JPS6023312A - Pharmaceutical preparation - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a pharmaceutical formulation used for transdermally absorbing drugs through the skin or mucous membranes of the body.

Conventionally, drugs are absorbed transdermally because the skin surface has a barrier function. Therefore, for example, occlusive therapy has been adopted as an administration method to reduce the barrier function. By sealing the surface, the skin surface (stratum corneum) swells and softens, and the barrier function is lowered, thereby allowing the drug to be absorbed smoothly through the skin.0 According to this method, the desired transdermal absorption is achieved. However, there is a problem in that the moisture generated by the sealed skin surface causes it to swell, causing irritation, and therefore it is necessary to further apply drugs to cure this irritation. there were.

The present invention relates to a novel pharmaceutical preparation that solves the drawbacks of the prior art. It is a pharmaceutical preparation that is intended for transdermal absorption in a completely sealed state, and the adhesive layer contains the main drug that exerts the desired pharmacological effect and a trace amount of anti-inflammatory corticosteroid that prevents irritation due to the sealed adhesive. Contains steroids.

The pharmaceutical formulation of the present invention has the characteristic that even if the pharmaceutical formulation is applied for a long period of time, for example, for about - weeks, the skin surface hardly feels tactile.

The carrier used in carrying out the present invention is intended to allow the drug to be absorbed transdermally in a sealed state, but it is also possible to use a carrier having a low moisture permeability of, for example, 100Mσ24Hrs. .

As such a carrier, a selected plastic film or sheet, firewood foil, or a bonded product of these low moisture permeability members and a high moisture permeability member such as cloth, nonwoven fabric, woven or knitted fabric, etc., is used.

The drug-containing adhesive layer formed on such a carrier is composed of a rubber and/or synthetic resin pressure-sensitive adhesive composition that is substantially non-irritating to the skin, and a pressure-sensitive adhesive composition that produces the desired pharmacological effect. It consists of the main drug, which is used to treat the skin, and a small amount of anti-inflammatory corticosteroid, which is sealed and pasted to prevent irritation.

As the main drug, either systemic or local drugs can be used, and these drugs are generally administered in doses of 1000 μg.
/cd or less.

The amount of anti-inflammatory corticosteroids is determined by the amount of the main drug or the thickness of the adhesive layer.
It is desirable that the voltage does not exceed 30 μVc4 at most. Commercially available corticosteroids can be used selectively.

The fact that the pharmaceutical preparation of the present invention has excellent pharmacological effects and anti-contaminant effects will be specifically explained with reference to the following examples.

Example: An acrylic pressure-sensitive adhesive composition made from a copolymer of 2-ethylhexyl acrylate:alkyl acid (weight ratio 96:4) was added with 400 il VCl of isosorbitol nitrate.
s Dexamethasone acetate 05 μg AJ, and coated on one side of a 6 μm thick polyester film.
A pharmaceutical preparation was obtained by applying the coating to a thickness of 0.07t 1n.

Example 2 Natural rubber: Polyterpene resin: Polybutene (weight ratio 5
:5:1), 100 μf 1M of clonidine, and 10 μg prednisolone acetate.
/ca, and 80 μm was applied to the vapor deposition surface of a polyester film with a thickness of 80 μm that was aluminum-deposited on one side.
A pharmaceutical preparation was obtained by applying the coating to a thickness of 2 m.

Example 3 A rubber-based pressure-sensitive adhesive composition consisting of styrene-isoprene-styrene block copolymer: hydrogenated rosin (softening point 100°C): polybutene: liquid paraffin (weight ratio 10:9:2:4), Scopolamine hydrobromide 200μg/c and fluocinolone acetate 1μ9Ad were mixed together and applied to one side of a polybutadiene closed cell foam with a thickness of 100μm. A pharmaceutical formulation was obtained.

Example 4 Isooctyl acrylate: Acrylamide (weight ratio 95
An acrylic pressure-sensitive adhesive composition prepared by blending 10 parts by weight of the copolymer of 5) with 10 parts by weight of isopropyl myristate as a transdermal absorption promoting agent, 100 μji/c4 of indomethacin, and hydrocortisone acetate. A composite sheet (thickness: 150 μm) made by laminating ethylene-vinyl acetate copolymer (vinyl acetate content: 8% by weight) on acetate cloth was coated with a thickness of 80 μm on one side of the composite sheet (thickness: 150 μm). A pharmaceutical preparation was obtained by coating.

Table 1 shows the test results of Examples 1 to 4. Reference Examples 1 to 4 in Table 1 correspond to Examples 1 to 4, respectively, and in each case, no anti-inflammatory corticosteroid was added.

Table 1 Test method in Table 1 Drug absorption rate: Hair was removed from the back of a rabbit, and each sample (5c
7rLX 10 crn) was pasted, 1 hour later, 3
After 1 hour, 6 hours, 12 hours, and 24 hours, blood was collected, the blood concentration was measured, a blood concentration curve was drawn, and the area under the curve was calculated to determine the amount of drug absorbed, which was then used as the initial formulation. It was calculated by dividing by the amount (average value of n=3).

Positive rate: A sample (diameter 1
A 5 crn circle) was pasted, removed after 48 hours, and after another hour, the condition of the skin was observed and evaluated using a 5-step method. The criteria for judgment are as follows: → and the ratio of 10 (average value of n = 20) 0+-: 12 edema ±: 1 red spot: 11 red spots: No change Patent applicant date T41 Electric Industry Co., Ltd. Representative Kamigata Sanbe 85-

Claims (1)

[Claims] A pharmaceutical formulation for transdermal absorption of a drug contained in a sealed state, comprising a carrier and a drug-containing adhesive layer formed on the carrier, wherein the adhesive layer has a target pharmacological effect. 1. A pharmaceutical preparation characterized by containing a main drug that exhibits this effect and a trace amount of an anti-inflammatory corticosteroid that prevents irritation due to sealed application.