JPS59130809A - Plaster base for pharmaceutical preparation of adherent application - Google Patents

Abstract

PURPOSE:The titled plaster base capable of keeping a blended drug stably without decomposing it, obtained by adding an oxyanthraquinone compound to rubber-like adherent substance. CONSTITUTION:A plaster base consisting of a rubber-like adherent substance of natural rubber or synthetic rubber or their mixture is blended with an oxyanthraquinone compound such as a compound shown by the formula (R<1> is lower alkyl, hydroxymethyl, or carboxyl; R<2> is H, OH, or lower alkoxy). A natural compound is preferable as the compound shown by the formula, chrysophanol, emodin, rhein, etc. may be cited as it, and plants containing them are used in the form of extracts too. A preferable amount of the compound shown by the formula blended is 0.02-2wt% based on the adherent substance, an amount of plant containing it is 0.02-5wt%, and an amount of plant extract is 0.005- 4wt%. It is especially effective for drugs consisting of phenolic hydrogyl group- containing compounds or amine compounds, which are extremely decomposed with a common plaster base.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a body for adhesive patch preparations and a viscous patch preparation using this plaster. For more details on the length, ``Kibari'' is an adhesive patch preparation made by improving the η-body made of a sticky substance used for sticky preparations and further adding a drug to the improved paste. Regarding.

Conventionally, drugs administered to the integument have been intended to locally act on the integument and its underlying tissues, such as M, fungicides, disinfectants, and skin irritants. However, in recent years, attempts have been made to administer drugs with systemic effects through the skin.
Various drugs have been proposed or attempted to be administered to the skin.

Dermal administration of drugs is carried out, for example, in the form of adhesive preparations in which the drug is mixed into a plaster made of an adhesive substance. When a preparation containing a drug in a plaster 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 shielding them from light. Compounds, amine thread compounds, etc., even when covered with aluminum laminate, the decomposition of drugs continues to progress.
Many items become unusable after being stored for two to three years. In particular, methyl salicylate as an anti-inflammatory analgesic;
Salicylic acid visiting agents such as monoglycol salicylate, skin irritation removers such as cabzaicin, nonyl panillyl amide, and pepper extract, ethanolamine antihistamines such as diphenhydramine, and oral medications such as vitamin E such as dt-α-tocopherol. There is a significant decrease in free content.

Therefore, it is desired to develop a single body or an adhesive patch preparation made of an adhesive substance in which the decomposition of the drug does not proceed even if the drug is mixed therein.

Under these circumstances, the inventors of the present invention have conducted various experiments and have found that if an oxyanthraquinone compound is mixed into a plaster made of a sticky substance made of rubber threads, then one substance can be added to the bone paste. It was discovered that the drug exists stably without decomposition even when the drug is used.

The present invention has been completed based on this new knowledge, and provides a bone patch preparation for adhesive patch B, which is made by blending an oxyanthraquinone compound into a plaster made of a rubber thread adhesive substance.
The present invention relates to an adhesive patch preparation comprising a bone supplement and a drug.

Examples of the rubber thread adhesive material rt include diene thread polymer compounds that have traditionally been 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 aggregate rubber, styrene-butadiene rubber, polygden rubber, polyisoprene rubber,
Butyl rubber, silicone rubber, etc. are included in the plaster made of rubber thread sticky substances, and as third components, viscosity imparting agents such as terpene resins and petroleum resins, liquid paraffin, animal and vegetable oils (for example, , olive oil, soybean oil,
Bonding force/retention force Nu agent such as beef tallow, tonne fat), bolybdenum, lower grade isoprene, wax, titanium oxide, zinc oxide, aluminum mekusilicate, sulfuric acid force! Fillers such as lesium and calcium phosphate, water, emulsifiers (eg, sorbitan monooleate, sodium lauryl sulfonate), emulsifying aids (eg, magnesium stearate, aluminum stearate), and the like may be blended.

The oxyanthraquinone compound used in zero-start IJJ is, for example, one represented by the general formula (wherein R1 represents a lower alkyl group, hydroxymethyl group, or carboxyl group, and R2Vi represents a hydrogen atom, a hydroxyl group, or a lower alkoxy group). Examples include compounds that

In the general formula (1), the lower alkyl group represented by R1 is preferably one having 1 to 4 carbon atoms, such as methyl, ethyl, n-propyl, 1so-propyl, n-butyl, among others methyl, and a lower alkoxy group Toshi is methoxy,
Ethoxy, n-propoxy, 1so-propoxy,
Of those having 1 to 4 carbon atoms such as n-methoxy, methoxy is preferred.

The compound (1) is preferably derived from natural products,
For example, chrysophanol (chrysophanol)
l), emvdin, thei
n), talinphanol anthoron (chrysop
Examples thereof include hanolanLhron), aloe-emodin (alop-emodinl), and emodin-monomethyl-ether.

