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Salmeterol xinafoate chitosan nanoparticle preparation modified by wheat germ agglutinin

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

Active Publication Date: 2015-09-02
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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  • Salmeterol xinafoate chitosan nanoparticle preparation modified by wheat germ agglutinin
  • Salmeterol xinafoate chitosan nanoparticle preparation modified by wheat germ agglutinin
  • Salmeterol xinafoate chitosan nanoparticle preparation modified by wheat germ agglutinin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle formulation

[0037] 1) Dissolve 150 mg of chitosan 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) Dissolve 25 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;

[0040] 4) Under continuous magnetic stirring at 600 rpm, the sodium tripolyphosphate solution containing salmeterol xinafoate is slowly added dropwise to the chitosan solution, and stirring is continued for 10 minutes to obtain salmeterol xinafoate Chitosan nanoparticle colloidal liquid;

[0041] 5) Add 3ml of 0.1% (v / v) glutaraldehyd...

Embodiment 2

[0043] Example 2 Preparation of wheat germ agglutinin modified salmeterol xinafoate chitosan nanoparticle formulation

[0044] 1) Dissolve 500 mg of chitosan 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℃, dissolve 50mg of salmeterol xinafoate in 2ml of absolute ethanol to obtain an ethanol solution of salmeterol xinafoate, and add it to the chitosan solution to obtain The chitosan solution of salmeterol nitrate;

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

[0047] 4) Under continuous magnetic stirring at 600 rpm, the sodium tripolyphosphate solution was slowly added dropwise to the chitosan solution containing salmeterol xinafoate, and stirring continued for 10 minutes to obtain salmeterol xinafoate Chitosan nanoparticle colloidal liquid;

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

Embodiment 3

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

[0051] 1) Dissolve 900 mg of chitosan 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 it to obtain a sodium tripolyphosphate solution containing salmeterol xinafoate;

[0054] 4) Under continuous magnetic stirring at 600 rpm, the sodium tripolyphosphate solution containing salmeterol xinafoate is slowly added dropwise to the chitosan solution, and stirring is continued for 10 minutes to obtain salmeterol xinafoate Chitosan nanoparticle colloidal liquid;

[0055] 5) Add 3ml of 0.6% (v / v) glutaraldehyde aqueous solution to the colloidal solut...

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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 is a wheat germ agglutinin-modified salmeterol chitosan nanoparticle preparation and a preparation method thereof. Background technique [0002] With the acceleration of the urbanization of lifestyles, the prevalence of asthma is gradually increasing, which will undoubtedly bring a huge economic and social burden. 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 anti-asthmatic and anti-inflammatory drugs. It is the first major breakthrough in the treatment of asthma in the past 20 years. It is mainly used to treat asthma, chronic bronchitis and chronic obstructive pulmonary disease. [0003] Currently commonly used clinically is a salmeterol xinafoate aerosol (salmeterol xinafoate aerosol: Harbin Huili Pharmaceutical Co., Ltd.), which...

Claims

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Application Information

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Patent Type & Authority Patents(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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