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Patch containing isosorbide dinitrate

A technology of isosorbide and dinitrate, applied in the direction of drug combination, cardiovascular system diseases, active ingredients of heterocyclic compounds, etc.

Inactive Publication Date: 2003-03-05
TEIJIN LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The inventors of the present invention have earnestly pursued studies to accomplish the above tasks and have accomplished the present invention by the following findings: acrylic adhesive (A), polyvinyl acetate adhesive (B), plasticizing component (C) Combination with isosorbide dinitrate (D) can realize the purpose of the present invention by specific weight ratio, but can't realize with conventional method

Method used

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  • Patch containing isosorbide dinitrate
  • Patch containing isosorbide dinitrate
  • Patch containing isosorbide dinitrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0150] 87.5 parts of polyvinyl acetate binder solution (coating solution B), 87.5 parts of acrylic binder solution (coating solution A), 35 parts of isopropyl myristate (C), 30 parts of isosorbide dinitrate Ester (D), 193 parts of ethyl acetate and 0.14 parts of aluminum acetylacetonate were mixed to an almost uniform state, and the resulting mixture was used to coat a 75 μm thick polyethylene terephthalate spacer (Japanese Pharmaceutical Excipient Forming agent) so that the thickness after drying is 45 μm, it is fully dried, and the residual ethyl acetate becomes 100 ppm or less to obtain a drug storage layer. A polyethylene terephthalate film (PET film, Teijin film F3 type) having a thickness of 2.0 μm was pressed so as to be bonded to the free surface of a drug reservoir layer having a thickness of 45 μm containing 30% by weight of isosorbide dinitrate .

[0151] In addition, after mixing 117.5 parts of coating solution B, 117.5 parts of coating solution A, 35 parts of iso...

Embodiment 3

[0158] Mix 60 parts of coating solution B, 140 parts of coating solution A, 30 parts of isopropyl myristate (C), 30 parts of isosorbide dinitrate (D), 140 parts of ethyl acetate and 0.16 parts of aluminum acetylacetonate to almost After a uniform state, the formed mixture was coated with a polyethylene terephthalate separator (Japanese pharmaceutical excipient) with a thickness of 75 μm to a thickness of 53 μm after drying, and it was fully dried, and the remaining Vinyl acetate becomes 100 ppm or less to obtain a binder.

[0159] A polyethylene terephthalate film (Teijin film F3 type) having a thickness of 2.0 μm was pressed to be bonded to the free surface of the adhesive layer containing 30% by weight of isosorbide dinitrate to obtain a crude fabric patch. Cut the rough fabric patch to size 25cm 2 (long 3.5cm, wide 7.1cm), obtain the 25cm that contains 40mg isosorbide dinitrate 2 Patches (TC-3). TC-3 was evaluated as in Example 1, and the results are listed in Table 1. ...

Embodiment 4

[0159] A polyethylene terephthalate film (Teijin film F3 type) having a thickness of 2.0 μm was pressed to be bonded to the free surface of the adhesive layer containing 30% by weight of isosorbide dinitrate to obtain a crude fabric patch. Cut the rough fabric patch to size 25cm 2 (long 3.5cm, wide 7.1cm), obtain the 25cm that contains 40mg isosorbide dinitrate 2 Patches (TC-3). TC-3 was evaluated as in Example 1, and the results are listed in Table 1. [Example 4 and Comparative Examples 1-10]

[0160] The weight ratio of A, B, C and D of embodiment 3 is changed into as shown in table 1, obtains patch (embodiment 4 and comparative example 1-10) in the same manner as embodiment 3, and evaluation result is listed in in FIG. 1.

[0161] As can be seen from the results of Experiments 1 to 4 shown in Table 1, the specific combination of A, B, C, and D gave extremely high transdermal absorption levels, and especially under the conditions of Experiments 1 and 2, the patch had a ...

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Abstract

The present invention relates to an isosorbide dinitrate-containing patch, in which an adhesive layer comprising an adhesive composition is formed on a flexible support, and the adhesive composition consists of an acrylic-based adhesive (A), a polyvinyl acetate-based adhesive (B), a plasticizing component (C) and isosorbide dinitrate (D), and satisfies the following weight ratios (1) through (3) of each of the components: (1) A:B = 70:30 to 10:90, (2) the weight ratio of the component C based on the adhesive composition is 10 to 40% by weight, and (3) the weight ratio of the component D based on the adhesive composition is 20 to 35% by weight. Provided is a patch excellent in percutaneous absorption, handleability, resistance to skin irritation, sustained release, adhesivity, etc.

Description

technical field [0001] The invention relates to a patch containing isosorbide dinitrate. More specifically, the present invention relates to a patch having advantages such as excellent sustained release and good transdermal absorption, in which an adhesive layer containing an adhesive composition is formed on a flexible carrier, the The binder composition is composed of acrylic binder, polyvinyl acetate binder, plasticizing active components and isosorbide dinitrate in a specific weight ratio. Background of the invention [0002] Patches containing isosorbide dinitrate are generally known, for example, in Japanese Laid-Open Patent Publication 57-116011, pressure-sensitive adhesives such as silicone-based, rubber-based or acrylic adhesives Adhesives are preferred adhesives for use as pressure sensitive adhesives in these patches. In addition, at the 5th meeting of the Japanese Pharmacological Association (September 26-28, 1989), Okuni et al. reported that for patches contai...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/34
CPCY10S514/947A61K9/7061A61K9/703A61K9/7053A61K31/34A61P9/10A61K9/70
Inventor 日高修文村上敏史日月台房大江通介
Owner TEIJIN LTD
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