JPH07106979B2 - Transdermal formulation - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention is intended to prevent skin irritation by incorporating a small amount of a nonsteroidal anti-inflammatory agent in a transdermal preparation.

[Prior art]

Conventionally, as a means for transdermally administering a drug, a plaster agent or a pap which is directly or indirectly spread on a carrier such as a flexible cloth, a non-woven fabric or various plastic films by containing the drug in an adhesive polymer. Agents, tapes, etc. have been used, but physical effects such as pulling hair during exfoliation, exfoliation of keratin, stuffiness caused by long-term application, redness due to physiological effects such as sweating, and side effects such as touch Was a problem.

For example, JP-A-58-4721, JP-A-60-5114, and JP-A-60-5114
60-56911, JP-A-60-23312 and the like disclose drug formulations for preventing contact with the skin and reducing skin irritation.

[Problems to be solved by the invention]

However, in any case, there is a problem in practicability and the effect is insufficient, so that further improvement is currently awaited.

[Means for solving problems]

In view of the above technical situation, the present inventors have conducted intensive studies for the purpose of developing a transdermal patch that solves the problems in the prior art, and as a result, in a transdermal preparation, a nonsteroidal anti-steroid drug is contained in the preparation. The present invention provides a transdermal preparation that prevents contact with the skin by incorporating an inflammatory agent.

Next, the constituent components of the present invention will be described.

As the non-steroidal anti-inflammatory agent mixed as an anti-feeling agent, known ones can be widely used, for example, ibuprofen, ketoprofen, flurbiprofen, fluphenamic acid, fenoprofen, naproxen, fenbufen, and ester derivatives thereof. The content is 0.001 to ² mg / cm ² , preferably 0.005 to 1
a mg / cm ^2, more preferably from 0.01 to 0.5 / cm ^2.

The pressure-sensitive adhesive is not particularly limited as long as it exhibits tackiness at room temperature. For example, silicone-based, styrene-isoprene-styrene-based, acrylic-based, natural rubber-based, urethane-based, polyisobutylene-based oil-based adhesives, vinyl ether-based, gelatin / sodium polyacrylate-based water-based adhesives, etc. are used at appropriate times. be able to. Further, it goes without saying that conventionally known tackifiers, antioxidants and the like can be used as necessary.

As the main drug, transdermal drug (eg, hypnotic sedative, antiepileptic drug, antipyretic analgesic / antiinflammatory drug, stimulant / stimulant, sedative,
Psychiatry, antispasmodics, antihistamines, cardiotonics, arrhythmias, diuretics, antihypertensives, vasodilators, arteriosclerosis agents, antitussive agents, hormones, chemotherapeutic agents, anticancer agents, etc.) There is no particular limitation as long as it is 0.001 to 3 mg / c.
It can be used in a blending amount of m ² .

As the support, stretchable and non-stretchable ones are used, for example, polyethylene, polypropylene, polybutadiene, ethylene vinyl acetate copolymer, polyvinyl chloride,
It is selected from a film or sheet of polyester, nylon, polyurethane or the like, or a laminated body, a porous body, a foamed body thereof, paper, cloth, non-woven fabric or the like.

[Action effect]

The percutaneous preparation of the present invention obtained as described above, by virtue of the incorporation of a non-steroidal anti-inflammatory agent as the anti-feeling agent, is capable of eliminating the feeling of touch that was frequently occurring in the conventional transdermal preparations. It is very useful medically.

Hereinafter, the present invention will be described in more detail by showing test examples and examples.

Example 1 A copolymer of 2-ethylhexyl acrylate-acrylic acid was added to scopolamine 0.1 mg / cm ² and ketoprofen 0.03 mg / cm ² as a non-steroidal anti-inflammatory agent, and aluminum was vapor deposited. It was spread on a vinyl chloride film with a thickness of 60 μm to give a transdermal preparation of the present invention.

Example 2 Styrene-isoprene-styrene block copolymer / hydrogenated rosin resin / mineral oil with a ratio of 4.5 / 3/3, methyl salicylate 0.4 mg / cm ² , l-menthol 0.5 mg / cm ^2. Was added as a non-steroidal anti-inflammatory agent, and 0.01 mg / cm ² of flurbiprofen was added, followed by spreading on a release paper with a thickness of 90 μm and covering with a vinyl chloride sheet to give a transdermal preparation of the present invention.

Example 3 Styrene-isoprene-styrene block copolymer / petroleum resin / mineral oil, in a ratio of 5/4/3, with ketotifen 0.1.
mg / cm ² , ketoprofen 0 as a non-steroidal anti-inflammatory drug.
02 mg / cm ^{2 was} mixed and spread on a polyester film with a thickness of 100 μm to give a transdermal preparation of the present invention.

Example 4 Natural rubber / rosin-modified resin / polybutene / zinc oxide, 7 /
Methyl salylate 1.6 mg / cm ² , l-menthol 1.0 mg / cm ² , dl-camphor 0.3 mg / cm ² , pranoprofen 0.04 mg / cm ^{2 as} a non-steroidal anti-inflammatory drug in a ratio of 6/2/3 ^It was blended so as to be ² and spread on a cloth with a thickness of 200 μm to give a transdermal preparation of the present invention.

Example 5 2-Ethylhexyl acrylate-Vinyl acetate copolymer was blended in an amount of 0.01 mg / cm ² indomethacin and 0.006 mg / cm ² ketoprofen as a non-steroidal anti-inflammatory agent,
It was spread on a polyethylene film with a thickness of 60 μm to give a transdermal preparation of the present invention.

Example 6 Styrene-isoprene-styrene block copolymer / petroleum-based resin / mineral oil in a ratio of 1 / 0.6 / 1 with clonidine 0.7.
mg / cm ² , ketoprofen 0 as a non-steroidal anti-inflammatory drug.
02 mg / cm ^{2 was} mixed and spread on a polyester-vinyl chloride composite film with a thickness of 100 μm to give a transdermal preparation of the present invention.

Example 7 Styrene-isoprene-styrene block copolymer / petroleum resin / mineral oil, with a ratio of 1 / 1.2 / 1.8, isosorbite dinitrate 0.6 mg / cm ² , ketoprofen 0.015 mg / non-steroidal anti-inflammatory agent cm ^{2 was} mixed and spread on a polyester film with a thickness of 100 μm to obtain a transdermal preparation of the present invention.

Test Example 1 (Skin Irritation Test) Using Examples 1, 2, 3, 4 and 5 of the present invention, healthy adult males 30
It was applied to the back of the name for 48 hours, and judged 1 hour and 24 hours after the peeling, respectively, and the condition of skin irritation was observed. (As reference examples, those obtained by removing the non-steroidal anti-inflammatory agent from the examples are used, and the reference examples 1 to 5 are in accordance with the examples 1 to 5.
Each sample was punched out with a diameter of 20 mm and pressed with a patch test plaster. ) The results are shown in Table 1.

In addition, the following was used as a judgment standard, and the sum of each score was divided by the number of volunteers and multiplied by 100, and expressed as a skin irritation index.

Judgment score No change − 0 Weak redness ± 0.5 Clear redness + 1.0 Serious feeling 2.0 From the above test results, the present invention showed a remarkable skin irritation inhibitory effect by containing a small amount of a nonsteroidal drug.

Claims (2)

[Claims] 1. A transdermal patch containing a transdermal drug and an adhesive, further comprising a non-steroidal anti-inflammatory agent different from the transdermal patch. Agent. 2. The transdermal patch according to claim 1, wherein the nonsteroidal anti-inflammatory drug is added in an amount of 0.001 to ² mg / cm ² .