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Percutaneous administration device of bisoprolol

A technology of bisoprolol and drug delivery device, applied in the field of bisoprolol transdermal drug delivery device, can solve problems such as skin irritation, and achieve the effects of reducing skin irritation, suppressing large fluctuations, and improving cohesion

Inactive Publication Date: 2014-05-14
NITTO DENKO CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in such a patch, since the maximum value of the human skin permeation rate exceeds 30 μg / cm 2 / hour, so depending on the patient there is a high potential for strong skin irritation from bisoprolol

Method used

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  • Percutaneous administration device of bisoprolol
  • Percutaneous administration device of bisoprolol
  • Percutaneous administration device of bisoprolol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 2

[0125] A viscous toluene solution of the pressure-sensitive adhesive composition was prepared according to the mixing ratio shown in Table 1; On a pad (thickness 75 μm), which had previously been subjected to a silicone release treatment; it was then dried in a hot air circulation type dryer at 100° C. for 5 minutes, thereby forming a pressure-sensitive adhesive layer. The pressure-sensitive adhesive layer was bonded on a PET film with a thickness of 12 μm, or a PET film with a thickness of 2 μm and 12 g / m 2 A laminated film of PET nonwoven fabric was placed on the nonwoven fabric side, thereby obtaining a sheet-shaped laminate. The liner made of PET of this laminate was peeled off, and several pressure-sensitive adhesive layers having the same composition and thickness as above were laminated on the exposed pressure-sensitive adhesive surface, thereby obtaining Thickness of the pressure-sensitive adhesive layer of the transdermal drug delivery device. The mixing amount of e...

Embodiment 3 and comparative example 1 to 3

[0127] In an inert atmosphere, 70 parts by weight of 2-ethylhexyl acrylate, 20 parts by weight of 2-methoxyethyl acrylate, 10 parts by weight of 2-hydroxyethyl acrylate and 0.2 parts by weight of azobisiso Nitrile was solution-polymerized in ethyl acetate at 60° C., thereby preparing a solution of an acrylic pressure-sensitive adhesive. The acrylic pressure-sensitive adhesive, isopropyl myristate and bisoprolol were uniformly mixed and stirred in a container according to the mixing ratio shown in Table 1; 0.6% by weight (relative to the pressure-sensitive adhesive solid) of ethyl acetoacetate aluminum diisopropionate; and adjust the viscosity with ethyl acetate. The obtained solution was coated on a liner (thickness 75 μm) made of polyethylene terephthalate (PET) which had previously been treated with silicone release in the dried thickness shown in Table 1 ; and then it was dried at 100° C. for 5 minutes in a hot-air circulation type dryer, thereby forming a pressure-sensiti...

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Abstract

The present invention relates to a percutaneous administration device of bisoprolol. The percutaneous administration device includes a substrate material and a pressure-sensitive adhesive layer which is laminated on one surface of the substrate material and contains bisoprolol, wherein the maximum value of a release rate of bisoprolol during a period of from immediately after the application on skin until a lapse of 24 hours is 30 [mu]g / cm<2> / hr or less; and wherein the release rate of bisoprolol at the time of a lapse of 24 hours after the application on skin is 10 [mu]g / cm<2> / hr or less. The percutaneous administration device of the present invention is reduced in the skin irritation during the application, especially at the time of peeling, and is capable of persistently administrating a therapeutically or preventively effective amount of bisoprolol into a living body.

Description

[0001] This application is a divisional application of a Chinese national patent application with an application date of March 6, 2008 and an application number of 200880007650.1. technical field [0002] The present invention relates to a bisoprolol transdermal administration device capable of administering bisoprolol from the skin surface to the body. Background technique [0003] Bisoprolol is a highly selective antagonist of β1-receptors of the sympathetic nerve (β-blocker), which has been used to improve essential hypertension, angina pectoris and arrhythmia, and its fumarate as a tablet For oral use. On the other hand, in the case of oral administration, the persistence of the effect of bisoprolol is insufficient, and its concentration in the blood is higher than the necessary concentration for a short time after administration, so that side effects are prone to occur. In order to improve these problems, a transdermal drug delivery device is required. [0004] Among ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/138A61P9/12A61P9/10A61P9/06
CPCA61K9/7053A61K9/7061A61K31/138A61P25/02A61P43/00A61P9/00A61P9/06A61P9/10A61P9/12A61K9/70A61K47/32
Inventor 岩男美宏松冈贤介冈田胜博南邦弘汤浅修一朗
Owner NITTO DENKO CORP
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