The oxyanthraquinone compound may be used in the form of a plant containing it or an extract of the plant. Plants containing oxyanthraquinone compounds include the genus Almium (
Rheun), Kisikig (R 1゜Po)
lygonum), and the content is particularly high in the roots and rhizomes of these plants.
lmajum L INNE var tanguti
(:urn h4AX IM (root brocade rhubarb), Rhe
um officiale BQILL (root: Tang rhubarb), Rheum undulatum LINNE
(Japanese rhubarb), Polygonum multiflon
Examples include um 'I" HUNB (how many birds), etc.
These are used as dry powders, especially powders of 100 mesh or less.

As such plant extracts, powders of dried extracts prepared by solvents such as water, alcohols (methanol, ethanol, gropanol), and ritone (acetone, methyl ethyl ketone), especially powders of 100 mesh or less, are used.

The oxyanthraquinone compound is used in a proportion of about 0.001 viw% to 5w/w%, preferably 0.02w/w% to Qw/w%, based on the rubber adhesive substance, and in the case of containing plants, Kij O, About 01w/w%-10w/w%,
Preferably at a ratio of 0.02w/911% to 5w/y.-, and in the case of plant extracts, 0.002w/w% to 8%.
About w/w%, preferably 0.005w/w% to 4W
It is blended at a ratio of about 1/w.

The paste of Reihatsu J can be made into an adhesive patch by adding a drug that can be applied to the skin.

Therefore, the adhesive patch preparation using the back body 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 paste 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 is particularly useful for preparing such drugs.

Examples of compounds containing phenolic hydroxyl groups include salicylic acid derivatives, monoglycol salicylate, methyl salicylate, etc.), vitamin E and its derivatives, and kabsaicin, and examples of amine compounds include ethanolamine antihistamines such as diphenhydramine, and chloride. Ethylenediamine antihistamine drugs such as pheniramine, lidocaine, etc. are available. Other nest-active ingredients include t-menthol, di
= Hot and cold skin irritating drugs such as camphor, thymol, and d-borneol, non-steroidal anti-inflammatory drugs such as indomethacin and cyclo-7-entuc sodium, steroidal anti-inflammatory drugs such as dexamethacin and betamethacin,
Chlorhexidine diglyconate, acrinol and other planericides, chili pepper extract, nonylic acid panillylamide, kabsaicin, ginger extract, cantharis tincture,
Examples include heat-sensitive skin irritating drugs such as cantharidin, and herbal medicines such as shikon and turmeric.

In preparing the adhesive patch preparation of the present invention, it goes without saying that the drug may be added directly to the rubber-based adhesive, and then the oxyanthraquinone compound t-added.

In addition, non-explosion adhesive patch preparations are usually used by being spread on a support such as cloth or plastic film.

The present invention will be explained below in more detail by showing an example and a practical example, but the present invention is not limited thereto.

In addition, in the following description, "Miyako" means [parts by weight].

Example 1 489 styrene-butadiene-styrene rubber and 25 parts of natural rosin are kneaded for 20 minutes in a kneader maintained at 150 DEG C., 8 tons of Emodin are added thereto, mixed, and kneaded for 10 minutes. Next, 25 parts of Poly 1F, 7 parts of liquid paraffin,
Titanium oxide powder 6m.

Five talcums were added and kneaded for 10 minutes to obtain a paste for adhesive patch preparation.

Example 2 5 parts of salicylic acid monoglycol and 0.0 nonylic acid vanillylamide were added to the plaster obtained in Example 1 at 90°C.
2 parts and 0.8 parts of diphenhydramine were added and kneaded for 5 minutes, and the resulting product was spread on cloth to a thickness of 0.2 cm to obtain an adhesive patch preparation.

Example 8 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2 using the same formulation as in Example 1, but using Tang rhubarb instead of emoji.

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 replaced with a mixture of Emodin.

Comparative Example 1 An adhesive patch preparation was obtained in the same manner as in Examples 1 and 2 except that emodin was removed from the formulation in Example 1.

Example Decomposition rate (%) of the drug when the preparations obtained in Example 2.8 and Comparative Example 1 were sealed and stored at 40°C for 8 months in an aluminum-polyester laminate packaging material.
) and the results are shown in Table 1.

Below margin Male Table 1: Drug degradation rate (%)

Claims (2)

[Claims] (1) A viscous adhesive patch comprising a sticky substance made of rubber thread and an oxyanthraquinone compound. (2) The oxyanthraquinone compound has the general formula 1% (wherein R'tj: lower alkyl group, hydroxymethyl group or carboxyl group is represented by 1 (2 represents a hydrogen atom, hydroxyl group or lower alkoxy group)). The plaster according to claim (1), which is a compound comprising: