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Nisoldipine controlled-release patch and preparation method thereof

A nisoldipine and prescription technology, applied in the antihypertensive transdermal drug delivery system, the nisoldipine transdermal patch and the field of preparation thereof, can solve the problem of low bioavailability, large fluctuation of blood concentration, reduction of medication frequency, etc. problem, to achieve the effect of smooth percutaneous penetration

Inactive Publication Date: 2013-04-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the drug has the characteristics of low dosage and suitable physical and chemical properties, if it is made into a transdermal preparation, the frequency of medication can be reduced, the first-pass effect can be avoided, and the defects of low bioavailability and large blood concentration fluctuation of oral preparations can be overcome

Method used

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  • Nisoldipine controlled-release patch and preparation method thereof
  • Nisoldipine controlled-release patch and preparation method thereof
  • Nisoldipine controlled-release patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Composition of the drug-loaded polymer layer: 2 g of polyvinyl alcohol (PVA205), 0.8 g of polyvinylpyrrolidone (PVP), 0.375 g of azone, 0.375 g of propylene glycol, 0.6 g of glycerin, and 100 mg of nisoldipine.

[0026] Preparation method: add the prescribed amount of penetration enhancer and plasticizer to 65% ethanol and mix evenly, dissolve the prescribed amount of medicine, add polyvinyl alcohol and polyvinylpyrrolidone to swell overnight at 45°C, dissolve in a water bath at 60°C until clear, After magnetically stirring evenly, degas, coat on release paper, dry at 50°C, cover with aluminum foil and compound polyethylene, cut and divide the dose, and seal it for storage. Wherein the content of nisoldipine is 4mg / cm 2 .

[0027] The in vitro permeation behavior of the drug-loaded patch through the shaved abdominal skin of rats was measured by a modified Franz diffusion cell, and the experiment lasted for 72 hours. The calculated permeation rate is 2.476μg / (cm 2 h),...

Embodiment 2

[0029] Composition of the drug-loaded polymer layer: 2.4 g of polyvinyl alcohol (PVA205), 0.4 g of polyvinylpyrrolidone (PVP), 0.75 g of propylene glycol, 0.6 g of glycerin, and 50 mg of nisoldipine.

[0030] With the preparation method of embodiment 1, it is 2mg / cm2 that nisoldipine content is obtained 2 patch.

[0031] The same method as in Example 1 measured that the penetration rate through the skin of the abdomen of the rat was 3.043 μg / (cm) during the 72h period. 2 h), the cumulative percutaneous penetration is 215.34μg / cm 2 .

Embodiment 3

[0033] Composition of the drug-loaded polymer layer: 2.4 g of polyvinyl alcohol (PVA205), 0.4 g of hydroxymethylpropyl cellulose (HPMC), 0.9 g of oleic acid, 0.6 g of glycerin, and 25 mg of nisoldipine.

[0034] With the preparation method of embodiment 1, it is 1mg / cm to make nisoldipine content 2 patch.

[0035] Measured with the method of Example 1 during 72 hours through the permeation rate of rat abdominal hair removal skin is 1.595 μ g / (cm 2 h), 72h cumulative transdermal penetration is 113.12μg / cm 2 .

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PUM

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Abstract

The invention belongs to the field of pharmaceutic preparation, and particularly relates to a transdermal patch of antihypertensive drug nisoldipine, and a preparation method thereof. The nisoldipine controlled-release patch disclosed by the invention is composed of a backing layer, a drug-polymer layer and a release liner, wherein the drug-polymer layer is composed of drug nisoldipine, a drug-polymer, a penetration enhancer and a plasticizer. The nisoldipine transdermal patch prepared by the preparation method can lastingly release drug within three days at a constant speed.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an antihypertensive transdermal drug delivery system, in particular to a nisoldipine transdermal patch and a preparation method thereof. Background technique [0002] Nisoldipine is a dihydropyridine calcium antagonist, which has a specific blocking effect on smooth muscle and cardiac calcium channels, which can dilate peripheral blood vessels and reduce resistance, thereby reducing blood pressure. Clinical studies have shown that while nisoldipine causes a drop in blood pressure, it has no significant effect on the respiratory and central nervous systems, and long-term treatment does not produce tolerance. However, the drug has a large first-pass effect in the gastrointestinal tract and liver, and its oral bioavailability is less than 5%. Common tablets require frequent and multiple medications to achieve the antihypertensive effect, thus increasing the toxic and side ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4422A61P9/12
Inventor 刘建平肖琰
Owner CHINA PHARM UNIV
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