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Wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle preparation

A technology of chitosan nanoparticles and wheat germ agglutinin is applied in the field of medicine to achieve the effects of enhancing the therapeutic effect, reducing the dosage and reducing the toxic and side effects

Active Publication Date: 2012-04-11
上海市第八人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far there is no report that salmeterol xinafoate is prepared into nanoparticle preparations

Method used

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  • Wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle preparation
  • Wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle preparation
  • Wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of Wheat Germ Agglutinin-modified salmeterol xinaateroic acid chitosan nanoparticle preparation

[0037] 1) 150 mg of chitosan was dissolved in 100 mL of 0.2% dilute acetic acid aqueous solution to obtain a chitosan solution;

[0038] 2) Dissolve 5 mg of salmeterol xinafoate (Wuhan Yitai Technology Co., Ltd., the same below) in 1 ml of absolute ethanol under heating at 40°C to obtain an ethanol solution of salmeterol xinafoate;

[0039] 3) 25 mg of sodium tripolyphosphate was dissolved in 15 ml of distilled water, and an ethanol solution of salmeterol sinafoate was added thereto to obtain a sodium tripolyphosphate solution containing salmeterol sinafoate;

[0040] 4) Under continuous magnetic stirring at 600 rpm, slowly drop the sodium tripolyphosphate solution containing salmeterol sinafoate into the chitosan solution, and keep stirring for 10 minutes to obtain salmeterol sinafoate Chitosan nanoparticle colloid;

[0041] 5) Add the glutaraldehyd...

Embodiment 2

[0043] Example 2 Preparation of Wheat Germ Agglutinin-modified salmeterol xinafoate chitosan nanoparticle preparation

[0044] 1) 500 mg of chitosan was dissolved in 100 mL of 0.5% dilute acetic acid aqueous solution to obtain a chitosan solution;

[0045] 2) Under the condition of heating at 40°C, 50mg of salmeterol sinafoate was dissolved in 2ml of absolute ethanol to obtain an ethanol solution of salmeterol sinafoate, which was added into the chitosan solution to obtain Chitosan solution of salmeterol naphthalene;

[0046] 3) Dissolve 100mg sodium tripolyphosphate in 15ml distilled water to obtain sodium tripolyphosphate solution;

[0047] 4) Under continuous magnetic stirring at 600 rpm, slowly add the sodium tripolyphosphate solution dropwise into the chitosan solution containing salmeterol sinafoate, and keep stirring for 10 minutes to obtain salmeterol sinafoate Chitosan nanoparticle colloid;

[0048] 5) Add the glutaraldehyde aqueous solution of 3ml 0.3% (v / v) in th...

Embodiment 3

[0050] Example 3 Preparation of salmeterol xinafoate chitosan nanoparticle preparation modified by wheat germ agglutinin

[0051] 1) 900 mg of chitosan was dissolved in 100 mL of 0.8% dilute acetic acid aqueous solution to obtain a chitosan solution;

[0052] 2) Dissolve 300 mg of salmeterol xinafoate in 20 ml of absolute ethanol under heating at 40°C to obtain an ethanol solution of salmeterol xinafoate;

[0053] 3) Dissolve 200 mg of sodium tripolyphosphate in 15 ml of distilled water, and add an ethanol solution of salmeterol xinafoate to obtain a sodium tripolyphosphate solution containing salmeterol xinafoate;

[0054] 4) Under continuous magnetic stirring at 600 rpm, slowly drop the sodium tripolyphosphate solution containing salmeterol sinafoate into the chitosan solution, and keep stirring for 10 minutes to obtain salmeterol sinafoate Chitosan nanoparticle colloid;

[0055] 5) Add the glutaraldehyde aqueous solution of 3ml 0.6% (v / v) in the colloid liquid of salmeter...

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Abstract

The invention provides a wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle preparation and a preparation method thereof, relating to the technical field of medicines. In the invention, an ion cross-linking method is used for preparing salmeterol xinafoate chitosan nanoparticles; and by utilizing the characteristic that the alveolar epithelium has specific sugar receptor N-acetyl glucosamine, wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticles are prepared, so that the specific sugar receptor N-acetyl glucosamine of the alveolar epithelium can be combined through the wheat germ agglutinin to enable the salmeterol xinafoate chitosan nanoparticles to have the targeting property of guiding the alveolar membrane. In-vitro sugar-binding test results show that the wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticles have the advantage of guiding the alveolar membrane, thus the administration dosage can be lowered, and the toxic side effect can be reduced; and by the slow release of the medicament, the effective concentration maintaining time of the medicament in the lung is long, thereby enhancing the treatment effect. The preparation provided by the invention can be used for preparing medicaments for treating asthma, chronic bronchitis or chronic obstructive pulmonary disease.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a preparation of salmeterol xinafoate chitosan nanoparticles modified by wheat germ agglutinin and a preparation method thereof. Background technique [0002] With the accelerated urbanization of lifestyles, the prevalence of asthma is gradually increasing, which will undoubtedly bring huge economic and social burdens. Salmeterol xinafoate is a long-acting adrenergic receptor agonist and a bronchodilator with anti-inflammatory activity. It has a good therapeutic effect on patients with nocturnal asthma and is the first choice for asthma and anti-inflammation. , which is the first major breakthrough in the treatment of asthma in the past 20 years, mainly used for the treatment of asthma, chronic bronchitis and chronic obstructive pulmonary disease. [0003] What is commonly used clinically at present is a kind of salmeterol xinafoate aerosol (salmeterol xinafoate aerosol: Harbin H...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/137A61K47/42A61K47/48A61P11/00A61P11/06
Inventor 李凤前李慧毕娟钱之光
Owner 上海市第八人民医院
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