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Ramipril-containing external-application slow-release transdermal patch and application thereof

A slow-release transdermal patch and slow-release transdermal technology, applied in the field of pharmaceutical preparations, can solve problems such as difficulty in achieving therapeutic effects in patients with hypertension, inability of drugs to enter the human body, and large fluctuations in blood drug concentration, so as to avoid blood drug Concentration peak and trough phenomenon, avoid interference and degradation, and reduce the effect of individual differences

Inactive Publication Date: 2016-01-06
徐静 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the large fluctuation of blood drug concentration caused by the existence of peak and trough phenomena in the prior art when ramipril is taken orally for the treatment of hypertension, which leads to unstable antihypertensive effect, and it is difficult to realize the optimal treatment for hypertensive patients. The therapeutic effect of stable blood pressure reduction, the shortcoming that the drug cannot enter the human body at a nearly constant rate for a long time

Method used

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  • Ramipril-containing external-application slow-release transdermal patch and application thereof
  • Ramipril-containing external-application slow-release transdermal patch and application thereof
  • Ramipril-containing external-application slow-release transdermal patch and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: To prepare a topical sustained-release transdermal patch containing ramipril:

[0038] Raw materials Composition ratio (g) Ramipril 6.0 50% ethanol solution 18.0 Water Soluble Acrylic Pressure Sensitive Adhesive 66.0

[0039] Prepare according to the following preparation process:

[0040] ① Dissolve ramipril in 50% ethanol solution, add water-based acrylate pressure-sensitive adhesive and mix well. ②Apply the mixed glue on the backing material with an area of ​​20000cm 2 , heated and dried, and then covered with a protective layer. ③Cut according to the required size, pack, and then make an external slow-release transdermal patch containing ramipril.

Embodiment 2

[0041] Example 2: To prepare a topical extended-release transdermal patch containing ramipril:

[0042] Raw materials Composition ratio (g) Ramipril 10.0 50% ethanol solution 15.0 Water Soluble Acrylic Pressure Sensitive Adhesive 60.0

[0043] Prepare according to the following preparation process:

[0044] ① Dissolve ramipril in 50% ethanol solution, add water-based acrylate pressure-sensitive adhesive and mix well. ②Apply the mixed glue on the backing material, with an area of ​​5000cm 2 , heated and dried, and then covered with a protective layer. ③Cut according to the required size, pack, and then make ramipril-containing transdermal patch for external use.

Embodiment 3

[0045] Example 3: To prepare a topical extended-release transdermal patch containing ramipril:

[0046] Raw materials Composition ratio (g) Ramipril 15.0 Triacetin 3.0 acetone 30.0 Fat soluble acrylate pressure sensitive adhesive 105.0

[0047] Prepare according to the following preparation process:

[0048] ① Dissolve ramipril and triacetin in acetone, add fat-soluble acrylate pressure-sensitive adhesive and mix well. ②Apply the mixed glue on the backing material with an area of ​​10000cm 2 , heated and dried, and then covered with a protective layer. ③Cut according to the required size, pack, and then make an external slow-release transdermal patch containing ramipril.

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Abstract

The invention relates to a ramipril external-application slow-release transdermal patch and an application thereof. The external-application patch is used for treating hypertension with ramipril as a main drug. According to the ramipril external-application slow-release transdermal patch, as transdermal absorption is achieved, drugs are evenly released, the effect is mild and durable, and blood pressure fluctuation caused by oral medication is avoided. The ramipril external-application slow-release transdermal patch directly acts on the skin and does not pass through the gastrointestinal tract, the first-pass effect of the liver is avoided, adverse effects are reduced, and the occurrence rate of the adverse effects is reduced. Patient compliance is good, and use and carrying are convenient.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an external slow-release transdermal preparation of medicine, in particular to an external slow-release transdermal preparation containing ramipril and its application. Background technique [0002] Ramipril is a prodrug that is hydrolyzed in the liver after absorption from the gastrointestinal tract to yield ramiprilat - an active, potent and long-acting angiotensin-converting enzyme (ACE) inhibitor. Taking ramipril can lead to an increase in plasma renin activity and a decrease in plasma concentrations of angiotensin II and aldosterone. Because of the reduction of angiotensin II, ACE inhibitors can lead to peripheral vasodilation and decreased vascular resistance, resulting in beneficial hemodynamic effects. Evidence suggests that tissue ACE, especially the vasculature—rather than circulating ACE—is the major determinant of hemodynamic effects. ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K38/05A61P9/12
Inventor 徐静张艳红杨洋
Owner 徐静
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