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Crebanine transdermal patch and preparation method thereof

A transdermal patch and the technology of kebanin, applied in the field of medicine, can solve the problems of small antiarrhythmic therapeutic index, narrow safety range, and easy recurrence, and achieve stable antiarrhythmic effect, non-irritating and toxic, long-lasting effect

Active Publication Date: 2017-08-08
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the study also found that the therapeutic index of kebanine injection for arrhythmia is small, the safety range is relatively narrow, and improper dosage may lead to poisoning or death. The time is short, prone to repeated phenomena

Method used

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  • Crebanine transdermal patch and preparation method thereof
  • Crebanine transdermal patch and preparation method thereof
  • Crebanine transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) The drug-containing adhesive layer is prepared according to the following components by mass: 0.0624 parts of carbanin, 0.03 parts of succinic acid, 0.625 parts of polyacrylic resin pressure-sensitive adhesive, 0.19 parts of diethyl phthalate, glycerin 0.125 parts, 0.03 parts of clove volatile oil;

[0030] (2) Add the grambanine or grambanine hydrochloride in step (1) together with the cross-linking agent, after adding an appropriate amount of ethanol with a concentration of 70v / v%, ultrasonically dissolve it completely, then add the pressure-sensitive adhesive, and wait until it is completely dissolved Add plasticizer, humectant and transdermal penetration enhancer, mix evenly without air bubbles, pour into the mold with backing layer, spread by salivation process, cure in oven at 40°C for 1 hour, dry at room temperature for 12 hours, take it out Affix the paraffin-treated polyethylene protective layer, so that the backing layer, the drug-containing adhesive layer...

Embodiment 2

[0032] (1) The drug-containing adhesive layer is prepared according to the following components by mass: 0.03 parts of gbanine hydrochloride, 0.05 parts of succinic acid, 0.3 parts of polyisobutylene pressure-sensitive adhesive, 0.55 parts of diethyl phthalate, propylene glycol 0.1 part, Caoguo volatile oil and borneol (chemical penetration enhancer) 0.206 part;

[0033] (2) Add the grambanine or grambanine hydrochloride in step (1) together with the cross-linking agent, after adding an appropriate amount of ethanol with a concentration of 80v / v%, ultrasonically dissolve it completely, then add the pressure-sensitive adhesive, and wait until it is completely dissolved Add plasticizer, humectant and transdermal penetration enhancer, mix evenly without air bubbles, pour into the mold with backing layer, spread by salivation process, cure in oven at 40°C for 1 hour, dry at room temperature for 12 hours, take it out Paste the protective layer, the protective layer is made of polys...

Embodiment 3

[0035] (1) The drug-containing adhesive layer is prepared according to the following components by mass: 0.135 parts of carbanin, 0.09 parts of succinic acid, 0.9 parts of silicone pressure-sensitive adhesive, 0.63 parts of diethyl phthalate, 0.3 parts of glycerin 0.007 parts, peppermint volatile oil and clove volatile oil;

[0036] (2) Add the grambanine or grambanine hydrochloride in step (1) together with the cross-linking agent, after adding an appropriate amount of ethanol with a concentration of 85v / v%, ultrasonically dissolve it completely, then add the pressure-sensitive adhesive, and wait until it is completely dissolved Add plasticizer, humectant and transdermal penetration enhancer, mix evenly without air bubbles, pour into the mold with backing layer, spread by salivation process, cure in oven at 40°C for 1 hour, dry at room temperature for 12 hours, take it out Paste the protective layer, the protective layer is made of materials with low surface free energy, the ba...

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Abstract

The invention relates to a crebanine transdermal patch and a preparation method thereof. The crebanine transdermal patch is formed by sequentially overlapping a back lining layer, a medicine-containing adhesive layer and a protective layer, wherein the medicine-containing adhesive layer is prepared from the following components in parts by weight: 0.03 to 0.135 part of crebanine or crebanine hydrochloride, 0.03 to 0.09 part of cross-linking agent, 0.3 to 0.9 part of pressure sensitive adhesive, 0.19 to 0.63 part of plasticizer, 0.1 to 0.3 part of moisturizer, and 0.007 to 0.206 part of percutaneous penetration enhancer. The crebanine transdermal patch has relatively good percutaneous absorption, is more lasting in action time than that of an oral preparation, is more convenient to use than an injection preparation, is good in compliance of patients, and has the characteristics of security, effectiveness, convenience in using, and no irritation and toxicity. Crebanine in the transdermal patch disclosed by the invention is relatively high in cumulative infiltration capacity and can maintain effective blood drug concentration for a longer time, has obvious and lasting antiarrhythmic effect, and overcomes the phenomena that the lasting time of arrhythmia caused by intravenous injection or gastric infusion administration is relatively short and relapse easily occurs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a carbanin transdermal patch with antiarrhythmic effect and a preparation method thereof. Background technique [0002] Cardiac arrhythmia is a common clinical disease, mild cases affect the quality of life and work, and sudden cardiac death caused by malignant arrhythmia such as ventricular tachycardia, ventricular fibrillation, atrial fibrillation, etc. is the main cause of death from cardiovascular diseases. The incidence of the disease has been younger and growing trend. Drugs currently used in clinical prevention and treatment of arrhythmia can be divided into four categories: Category I: sodium ion channel blockers, divided into three subcategories IA, IB, and IC. Class Ⅱ is β-adrenoceptor blockers, such as metoprolol. Class III is a potassium channel blocker, a drug that selectively prolongs the repolarization process. They prolong the action potential durat...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4741A61K47/44A61P9/06
CPCA61K9/7076A61K31/4741
Inventor 马云淑李婧瑜程欣杨子贤陈成徐鹤邓林李俊
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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