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Ropinirole-containing sustained-release transdermal patch and application thereof

A sustained-release transdermal and patch technology, which is applied in the field of sustained-release transdermal preparations for external use and sustained-release transdermal preparations containing ropinirole, can solve the problems of inability to maintain stability, low skin permeability, and irritation. and other problems, to achieve the effect of balanced blood drug concentration, high penetration rate, and smooth onset of action.

Inactive Publication Date: 2017-11-24
徐静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The patch of the present invention can solve the problem that the skin permeability of the patch occurs in the acid addition salt (such as ropinirole hydrochloride) form of ropinirole; Stability cannot be maintained within the validity period; or the acid addition salt form of ropinirole is added to a base containing metal ions for reaction to generate a patch in the form of ropinirole free base, but due to the strong alkalinity containing metal ions Produce significant skin irritation problems

Method used

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  • Ropinirole-containing sustained-release transdermal patch and application thereof
  • Ropinirole-containing sustained-release transdermal patch and application thereof
  • Ropinirole-containing sustained-release transdermal patch and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1: prepare the slow release transdermal patch containing ropinirole, formula is as follows:

[0064]

[0065] Prepare according to the following preparation process:

[0066] ①Dissolve ropinirole, azone, and α-linolenic acid in dichloromethane, add fat-soluble acrylate pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, 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 ropinirole.

Embodiment 2

[0067] Embodiment 2: prepare the slow release transdermal patch containing ropinirole, formula is as follows:

[0068]

[0069] ①Dissolve ropinirole, azone, and α-linolenic acid in dichloromethane, add fat-soluble acrylate pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, 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 ropinirole.

Embodiment 3

[0070] Embodiment 3: prepare the slow release transdermal patch containing ropinirole, formula is as follows:

[0071]

[0072] ①Dissolve ropinirole, azone, and α-linolenic acid in dichloromethane, add fat-soluble acrylate pressure-sensitive adhesive and mix evenly. ②Apply the mixed glue on the backing material, with an area of ​​10000cm 2 , heated and dried, 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 ropinirole.

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Abstract

The invention relates to a ropinirole-containing sustained-release transdermal patch and the application thereof. The ropinirole-containing sustained-release transdermal patch consists of a backing layer, a medicine-containing storage layer and an anti-sticking protective layer, wherein a preparation method of the medicine-containing storage layer comprises the following steps: uniformly mixing ropinirole and a high molecular viscous material or a pressure-sensitive adhesive, coating the backing layer with a mixture, heating, and drying to obtain the medicine-containing storage layer; the high molecular viscous material or the pressure-sensitive adhesive is selected from a water-soluble acrylic pressure-sensitive adhesive, a fat-soluble acrylic pressure-sensitive adhesive, an organosilicone pressure-sensitive adhesive and a polyisobutylene pressure-sensitive adhesive; the medicine-containing storage layer contains a transdermal enhancer which is selected from azone, oleic acid and isopropyl myristate; the medicine-containing storage layer contains an antioxidant alpha-linolenic acid which is used for improving the stability of ropinirole free alkali and effectively reducing the skin irritation of the ropinirole-containing sustained-release transdermal patch.

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 sustained-release transdermal preparation containing ropinirole and its application. Background technique [0002] Ropinirole (ROP) is a non-ergot alkaloid drug, which is a second-generation selective dopamine receptor agonist, which can effectively and selectively stimulate the substantia nigra-striatum dopamine D2 receptors in the brain. It can significantly reduce the symptoms of Parkinson's disease (PD) in various stages, and can significantly reduce the symptoms of Parkinson's disease (PD). Therefore, ropinirole has high specificity and will not cause serious pulmonary complications, peripheral edema, erythematous extremity pain and retroperitoneal fibrosis. The main indications are the treatment of Parkinson's syndrome and restless legs. [0003] Ropinir...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4045A61K47/12A61K47/32A61K47/34A61P25/16A61P25/14
CPCA61K31/4045A61K9/0002A61K9/7053A61K9/7061A61K9/7069A61K47/12
Inventor 徐静
Owner 徐静
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