JPS5925317A - Plaster - Google Patents

Abstract

PURPOSE:To provide a plaster having good touch, color, sticking properties, etc., and excellent drug stability, and capable of maintaining sufficient drug activity for a long period, by coating a carrier with a drug-containing plaster layer containing crystalline calcium sulfate as a filler. CONSTITUTION:A plaster containing a drug, especially easily hydrolyzable salicylic acid ester derivative, d-alpha-tochopherol or its ester, nonylic acid amide, capsaicin, etc. is added with <=70wt%, preferably 0.1-50wt% of crystalline calcium sulfate as a filler, and the mixture is applied to a carrier to obtain the objective plaster. The rate of hydrolysis of the drug can be reduced to <=1/3 compared with the conventional filler (e.g. calcium carbonate), and the present composition exhibits remarkable effect to the stabilization of the drug and the keeping of the drug action.

Description

DETAILED DESCRIPTION OF THE INVENTION The invention relates to a patch that can be applied directly or indirectly to the affected area fik.

Paste 1' rill has "+'J +iJ effect, astringent effect, adhesive property, :,l r(,'2 :;J) g
Aruji ColoriiL'J I;14 81M Effectl
x to'tr purpose (!: L te, 1i.'/ratio 11
1I. Fillers such as il'l, kaolin, nonorsium carbonate, titanium oxide, and talc are generally blended depending on the purpose.

Therefore, if these fillers are added c:L, and the plaster system contains water t↑, the hydrolysis of the drug 1iγ
It also promotes the filling of water-free yarns.
Gold JjJ▲ ions and impurities 2 in R7'lll promote the drug's concentration lθi, and the drug's proboscis decreases for a while! , lJ'l.

Particularly, in the case of banops that contain water in the body, one C is the main d. The content of salicylic acid ester, which is used as a μ product, is significantly reduced due to hydrolysis of yc.

If we try to solve the problem of lowering the lit content without using fillers, it is difficult to adjust the fit, color, and adhesiveness of the poultice, and it is difficult to adjust the properties of the poultice, such as the fit, color, and adhesion. is something that cannot be viewed.

Considering this situation, the inventors of the present invention have made a point of view of the characteristics of a patch and a filled rill that have good fit, color, adhesive properties, etc., but are uncertain about the stability of the drug: '1.1'
．． As a result of 4σ1 B{2, the crystal i'J
．． ．． Sulfur tlin Karshi Ram is a ``Second Age Bh Satisfying Satisfaction - Cheating'' I saw this 22nd in the evening, 11th, and the main issue 1#J
VC has arrived.

The present invention is a patch comprising a drug-containing plaster layer containing a filler, which contains crystals as the filler.
iN? - Paste 1 characterized by using calsulam
・It provides one drug.

The adhesive patch of the present invention has excellent drug stability and maintains sufficient drug efficacy for 1 to 4 days.

+ The paste used for MMK is )ζ
Synthetic resins such as rubbers and/or acrylic copolymers, polyvinyl alkyl ethers, polyvinyl alkyl ethers, etc. (71
This year, terpene resin, rosin resin,
Adhesive resins such as petroleum resins, k jlf17 halafine, polybutene, low molecular weight isoprene, wax 1
．． Adhesive substances may include other additives such as grade 3 fatty acids. Then, as a plaster, add water and an emulsifier (and an emulsifier) to the ingredients selected from the ingredients listed in 111j.
emulsified using O/Vt type or t1: vilo
+, (It is also possible to use a gel formed by gelling an emulsion of 1,!). In this case, the moisture content is 80
It is preferable that the weight h is 1% or less, and the thickness f=J 17 (this is preferable because it imparts a cooling sensation).

The crystalline nonorsium sulfate is a food additive standard product or a Japanese Industrial Standard reagent grade 1 or higher purity product, and 300 menonyu is preferably used. The amount of calsulam in the plaster is less than 70 weights per diameter, preferably 0.1-50 weights!
11. The drug used in the practice of the present invention is not particularly limited, and it is effective to add it in a range of Many drugs are used, including topical drugs, transdermal absorption systemic drugs, drugs for treating skin diseases, skin irritants, and drugs for treating indefinite complaints, but especially salicylic acid ester, -9゛I) thylic acid, which is easily hydrolyzed. Nisder derivatives of salicylic acid such as monoglycols, d-α-1-::77erol or its esters, d6-α-tocopherol or esters of d6-α-tocopherol, nonylic acid amides, cabzaicin,
At least 181i selected from the group of chili pepper extracts
This method is preferable because a good adhesive patch can be obtained using the method.

The adhesive tape of the present invention has seven characteristics: the drug content decreases little due to hydrolysis and maintains good medicinal efficacy over a long period of time.

Examples are shown below. Does it mean the weight part of the sentence? Taste 4.

Example: 5 parts of Inogren rubber and 30 parts of styrene-isoprene-styrene copolymer rubber were masticated for 20 minutes in a 150° C. mold, and 10 parts of crystalline rhusium sulfate was added and mixed. Then, 15 parts of natural rosin are added and mixed.

The system was cooled to 95 c-, polybutene 11.48
1 part H-IC dynamic paraffin, 3 parts methyl salicylate
1 part, 3 parts monoglycol salicylate, tocopherol acetate
Add 0.02 parts of vanillyl-7mide and 2 parts of Norvita/monooleate and mix for 20 minutes, then emulsify while gradually adding 10 ilj of dehydrated water at 50°C. After cooling to
It is spread to a thickness of 8 mm and gelled at room temperature to obtain a patch.

This was packaged with a moisture-impermeable base material laminated with aluminum foil and stored at 40°C for 3 months, after which the amount of the drug degraded by hydrolysis was measured.

The results were as follows: Methyl salicylate: 13.2% Monoglycol salicylate: 163% Tocopheryl acetate: 6.9% Vanillylamide nonylate: 14.4% (each based on the theoretical value of 100%) Calculation) On the other hand, for comparison, when lucium carbonate was added in place of the crystalline calcium/nium sulfate, the amount of drug produced by hydrolysis, NJ&, was as follows.

Methyl salicylate: 40.5% Monoglycol salicylate: 45.8% Tocopherol acetate: 20.5% Nonylic acid vanillylamide: 3 (1.8%) - As is clear from Example F, crystalline trisium sulfate was used as a filler. When using this method, the amount of drug hydrolysis is reduced to about 1/3 or less of the conventional amount, and it has a remarkable effect on maintaining drug stability and drug efficacy.

patent applicant Nitto 1 “Ki Kogyo Co., Ltd.” Representative Sanbe Hijikata

Claims (1)

[Claims] 1) Contains 1 drug. It is a patch having a material-containing granite layer on a carrier, and a filler and L7 crystals (ife).
A patch characterized by not using calcium acid. 2nd - Qi qb was the first to visit Esther (
4C, ester of d-α-I copherol or so, de
-α-tocopherol or its nisdel, nonylic acid amide, 1) π1 when at least 1 selected from 711 of 1) Zozui//, Totsu/l Thirashikis. The adhesive patch according to claim 1.