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Method for preparing salmeterol transdermal patch

A technology of transdermal patch and penetration enhancer, applied in the field of prevention and treatment of asthma, salmeterol transdermal patch, can solve the problems of complex preparation process and drug delivery device

Inactive Publication Date: 2018-04-06
ZHENGZHOU TAIFENG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process and drug delivery device of the inhalation preparation are complicated

Method used

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  • Method for preparing salmeterol transdermal patch
  • Method for preparing salmeterol transdermal patch
  • Method for preparing salmeterol transdermal patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 1.0 g of salmeterol, add 50.0 g of ethyl acetate to dissolve, add 20.0 g of laurocapram, stir and mix, then add 929.0 g of acrylic pressure-sensitive adhesive solution, mix and stir for 1 hour, and use a vacuum pump to remove air bubbles to obtain a uniform Colloidal solution, put on the coating machine, adjust the coating thickness to 0.1mm, coat on the backing layer, dry at 60°C for 2 hours, press with PET polyester film, divide into 2cm×2cm size (0.1mg / paste) , ready to pack. The resulting patch was applied to the back of depilated mice for 24 hours. Percent drug permeability was calculated by high performance liquid chromatography measuring the amount of drug in the patch before and 24 hours after application of the salmeterol patch.

Embodiment 2

[0020] Weigh 1.0 g of salmeterol, add 150.0 g of petroleum ether to dissolve, then add 50.0 g of oleic acid, stir and mix, add 799.0 g of silicone pressure-sensitive adhesive, mix and stir for 1 hour, and vacuum pump to remove air bubbles to obtain a uniform colloidal solution. Put it on the coating machine, adjust the coating thickness to 0.1mm, coat it on the backing layer, dry it at 60°C for 2 hours, press it with PET polyester film, divide it into 2cm×2cm size (0.1mg / paste), and pack it. . The resulting patch was applied to the back of depilated mice for 24 hours. Percent drug permeability was calculated by high performance liquid chromatography measuring the amount of drug in the patch before and 24 hours after application of the salmeterol patch.

Embodiment 3

[0022] Weigh 1.0 g of salmeterol, add 125.0 g of dichloromethane to dissolve, add 30.0 g of propylene glycol, stir and mix, add 844.0 g of polyisobutylene pressure-sensitive adhesive, mix and stir for 1 hour, and vacuum pump to remove air bubbles to obtain a uniform colloidal solution , on the coating machine, adjust the coating thickness to 0.1mm, coat on the backing layer, dry at 60°C for 2 hours, press it with PET polyester film, divide it into 2cm×2cm (0.1mg / paste), pack it have to. The resulting patch was applied to the back of depilated mice for 24 hours. Percent drug permeability was calculated by high performance liquid chromatography measuring the amount of drug in the patch before and 24 hours after application of the salmeterol patch.

[0023] The drug permeability and other parameters of Example 1, Example 2, and Example 3 were compared. The types and contents of pressure-sensitive adhesives, solvents, and penetration enhancers used in different examples were diff...

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PUM

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Abstract

The invention discloses a salmeterol transdermal patch, which contains salmeterol and its salts, a pressure-sensitive adhesive, a penetration enhancer, a solvent, and contains 0.05% to 0.1% of salmeterol and its salts, Sensitive glue 74.9%~98.5%, penetration enhancer 0.5~10%, solvent 1%~15%. It has excellent properties in transdermal absorption rate, mechanical properties and preparation process, and is used for the prevention and treatment of asthma.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to the preparation of salmeterol, in particular to a preparation made by mixing a penetration enhancer, a solvent, and a pressure-sensitive adhesive according to a certain ratio, and is characterized in transdermal absorption rate, mechanical properties, preparation process, etc. Salmeterol transdermal patch with excellent properties for the prevention and treatment of asthma. Background technique [0002] Salmeterol is a long-lasting, highly selective beta-beta drug developed by GlaxoSmithKline 2 Adrenergic receptor agonist, with obvious bronchodilator effect, is used for long-term conventional treatment of reversible airway obstruction and chronic bronchitis of asthma, and can also be used for patients who need to routinely use bronchodilators, and prevent nocturnal asthma attack or control day Instable asthma (such as before exercise or exposure to allergens), with strong efficac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/32A61K47/34A61K47/14A61K47/22A61K47/12A61K47/10A61K47/08A61K47/06A61K31/137A61P11/06
CPCA61K9/7061A61K9/0004A61K9/7053A61K9/7069A61K31/137A61K47/06A61K47/08A61K47/10A61K47/12A61K47/14A61K47/22
Inventor 杨艳丽沙薇常新义
Owner ZHENGZHOU TAIFENG PHARMA CO LTD
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