JPS6254402B2 - - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a paste for adhesive patch preparations and an adhesive patch preparation using this paste. 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. Traditionally, drugs administered to the integument include bactericides, disinfectants,
The purpose was to locally act on the outer skin and underlying tissues of skin irritants and the like. However, in recent years, attempts have been made to administer drugs that have systemic effects through the dermis, and cutaneous administration of various drugs has been proposed or attempted. Dermal administration of drugs is carried out, for example, in the form of an adhesive patch containing the drug in a plaster made of an adhesive substance. When a preparation containing a drug in a paste is stored for a long period of time, the therapeutic effect of the preparation tends to decrease significantly due to decomposition and volatilization of the drug. By the way, volatilization and photodecomposition of drugs can be prevented by sealing them with aluminum laminate packaging and blocking light, but drugs that are mixed in a plaster made of a rubber-based sticky substance, especially phenol For compounds containing hydroxyl groups, amine compounds, etc., drug decomposition continues to progress even in aluminum laminated packaging, resulting in 2 to 3
Many items become unusable after years of storage. In particular, salicylic acid derivatives such as methyl salicylate and monoglycol salicylate as anti-inflammatory analgesics, capsaicin, nonylvanillylamide,
Skin irritants such as capsicum extract, ethanolamine antihistamines such as diphenhydramine,
The content of vitamin E such as dl-α-tocopherol decreases significantly over time. Therefore, it is desired to develop a plaster or an adhesive patch made of an adhesive substance that does not allow the decomposition of the drug to proceed even when the drug is mixed therein. Under these circumstances, the present inventors have conducted various studies and found that if an oxyanthraquinone compound is blended into a plaster made of a rubber-based adhesive substance, even if a drug is added to the plaster, the drug will not be released. It was discovered that it exists stably without decomposition. The present invention has been completed based on this new knowledge, and includes a paste for an adhesive patch preparation made by blending an oxyanthraquinone compound into a paste made of a rubber-based adhesive substance, and a paste further containing a drug. This invention relates to an adhesive patch preparation. Examples of rubber-based adhesive substances include diene-based polymer compounds conventionally used as plasters for rubber-based adhesive patch preparations, specifically natural rubber, synthetic rubber, and mixtures thereof. Examples of synthetic rubber include styrene-isoprene-styrene block copolymer rubber, styrene-butadiene rubber,
Examples include polybutene rubber, polyisoprene rubber, butyl rubber, and silicone rubber. The paste made of a rubber-based adhesive substance further contains tackifiers such as terpene-based resins and petroleum-based resins, liquid paraffin, and animal and vegetable oils (for example, olive oil, soybean oil, beef oil, and tonne fat) as third components. , polybutene, lower isoprene, wax and other adhesive/retention force regulators, titanium oxide, zinc oxide, aluminum metasilicate, calcium sulfate, calcium phosphate and other fillers, water and emulsifiers (e.g. sorbitan monooleate, lauryl sulfonic acid) (sodium), emulsification aids (for example, magnesium stearate, aluminum stearate), etc. may be added. As the oxyanthraquinone compound used in the present invention, for example, the general formula (In the formula, R ¹ is a lower alkyl group, hydroxymethyl group or carboxyl group, R ² is a hydrogen atom,
Indicates a hydroxyl group or a lower alkoxy group. ) can be mentioned. In the general formula, the lower alkyl group represented by R ¹ is methyl, ethyl, n-propyl,
1-4 carbon atoms such as iso-propyl and n-butyl
Among them, methyl is preferred, and as the lower alkoxy group, methoxy is preferred among those having 1 to 4 carbon atoms such as methoxy, ethoxy, n-propoxy, iso-propoxy, and n-butoxy. The compounds are preferably derived from natural products, such as chrysophanol, emodin, rhein, chrysophanol anthron, and aloe emodin.
