JPS6351330A - External plaster containing steroidal agent - Google Patents

Abstract

PURPOSE:To obtain the titled plaster having improved side effect such as dermatic inflammation, etc., by adding a specific steroid agent to a pressure-sensitive adhesive gel substrate containing a water-soluble polymer, water and a water- retaining agent as essential components. CONSTITUTION:The objective external plaster is produced by compounding (A) a pressure-sensitive adhesive gel substrate containing a water-soluble polymer (e.g. gelatin, agar, arginic acid, etc.), water and a water-retaining agent (e.g. polyethylene glycol, glycerol, sorbitol, etc.) as essential components with (B) steroid agent such as fluocinolone acetonide, triamcinolone acetonide, etc. The plaster can be applied continuously without causing the dermatic inflammation, damage of diseased part in peeling and delamination of cuticle, etc., in contrast with a tape agent applied to aczema, urticaria, infantile strophulus, etc. Furthermore, the plaster is expected to have the effect of occlusive dressing technique and gives improved remedying effect by the increase of the absorption of the steroid agent used as a main component.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to an external patch containing a steroid agent. More specifically, a flexible support is prepared by blending a steroid agent for treating skin diseases (excluding debrodonbrobionate) into an adhesive gel base whose essential components are a water-soluble polymer, water, and a water-retaining agent. The present invention relates to a steroid-containing patch for administering the contained steroid to the skin and treating the skin by applying the preparation directly to a skin disease area.

Conventional technology Conventionally, oral preparations containing herbal medicines such as cortisone have been used to treat allergic skin diseases such as eczema, hives, infantile strophulus, erythema exfoliation, Hechenotism 1ffin, digital palmar dermatitis, and psoriasis. Injections and external preparations are used.

However, these preparations have some side effects and are inconvenient to use.For example, oral preparations pose a risk of forgetting to take doses or overdosing, while injection preparations cause great pain and stress during administration, and may be difficult for individuals to administer. Difficult to administer. With external preparations such as ointments and lotions, it is difficult to administer a fixed amount to clothing, as well as to θ dyes. In addition, many cases of skin phlegm are accompanied by a similar feeling, so it is possible that you have an urge to give physical stimulation, and this stimulation may worsen the symptoms. That's a childish thing to say. In order to improve the above-mentioned drawbacks, a pressure-sensitive sheet made of Daigong rubber or an acrylic ester-acrylic acid copolymer has been developed. A tape preparation containing a steroid agent as a premedication has been developed. These tapes have many advantages over conventional topical preparations, such as the effectiveness of the hermetically sealed package that can be applied to a small and distorted area, as well as superior workability during treatment. . However, when these tapes are applied to the affected area, it is not uncommon for contact dermatitis caused by the adhesive itself, folliculitis caused by bacteria on the skin surface, and skin inflammation due to stimulation of sweat glands to occur. In addition, these tape agents are
It must be said that it is still unsatisfactory, as it is not only difficult to apply continuously due to damage to the affected area and exfoliation of the dead skin during peeling, but also worsens the symptoms.

Purpose of the Invention Therefore, in order to improve the drawbacks of these tape preparations, the present inventors have conducted extensive research and have found that the present inventors have added herbal drug ingredients to an adhesive base containing a water-soluble polymer, water, and a water-retaining agent as essential ingredients. By incorporating a steroid agent (excluding debrodone propionate) as a base and spreading and coating this base on a flexible support, an excellent patch without the drawbacks of conventional tapes can be obtained. This discovery led to the completion of the present invention. That is, the present invention contains a water-soluble polymer, water, and a water-retaining agent as essential ingredients, and a steroid agent (
The present invention provides an external patch containing a combination of debrodone propionate (excluding debrodone propionate).

+l14 Aspects and Effects of the Invention Water-soluble polymers used in the topical patch of the present invention include gelatin, agar, alginic acid, mannan, carboxymethyl cellulose, medyl cellulose, polyvinyl alcohol, polyacrylic acid, and gum arabic. etc. are mentioned,
In addition, metal salts of these and materials crosslinked with organic or inorganic crosslinking agents are used. These water-soluble polymers may be used singly or in combination of two or more depending on the physical properties of other raw materials used in the present adhesive gel base, and the blending amount in the present gel base may range from 0.1 to 30 w/w%, preferably 0.5 to +5 w/w%.

Next, examples of water retention agents include polyhydric alcohols such as polyethylene glycol, glycerin, sorbitol, marditol, propylene glycol, and 1,3-butanediol, which may be used alone or in combination of two or more. The blending amount is 5 to 60 w/w%, preferably IO to 5Ow/w%. In addition, starch-acrylonitrile graft, starch-acrylic acid graft, starch-styrene sulfonic acid graft, starch-vinyl sulfonic acid graft, cellulose-acrylonitrile graft, cellulose-styrene sulfonic acid graft, carboxydimethyl cellulose cross-linked It is possible to use super water-absorbing polymers such as polyhinyl alcohol crosslinked products, saponified acrylic acid-hinyl acetate products, polyacrylate crosslinked products, saponified polyacrylonitrile polymers, and polyethylene glycol diacrylate crosslinked products, In these cases, the content is 0.01-10.0 w/w%, preferably 0.05-7. It should be used within the range of Ow/w%.

The adhesive gel base used in the present invention is characterized by containing water, which improves the absorption of the active ingredient, the steroid. Its moisture content is lO~70w/w%, preferably 20~50w
/w%.

Next is the herbal medicine ingredient of this topical patch. Examples of steroids include fluoromelonatonide, triamnolone acetonide, dexamethasone, medilbrednisolone, bredonisoline, hydrocordesin, valamethacin, betamethacin, betamethacin sodium phosphate, dexamethacin acetate, cortisone acetate, and acetic acid. Hydrocortisone, medylprednisolone acetate, clobetasol propionate, hydrocortisone butyrate, fluocinonite, fluorometholone, fludroquincortide, flumethacin pivalate 1. Examples include beclomethasone propionate, betamethacin valerate, methylbredonin acetate, and the amount of these steroids in the adhesive gel base is 0.00.
1 to IW/W%, preferably 0.005 to 0.5 w/w
%, more preferably 0.01 to 0.25 w/w%.

In order to increase the solubility and dispersibility of the steroids in water, oil components such as crotamiton, bennoral alcohol, isopropyl myristate, ethylene glycol, diethyl-2-ethyl-5-pyrrolidone sepanolate, and surfactants are added. It can be done by blending.

Furthermore, conventionally known stabilizers, antioxidants, pI-(Q adjusters, inorganic fillers, etc.) may be added as desired.

Next, the support used in the present invention is preferably a flexible support that follows the movements of the human body, such as various woven fabrics,
Examples include non-woven fabrics and flannel. In addition, in the external patch of the present invention, since the adhesive gel base layer is a continuous phase,
The effect of the occlusive bandage method can be expected, but if a stronger effect of the occlusive bandage method is desired, the above-mentioned support may be
A support laminated with ethylene vinyl acetate, polyethylene, polyvinyl chloride, polyurethane, etc. can be used.

The present invention not only causes less side effects such as skin inflammation than conventionally known tape preparations, but also causes less damage to the affected area and less exfoliation of dead skin when peeling off, so it can be applied repeatedly. . In addition, when this topical patch is applied to a skin disease area, it can not only be expected to have the same occlusive dressing effect as conventional tapes, but also actively hydrate the stratum corneum due to the water contained in this topical patch. As a result, the absorption of the steroid drug, which is a component of the medicinal herbal medicine, is improved, and better therapeutic effects can be achieved.

