Ligustrazine film coating agent and preparation method thereof

A technology of ligustrazine and film-coating agents, which is applied in the direction of anti-toxic agents, anti-inflammatory agents, and pharmaceutical formulations, can solve the problems of cumbersome preparation process, large coating area, and inconvenient use, and reduce toxic and side effects and adhesion Strong, reduce the effect of water evaporation

Active Publication Date: 2020-02-14
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The relevant research and development of Ligustrazine transdermal preparations at home and abroad have disclosed Ligustrazine liposome type and microemulsion type controlled release transdermal administration. Due to the cumbersome and unstable preparation process, there are deficiencies such as difficulty in industrialization.
In addition, the ligustrazine patch currently developed has a limited drug loading capacity, and the coating area is large in clinical application, which is inconvenient to use

Method used

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  • Ligustrazine film coating agent and preparation method thereof
  • Ligustrazine film coating agent and preparation method thereof
  • Ligustrazine film coating agent and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0035] The invention provides the preparation method of the ligustrazine coating agent, comprising the following steps: 1) mixing water with a film-forming material, sealing, soaking and swelling, and swelling in a water bath to obtain a film-forming matrix; 2) mixing plasticizer, The organic solvent, ligustrazine, surfactant and penetration enhancer are mixed with the film-forming matrix prepared in step 1) to obtain ligustrazine coating agent.

[0036]In the present invention, water is mixed with polyvinyl alcohol, and after sealing, soaking and swelling, the water bath is swollen to obtain a film-forming matrix. In the present invention, the time for the sealing infiltration and swelling is preferably 20-28 hours, more preferably 22-26 hours, most preferably 24 hours; the sealing infiltration and swelling is natural swelling, and the temperature of the sealing infiltration and swelling is not limited. Room temperature is fine. In the present invention, after the seal is in...

preparation example 1

[0040] The composition of raw materials is as follows:

[0041]

[0042] The preparation method comprises the following steps:

[0043] (1) Take 80g of ultrapure water, seal and infiltrate 5g of polyvinyl alcohol for 24 hours, let it swell naturally, swell in a water bath at 90°C for 2 hours to gel, take it out and let it cool for later use, and obtain a film-forming matrix;

[0044] (2) Add 5.78g ligustrazine to the film-forming matrix in step (1) while stirring, then slowly add 11.046g ethanol solution, 3.132g glycerin, 1.02g Tween-80, 1.15g azone and 8.545g Ultrapure water, stirred to disperse evenly to obtain 114.845 mL of ligustrazine coating agent.

preparation example 2

[0046] The composition of raw materials is as follows:

[0047]

[0048] The preparation method comprises the following steps:

[0049] (1) Take 60g of ultrapure water, seal and infiltrate 13.5g of polyvinyl alcohol for 24 hours, let it swell naturally, swell in a water bath at 90°C for 2 hours to gel, take it out and let it cool for later use, and obtain a film-forming matrix;

[0050] (2) Add 8.68g ligustrazine to the film-forming matrix in step (1) while stirring, then slowly add 23.25g ethanol solution, 5.24g glycerol, 0.69g Tween-80, 0.46g azone and 3.853g Ultrapure water, stirred to disperse evenly to obtain 117.703 mL of ligustrazine coating agent.

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Abstract

The invention provides a ligustrazine film coating agent and a preparation method thereof, which belong to the technical field of film coating agent preparation, and the ligustrazine film coating agent comprises the following components in parts by weight: 3-20 parts of ligustrazine, 3-15 parts of a film forming material, 2-10 parts of a plasticizer, 5-25 parts of an organic solvent, 0.1-1 part ofa surfactant, 0.3-1.3 parts of a penetration enhancer, and 27.7-86.6 parts of water. The ligustrazine film coating agent provided by the invention has the advantages of quick effect, lasting effect,good spreading property, strong adhesive force, no irritation to skin, and convenience in administration; the ligustrazine film coating agent is administrated in a transdermal manner, has the characteristics of high safety, good compliance and large sample loading capacity, can continuously and stably release medicines within specified time, is stable in blood concentration, and fundamentally eliminates the defects of ligustrazine injections and tablets.

Description

technical field [0001] The invention belongs to the technical field of preparation of film-coating agents, and in particular relates to a film-coating agent of ligustrazine and a preparation method thereof. Background technique [0002] Cerebrovascular disease is the manifestation of systemic vascular disease or systemic vascular disease in the brain. Among them, stroke refers to the limited or comprehensive brain function defect syndrome caused by acute cerebral circulation disorder, also known as acute cerebrovascular disease. Stroke is generally divided into hemorrhagic stroke and ischemic stroke, which are often referred to as cerebral hemorrhage and cerebral infarction. At present, cerebrovascular disease has become the primary cause of disability and death in China, and the wave of population aging also makes its incidence increase year by year. In addition, cerebrovascular disease has the characteristics of high morbidity, high mortality, high disability rate and hi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4965A61K47/10A61K47/26A61K47/32A61K47/36A61P1/16A61P7/02A61P9/00A61P9/10A61P13/12A61P29/00A61P35/00A61P39/02
CPCA61K9/7015A61K31/4965A61K47/36A61K47/32A61K47/10A61K47/26A61P9/10A61P7/02A61P9/00A61P1/16A61P13/12A61P35/00A61P29/00A61P39/02
Inventor 杨志斌王颖何雅楠张成桂刘衡赵海荣赵昱
Owner DALI UNIV
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