JPS6256129B2 - - 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 improved plaster made of a rubber-based adhesive substance used for adhesive patch preparations, and to an adhesive patch preparation made by further incorporating a drug 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 adhesive patch preparations in which the drug is mixed into a plaster made of an adhesive substance. When stored, the therapeutic effect of the preparation tends to decrease significantly due to decomposition, volatilization, etc. of the drug. By the way, volatilization and photodecomposition of drugs can be prevented by sealing them with aluminum laminate packaging and shielding them from light. In the case of hydroxyl group-containing compounds, amine compounds, etc., drug decomposition continues to progress even when packaged in aluminum laminate, and many become unusable after being stored for 2 to 3 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, etc. over time. The decline seems to be significant. Therefore, a paste made of a rubber-based adhesive substance that does not allow the decomposition of the drug to proceed even if it is mixed with the drug, or
Development of adhesive patch preparations is desired. Under these circumstances, the present inventors have conducted various studies and found that if an apomorphine group alkaloid 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 absorbed. 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 apomorphine group alkaloid 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 resins and petroleum resins, liquid paraffin, animal and vegetable oils (for example, olive oil, soybean oil, beef tallow, and tonne fat) as third components, as well as polybutene. , lower isoprene, adhesion/retention force regulators such as wax, fillers such as titanium oxide, zinc oxide, aluminum metasilicate, calcium sulfate, calcium phosphate, water and emulsifiers (e.g. sorbitan monooleate, sodium lauryl sulfonate). , emulsifying aids (for example, magnesium stearate, aluminum stearate), etc. may be blended. The apomorphine group alkaloid used in the present invention has the following basic bone core, A specific example is Magnoflorin (Magno-
florine, Ushinsunine, Liriodenine, Michelalbine, Artabotrine, Anolobine, Bulbocapnine, Corytuberine, Domesticine, Dicentrine, etc. It will be done. The alkaloid is in the form of a plant containing it, or in the form of a solvent such as alcohol (methanol, ethanol, propanol, etc.), ketone (acetone, methyl ethyl ketone, etc.), ether (ethyl ether, petroleum ether, etc.), benzene, toluene, etc. from the plant. It may be used in the form of an extract (dry extract or soft extract). As plants containing apomorphine group alkaloids,
Examples include Magnolia magnolia, Kouboku, Annona reishi, Yabuengosaku, Corydalis, Nandina, and Dicentra. The amount of apomorphine group alkaloid blended is usually 0.001 to 3% by weight based on the rubber adhesive substance.
(preferably about 0.01 to 2% by weight),
In the case of containing plants, their dry powder (particularly 100%
In the case of extracts, it is about 0.01 to 20% by weight (preferably about 0.05 to 3% by weight), and in the case of extracts, it is about 0.002 to 5% by weight (preferably 0.05% by weight).
~2% by weight). 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, since the content of phenolic hydroxyl group-containing compounds, amine compounds, etc. in plasters made of rubber-based adhesive substances is significantly reduced, the plaster of the present invention is particularly useful 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 drug may be added to the adhesive substance first, and then the apomorphine group alkaloid may be added. 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 0.5 part of Magnoflorin, 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 adhesive patch preparation. Example 2 In addition to the paste obtained in Example 1, 5 parts of monoglycol salicylate and vanillylamide nonylate were added.
Add 0.02 parts of diphenhydramine and 0.8 parts of diphenhydramine and knead for 5 minutes.
It is spread to a thickness of mm to obtain an adhesive patch preparation. Example 3 In the formulation of Example 1, magnoflorin 0.5
An adhesive patch preparation was obtained by the same method as in Examples 1 and 2, except that 2 parts of Koboku extract (manufactured by ethanol) was added instead of 1 part. Example 4 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2, except that 3 parts of Koboku powder was used instead of 2 parts of Koboku extract in the formulation of Example 3. Comparative Example 1 Using the formulation of Example 1 from which magnoflorin was removed, an adhesive patch preparation was obtained by a method similar to Examples 1 and 2. Experimental Example 1 The drug decomposition rate (%) was determined when the formulations obtained in Examples 2, 3 and Comparative Example 1 were sealed and packaged in an aluminum-polyester laminate packaging material and stored at 40°C for 3 months. The results are shown in Table 1. 【table】

Claims (1)

[Claims] 1. A paste for adhesive patch preparations, which is made of a paste made of an adhesive substance and mixed with an apomorphine group alkaloid.