Furthermore, in order for a topical patch to exert its medicinal effect when applied to a skin disease area, it is necessary for the drug to be released from the base and migrate to the skin; This is thought to be related to the affinity of Factors that affect this affinity include the solubility, diffusion coefficient, and thermodynamic activity of the drug in the base or base components, but this topical patch has a combination of base components that can affect these factors. Since it is possible to control the concentration of each drug, it is possible to set the optimal concentration of each drug, and it is possible to obtain superior therapeutic effects compared to other preparations.

The present invention will be explained in more detail by giving examples and experimental examples below. "Parts" in the examples mean parts by weight.

Example I 31 parts of water, 5.0 parts of gelatin, paraoxyl, 0.1 part of methyl fragrant, 0.2 parts of citric acid, 0.1 part of triamunolone acetonide, 10 parts of crotamiton, 20 parts of sorbitol, glycerin 30 parts and polyacrylic acid 4.0
After stirring and dissolving a portion while heating in a kneader, a solution of 0.5 part of potassium aluminum sulfate dissolved in 8 parts of water was added to this, and the mixture was sufficiently stirred to obtain a sticky gel base. Apply 200g of this adhesive gel base onto release paper using a conventional method.
/m', then transferred to a polyurethane-laminated nonwoven fabric made of rayon, cut to desired size, and applied 20 parts g/m' of triamunolone acetonide.
An external patch containing cm' is obtained.

Example 2 25 parts of water, 10 parts of polyacrylic acid, 5 parts of zinc white, 6 parts of polyvinyl alcohol, 3.0 parts of benzyl alcohol, 10 parts of hydrocordesin, 0 parts of propyl roseoxybenzoate
．． 1 part, carboxymethylcellulose sodium salt8.
After dissolving 0 parts of glycerin, 20 parts of glycerin, and 20 parts of sorbitol in Nigu in the same manner as in Example I, a solution of 0.2 parts of dihydroquine aluminum aminoacetate dissolved in 2 parts and 5 parts of water was added, and the mixture was thoroughly stirred. to obtain a sticky gel base. From this base, an external patch containing 200 μg/cm' of hydrocortisone is obtained in the same manner as in Example I.

An external patch containing 20 parts g/cm2 of dexamethacin acetate is obtained in the same manner as in Example 1 except that 0.1 part of each four-membered dexamethacin acetate is used.

50 parts g/c of medylbretonisolone was prepared in the same manner as in Example 1 except that 0.25 parts of medylbretonisolone was used.
An external patch containing m2 is obtained.

Example 5 An external patch containing 100 μg/cm' of prednisolone is obtained in the same manner as in Example 1, except that 0.5 parts of prednisolone is used.

Example (An external patch containing 8 μg/cm” of fluoronono[7-acetonide] is obtained in the same manner as in Example 1 except that o , o = i parts of fluocinolone acetonide are used.

Fire Test Temporary ↓ According to the skin pallor test, the patches of Examples 1 to 6, and each containing fludoquincortide 4 μg/am', fluocinolone acetonide 8 μg/cm", and betamethacin valerate 6 μg/am' The effectiveness of commercially available acrylic adhesive tapes was compared.

Each of these steroid-containing patches and commercially available tapes was punched out into a circular shape with a diameter of 10 mm and used as a test sample.
These samples were randomly assigned and applied to the middle backs of 10 healthy male adults. Pasting time is 30 minutes, 1 hour, 2
The skin pallor was determined at 2 and 4 hours after peeling.

The results are shown in Tables 1 to 4. Tables 1 and 2 show the results measured 2 hours after the peeling.Table 1 shows the number of people who tested positive out of the 10 people who tested, and Table 2 shows the number of people who tested positive or who tested positive. represent Tables 3 and 4 show the results of measurements taken 4 hours after stripping, Table 3 shows the number of people who tested positive out of 10, and Table 4 shows the number of people who tested positive or clotted.

(Margin below)

Claims (1)

[Claims] (1) An external patch containing a steroid agent (excluding deprodone propionate) in an adhesive gel base containing a water-soluble polymer, water, and a water-retaining agent as essential ingredients.