become unusable after years of storage.

Therefore, it is desired to develop an adhesive patch preparation that is stable even when a medicinal ingredient, especially a phenolic hydroxyl group-containing compound, or an amine compound is blended with a rubber-based adhesive substance.

Under these circumstances, the present inventors have conducted repeated research to develop a rubber-based adhesive patch with excellent stability of the medicinal ingredient. The present invention was completed based on the discovery that the performance of the present invention can be increased.

That is, the present invention relates to an adhesive patch preparation comprising a rubber adhesive substance, at least one selected from flavonoids and flavonoid-containing plant extracts, and medicinal ingredients.

Examples of the flavonoids used in the present invention include rutin, quercetin, gosipetin, taxifolin,
fervacetin, luteolin, (c) shrimp catechin, (
c) epigallocatechin, (c) shrimp catechin gallate,
(c) Epigallocatechin gallate, etc. are listed, and particularly preferred ones include quercetin, gosipetin,
I can give you fervacetin.

Flavonoid-containing plant extracts include water, alcohol (methanol,
Preferred examples include aqueous extracts of flower buds and buckwheat flour, alcoholic (for example, methanol and ethanol) extracts, and Asenyaku.

The amount of flavonoid blended varies depending on the flavonoid, the type of plant containing it, medicinal ingredients, etc., but is approximately 0.002% to 5% based on the weight of the rubber-based sticky substance described below.
That's about it. Specifically, it is preferable to mix rutin and the like in an amount of about 20%, and 0.1% of gositupetin and the like exhibits a sufficient stabilizing effect.

The amount of flavonoid-containing plant extracts depends on the type of plant,
Although it varies depending on the extraction solvent, medicinal ingredients, etc., the dry matter of the extract is approximately 0.005% to 3% based on the weight of the rubber-based adhesive substance described below. Specifically, it is about 0.5-2% in the case of dried aqueous flower extract, and about 0.05-0.4% in the case of Asenyaku, which has sufficient stabilizing effect. show.

In the case of the above-mentioned blending amounts of flavonoids and flavonoid-containing plant extracts, sufficient stabilization of the medicinal ingredients is achieved and the adhesive properties of the rubber-based adhesive substance are not impaired.

Regarding the present invention, the rubber-based adhesive substance may be one that is generally used as a paste for adhesive patch preparations, such as natural rubber-based, synthetic rubber-based, mixtures thereof, and furthermore, rubber-based adhesive substances containing a third component. Examples include things that have been added.

Examples of the synthetic rubber include styrene-isoprene-styrene block copolymer rubber, styrene-butadiene rubber, polybutene rubber, polyisoprene rubber, butyl rubber, and silicone rubber. The above-mentioned third components include tackifiers such as terpene resins and petroleum resins, halafine sulfur, animal and vegetable oils (e.g. olive oil, soybean oil, beef tallow, and tonne fat), polybdenum, lower isoprene, and adhesives such as waxes.・Retention force adjusting agent, titanium oxide, zinc oxide,
Fillers such as aluminum metasilicate, calcium sulfate, calcium phosphate, water and emulsifiers (e.g. sorbitan monooleate, sodium lauryl sulfonate), emulsifiers (e.g. magnesium stearate,
aluminum stearate), etc.

There are no limitations, such as transdermal absorbable drugs (however, they may be transdermally absorbed with the aid of a drug transdermal absorption aid, and may be local or systemic drugs)
, drugs for treating skin diseases, drugs for skin irritation, drugs for treating indefinite complaints, etc. In particular, the content of phenolic hydroxyl group-containing compounds and amine compounds decreases markedly over time in rubber adhesive substances, so the present invention has particular significance when such unstable compounds are used as medicinal ingredients. . Examples of phenolic hydroxyl group-containing compounds include salicylic acid derivatives (monoglycol salicylate, methyl salicylate, etc.), vitamin E and its derivatives, kabsiren, etc., and amine compounds include diphenhydramicropheniramine and the like. Examples include ethylenediamine-based antihistamine drugs. Other drug components include, for example, dt-camphor,
Cold skin irritation drugs such as thymol and d-borneol, non-steroidal anti-inflammatory drugs such as indomethacin and cyclofenac sodium, steroidal anti-inflammatory drugs such as dexamethacin and betamethacin, hexicine diglyconate, acrinol, etc. bactericidal agents, hot-sensitive skin irritating drugs such as hot pepper extract, nonylic acid vanillylamide, ginger extract, cantharis tincture, and cantharidin.

Example I Phase A Isoprene rubber 50.7% Phase B Gossippetin 0.8% Phase C Natural rosin 33.0%
After masticating at °C for 20 minutes, after cooling to 120 °C, phase B was added and kneaded for 10 minutes. After further kneading, add Phase C, knead for 10 minutes, cool to 80°C, add Phase D, and knead for 5 minutes to obtain the desired adhesive patch preparation. Example 2 Implementation An adhesive patch preparation was obtained in which Phase B in Example 1 was changed to Asenyaku.

Comparative Example 1 An adhesive patch preparation was obtained from the formulation of Example 1, with Phase B removed.

Example The preparations obtained in the above Examples and Comparative Examples were incubated at 40°C for 3 hours.
The results of investigating the residual rate of the drug after storage for several months were
Shown in the table.

(Margin below) Table 1: Residual rate (%) of each drug Patent applicant: Nitto Electric Industry Co., Ltd. Representative Patent Attorney Takashima -

Claims (1)

[Scope of Claims] (1) An adhesive patch preparation comprising a com-based adhesive substance, at least one selected from the group of flavonoids and flavonoid-containing plant extracts, and medicinal ingredients. (2) The flavonoid is at least one selected from the group of rutin, quercetin, gosipetin, taxifolin, fervacetin, luteolin, H shrimp catechin, (c) epigallocatechin, (c) shrimp catechin gallate, and (c) epigallocatechin gallate. An adhesive patch preparation according to claim (1). The adhesive patch preparation according to claim (1), which is also a type of adhesive preparation. (4) The adhesive patch preparation according to claim 1, (2) or (8), wherein the medicinal ingredient is a phenolic hydroxyl group-containing compound. (6) The adhesive patch preparation according to claim (4), wherein the phenolic hydroxyl group-containing compound is at least one selected from salicylic acid and its derivatives, kabsaicin and its derivatives, and vitamin F and its derivatives. (6) The adhesive patch preparation according to claim 111, (2) or (8), wherein the medicinal ingredient is an amine compound. (7) Claim No. 6, wherein the amine compound is at least one selected from ethanolamine-based antihistamine drugs and ethylenediamine-based antihistamine drugs.
) Adhesive patch preparations described in item ).