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Slow-release transdermal patch containing isosorbide mononitrate and application thereof

An isosorbide dinitrate, sustained-release transdermal technology, applied in the directions of heterocyclic compound active ingredients, cardiovascular system diseases, pharmaceutical formulations, etc. Frequent dosing and other problems to achieve the effect of improving drug safety, small changes in color and stickiness, and avoiding interference and degradation

Inactive Publication Date: 2017-11-07
徐静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to overcome the short half-life and frequent administration of isosorbide mononitrate in the prior art for the oral treatment of angina pectoris, making it difficult to achieve the most ideal stable treatment and preventive effects for patients with angina pectoris, and the medicine cannot be used for a long time. The problem with the disadvantages of entering the body at a near constant rate

Method used

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  • Slow-release transdermal patch containing isosorbide mononitrate and application thereof
  • Slow-release transdermal patch containing isosorbide mononitrate and application thereof
  • Slow-release transdermal patch containing isosorbide mononitrate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: The sustained-release transdermal patch formula of isosorbide mononitrate is as follows:

[0048]

[0049] The preparation method is as follows:

[0050] ①Dissolve isosorbide mononitrate, azone, and stearyl alcohol in ethyl acetate, add silicone pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material with an area of ​​10000cm2, heat and dry , and then covered with a protective layer, ③ cut according to the required size, packaged, and then made into a slow-release transdermal patch containing isosorbide mononitrate. Embodiment 2: The sustained-release transdermal patch formula of isosorbide mononitrate is as follows:

Embodiment 2

[0050] ①Dissolve isosorbide mononitrate, azone, and stearyl alcohol in ethyl acetate, add silicone pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material with an area of ​​10000cm2, heat and dry , and then covered with a protective layer, ③ cut according to the required size, packaged, and then made into a slow-release transdermal patch containing isosorbide mononitrate. Embodiment 2: The sustained-release transdermal patch formula of isosorbide mononitrate is as follows:

[0051]

[0052] The preparation method is as follows:

[0053] ① Dissolve isosorbide mononitrate and stearyl alcohol in ethyl acetate, add silicone pressure-sensitive adhesive and mix well.

[0054] ②Apply the mixed glue on the backing material with an area of ​​10000cm2, heat and dry, and then cover with a protective layer.

[0055] ③Cut according to the required size, pack, and then make a transdermal patch containing isosorbide mononitrate.

Embodiment 3

[0056] Embodiment 3: The sustained-release transdermal patch formula of isosorbide mononitrate is as follows:

[0057]

[0058]

[0059] The preparation method is as follows:

[0060] ①Dissolve isosorbide mononitrate, azone, and stearyl alcohol in ethyl acetate, add fat-soluble acrylate pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material with an area of ​​10000cm2, heat and dry, and then covered with a protective layer, ③ cut according to the required size, packaged, that is, to make a slow-release transdermal patch containing isosorbide mononitrate.

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Abstract

The invention relates to a slow-release transdermal patch containing isosorbide mononitrate and an application thereof. The slow-release transdermal patch is composed of a backing layer, a drug-containing storage layer and an anti-sticking protecting layer; the drug-containing storage layer is prepared according to a preparation method which comprises the following steps: uniformly mixing isosorbide mononitrate with macromolecule adhesive material or pressure-sensitive adhesive, coating on the backing layer, heating and drying, thereby acquiring the drug-containing storage layer; the macromolecule adhesive material or pressure-sensitive adhesive is selected from water-soluble crylic acid pressure-sensitive adhesive, fat-soluble crylic acid pressure-sensitive adhesive, organosilicone pressure-sensitive adhesive and polyisobutene pressure-sensitive adhesive; the drug-containing storage layer contains a transdermal accelerant and is selected from azone, oleic acid, glyceryl triacetate and isopropyl myristate; the drug-containing storage layer contains crystallization inhibitor octadecanol.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a slow-release transdermal preparation for external use of medicine, in particular to a slow-release transdermal preparation containing isosorbide mononitrate and its application. Background technique [0002] Isosorbide mononitrate is the main active metabolite of isosorbide dinitrate. Like other organic nitrates, isosorbide mononitrate releases nitric oxide. Nitric oxide increases cGMP by activating guanylate cyclase, activates cGMP-dependent protein kinase, and changes the rings of various proteins in smooth muscle cells. Phosphorylation, thereby relaxing vascular smooth muscle. Isosorbide mononitrate dilates peripheral arteries and veins by relaxing vascular smooth muscle and causing vasodilation. Decreases ventricular end-diastolic pressure and volume (preload) by dilating the veins to increase venous volume and reduce return to the heart. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/34A61K47/10A61K47/22A61K47/14A61P9/10
CPCA61K9/7061A61K9/0002A61K31/34A61K47/10A61K47/14A61K47/22
Inventor 徐静
Owner 徐静
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