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Percutaneous absorption type preparation

A preparation and adhesive technology, which can be used in respiratory diseases, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of reducing skin adhesion characteristics, short-term efficacy, difficulties, etc. Absorption characteristics, excellent transdermal absorption rate, excellent efficacy period effect

Inactive Publication Date: 2003-12-03
NITTO DENKO CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method faces the following problems: difficulties in administration to infants, etc., occurrence of side effects caused by a sharply increased blood concentration, short-term drug effects, etc.
[0005] Formulations containing solid drug crystals in the plaster layer are susceptible to deposition of drug crystals on the surface of the plaster layer when in contact with the skin, thereby reducing the adhesive properties to the skin

Method used

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  • Percutaneous absorption type preparation
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Examples

Experimental program
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Embodiment 1

[0051] Polymerization of 2-ethylhexyl acrylate (50 parts), 2-methoxyethyl acrylate (25 parts) and vinyl acetate (25 parts) in ethyl acetate under an inert atmosphere produces a An acrylic adhesive solution. Chlorbuterol was added to the solution so that its content in the plaster layer was 10%, and the mixture was thoroughly stirred. The solution was cast on a pad so that the thickness after drying became 40 µm, and dried to produce a plaster layer. The plaster layer was bonded to a support (12 µm thick polyester film) to obtain a transdermal preparation of the present invention.

Embodiment 2

[0053] In the acrylic adhesive obtained in embodiment 1, add chlorbutazone and polyoxyethylene octyl phenyl ether (the addition mole number of oxyethylene is 3, OP-3, by NIKKO Chemicals CO.LTD. Production), so that their content in the plaster layer is 10%. The mixture was well stirred and in the same manner as in Example 1, a transdermal preparation of the present invention was obtained.

Embodiment 3

[0055] An acrylic binder solution was produced by polymerizing 2-ethylhexyl acrylate (95 parts) and acrylic acid (5 parts) in ethyl acetate under an inert atmosphere. Chlorbuterol and isopropyl myristate as an additive are added to the solution so that their contents in the plaster layer are divided into 20% and 30%, and the mixture is fully stirred. A polyisocyanate compound (trade name: CORONATEHL, produced by NIPPON POL YURETHANE INDUSTRY CO., LTD.) in a proportion of 0.15% of an acrylic binder was added as a crosslinking agent, and the mixture was thoroughly stirred. The solution was cast on a release liner so that the thickness became 60 µm after drying, and dried to obtain a plaster layer. Then, make the plaster layer and the support on the nonwoven side [polyester nonwoven laminated film (basis weight 12g / m 2 ) and 6 μm thick polyester film] bonded to obtain the transdermal preparation of the present invention.

[0056] To accelerate the crosslinking reaction, the for...

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Abstract

A percutaneous absorption type preparation comprising a support and a plaster layer laminated thereon, which comprises tulobuterol in a proportion of not less than 5 wt% in a dissolution state and an adhesive. The preparation of the present invention retains the active ingredient, tulobuterol, at a high concentration in a complete dissolution state in the plaster layer. Therefore, it is free of time-course changes in drug releasing property and adhesive property caused by precipitation of drug crystals with the lapse of time. The inventive preparation is superior in percutaneous absorption of the drug, particularly percutaneous absorption rate at the initial stage of the administration; shows superior duration of efficacy by maintaining effective blood concentration for a long time; and is associated with less changes with the lapse of time in adhesive property such as adhesion to the skin.

Description

field of invention [0001] The present invention relates to a percutaneous absorption type preparation, which can make chlorbuterol continuously administered into the body through the skin when it is applied on the skin surface. More specifically, the present invention relates to a drug which, when applied to the skin surface, is superior in adhesion to the skin, superior in the initial absorption characteristics of clonbuterol, and capable of maintaining an effective concentration of clonbuterol in the blood. Percutaneous absorption preparations. Background technique [0002] Chlorbuterol selectively stimulates sympathetic beta 2 Receptors have a bronchodilation effect. Therefore, it is widely used in the treatment of chronic bronchitis, bronchial asthma, etc. in an attempt to relieve the dyspnea of ​​patients with narrowed airways. [0003] For example, clonbuterol is generally administered to the body by oral tablet or the like. However, this method faces the following...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/00A61K31/045A61K31/135A61P11/00A61P11/08
CPCY10S514/946A61K9/7053Y10S514/947A61K9/7061A61K31/135A61P11/00A61P11/06A61P11/08
Inventor 仲野善久堀光彦山本启二大塚三郎
Owner NITTO DENKO CORP
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