-emodin), emodin-monomethyl-ether, and the like. The oxyanthraquinone compound may be used in the form of a plant containing it or an extract of the plant. Examples of plants that contain oxyanthraquinone compounds include Rheum, Rumx, and Polygonum, and the roots and rhizomes of these plants contain particularly high amounts, and representative plants include Pheum palmatum LINNE. var
tanguticum MAXIM (root brocade rhubarb), Rheum
officinale BQILL (Tang rhubarb), Rheum
undulatum LINNE (Japanese rhubarb), Polygonum
multiflonum THUNB, etc., and these are used as dry powders, especially powders of less than 100 mesh. As such plant extracts, powders of dried extracts prepared with solvents such as water, alcohols (methanol, ethanol, propanol), ketones (acetone, methyl ethyl ketone), etc. are used, especially powders of 100 mesh or less. The oxyanthraquinone compound is used at a rate of about 0.001w/w% to 5w/w%, preferably 0.02w/w% to 2w/w%, and 0.01w/w% in the case of plants containing the oxyanthraquinone compound. w%~10w/w%,
Preferably at a rate of 0.02w/w% to 5w/w%, and in the case of plant extracts, 0.002w/w% to 8w/w
%, preferably 0.005w/w% to 4w/w%. The plaster of the present invention can be formulated into an adhesive patch preparation by incorporating a drug that can be applied to the outer skin. Therefore, the adhesive patch preparation using the plaster according to the present invention has the effect that the drug blended therein is kept stable without being decomposed. 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 in the form of an adhesive patch. Examples include drugs for treating skin diseases, drugs for skin irritation, and drugs for treating indefinite complaints. In particular, the content of phenolic hydroxyl group-containing compounds, amine compounds, etc. is significantly reduced in plasters made of conventional adhesive substances, so the plaster of the present invention has particular significance when formulating such drugs.
Examples of compounds containing phenolic hydroxyl groups include salicylic acid derivatives (monoglycol salicylate, methyl salicylate, etc.), vitamin E and its derivatives, capsaicin, and examples of amine compounds include ethanolamine antihistamines such as diphenhydramine. drugs, ethylenediamine antihistamines such as chlorpheniramine, and lidocaine. Other medicinal ingredients include l-menthol, dl
- Cold-sensitive skin irritating drugs such as camphor, thymol, d-borneol, non-steroidal anti-inflammatory drugs such as indomethacin, cyclofenac sodium, steroidal anti-inflammatory drugs such as dexamethasone, betamethasone, chlorhexidine diglyconate, Examples include bactericides such as acrinol, heat-sensitive skin irritating drugs such as chili pepper extract, nonylic acid vanillylamide, capsaicin, canthari extract, cantharis tincture, cantharidin, and herbal medicines such as chicon and cantaloupe. In preparing the adhesive patch preparation of the present invention, it goes without saying that the oxyanthraquinone compound may be added after first adding the drug to the rubber adhesive substance. The adhesive patch preparation of the present invention is usually used by being spread on a support such as cloth or plastic film. EXAMPLES The present invention will be explained in more detail by showing Examples and Experimental Examples below, but the present invention is not limited thereto. In the following description, "parts" means "parts by weight." Example 1 43 parts of styrene-butadiene-styrene rubber and 25 parts of natural rosin were mixed in a kneader maintained at 150°C.
Knead for 20 minutes, add 3 parts of Emodin, mix and knead for 10 minutes. Next, 5 parts of polybdenum, 7 parts of liquid paraffin, 6 parts of titanium oxide powder, and 5 parts of talc are added and kneaded for 10 minutes to obtain a paste for an adhesive patch preparation. Example 2 5 parts of monoglycol salicylate, 0.02 part of vanillyl nonylate acid, and 0.8 part of diphenhydramine were further added to the paste obtained in Example 1 at 90°C, and the mixture was kneaded for 5 minutes. The material is spread on cloth to a thickness of 0.2 mm to obtain an adhesive patch preparation. Example 3 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2, except that Tang rhubarb was added in place of emoji in the formulation of Example 1. Example 4 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2, using the same formulation as in Example 1, except that Emodin was mixed with a mixture of Isshu Tori instead of Emodin. Comparative Example 1 Emodin was removed from the formulation of Example 1, and Example 1
An adhesive patch preparation is obtained by a method similar to 2. Experimental Example 1 The drug decomposition rate (%) when the preparations obtained in Examples 2, 3 and Comparative Example 1 were stored at 40°C for 3 months in light-shielded and sealed packaging with aluminum-polyester laminate packaging material. The results are shown in Table 1. 【table】

Claims (1)

[Scope of Claims] 1. A plaster for an adhesive patch preparation, which is made of a rubber-based adhesive substance and blended with an oxyanthraquinone compound. 2 The oxyanthraquinone compound has the general formula (In the formula, R ¹ is a lower alkyl group, hydroxymethyl group or carboxyl group, R ² is a hydrogen atom,
Indicates a hydroxyl group or a lower alkoxy group. ) The paste according to claim 1, which is a compound represented by: