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Biological adhesive lung aspiration nanometer composite microparticle and preparation method thereof

A technology of bioadhesion and composite particles, which is applied in the field of medicine, can solve the problems of inconsistent drug dissolution rate, difficult mixing process, low preparation deposition rate, etc., and achieve the effects of anti-scavenging, prolonging the residence time of the lungs, and easy dispersion

Inactive Publication Date: 2018-11-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the defects of the prior art, and provide a compound lung inhalation powder mist preparation that can effectively solve the problem of inconsistent drug dissolution rate, difficult mixing process and the problem of the drug composition of the drug with large differences in dosage and physical and chemical properties. Bioadhesive compound lung inhalation nanocomposite particle aerosol with low deposition rate, short residence time and fast drug elimination

Method used

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  • Biological adhesive lung aspiration nanometer composite microparticle and preparation method thereof
  • Biological adhesive lung aspiration nanometer composite microparticle and preparation method thereof
  • Biological adhesive lung aspiration nanometer composite microparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Preparation of bioadhesive compound lung inhalation nanocomposite particles (SAS-BUD-HA / MS) comprising salbutamol sulfate (salbutamol sulfate, SAS) and budesonide (budesodine, BUD) nanocrystals

[0059] Weigh 0.5 g of hyaluronic acid, add 100 mL of double-distilled water, stir magnetically until fully swollen and dissolved, then add 250 mg of albuterol and 2 mL of a suspension containing 100 mg of budesonide nanocrystals with a particle size of 200 ± 2 nm, and continue stirring to make the drug Disperse evenly and spray dry. As a control, the raw materials of salbutamol sulfate and budesonide were added in proportion to redistilled water (8%, w / v), dispersed evenly, and spray-dried. The conditions of spray drying are: inlet temperature 160°C, dry air flow rate 35m 3 / h, atomization pressure 414L / h, liquid feed rate 4.5mL / min, prepared bioadhesive pulmonary inhalation nanocomposite particles containing albuterol and budesonide nanocrystals.

[0060] The aero...

Embodiment 2

[0063] Example 2: Preparation of bioadhesive lung inhalation nanocomposite particles (ST-FP-HA / MS) comprising salmeterol (Salmeterol, ST) and fluticasone propionate (Fluticasonepropionate, FP) nanocrystals

[0064] Weigh 1.5g of hyaluronic acid, add 150mL double-distilled water, stir magnetically to make it fully swell and dissolve, then accurately add 120mg of salmeterol and 600mg of fluticasone propionate nanocrystalline suspension with an average particle size of 200±10nm Solution 50mL, continue to stir, make two kinds of medicines disperse evenly in the solution, carry out spray drying. As a control, salmeterol and fluticasone propionate raw materials were added in proportion to redistilled water (10%, w / v), dispersed evenly, and spray-dried. The spray drying conditions are all: the spray drying conditions are all, the inlet temperature is 120°C, and the drying air flow rate is 35m 3 / h, atomization pressure 414L / h, liquid inlet speed 6.0mL / min, obtain the bioadhesive lun...

Embodiment 3

[0068] Example 3: Preparation of bioadhesive lung inhalation nanocomposite particles (VT-FF-CS / MS) comprising Vilanterol (VT) and fluticasone furoate (Fluticasonefuroate, FF) nanocrystals

[0069] Weigh 1.0 g of chitosan as a pharmaceutical excipient, add 150 mL of 0.5% acetic acid aqueous solution and stir until dissolved, then accurately add 67 mg of vilanterol and 50 mL of fluticasone furoate nanocrystal suspension containing 533 mg, stir evenly, and spray dry. As a control, the raw materials of vilanterol and fluticasone furoate were dispersed in double distilled water (5%, w / v) at a ratio of 1:8 for spray drying. Spray drying conditions are: inlet temperature 120 ℃, dry air flow 35m 3 / h, the atomization pressure was 357L / h, and the liquid feed rate was 4.5mL / min, to obtain bioadhesive pulmonary inhalation nanocomposite particles containing itraconazole nanocrystals.

[0070] The aerodynamic particle size and the fraction of fine particles (FPF value) with particle size ...

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Abstract

The invention belongs to the technical field of medicine, and relates to a biological adhesive compound lung aspiration nanometer composite microparticle and preparation thereof. The prepared nanometer composite microparticle is formed by simultaneously embedding nanometer crystals of one or two kinds of water-soluble anti-asthma and chronic pulmonary obstruction medicine and another kind of insoluble anti-asthma and chronic pulmonary obstruction medicine into a biological adhesive framework material. The composite microparticle uses a spray drying technology, and can realize the effects that1, the dissolution difficulty of the insoluble medicine is improved; the synchronous release of several kinds of medicine with different dissolution properties can be realized; the cooperated effectsare better achieved; 2, the uniform mixing of several kinds of medicine with different dose differences can be ensured; the technical process of the preparation is greatly simplified; the medicine quality is improved; the cost is reduced; the energy consumption is reduced; 3, through the application of the biological adhesive material, the lung mucous cilia clearing effect resistance can be effectively realized; the lung retention time is prolonged; the medicine concentration in the focus position is improved; the medicine absorption is delayed; the goals of improving the curative effect and reducing the whole body toxic and side effects can be achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a bioadhesive compound lung suction nanocomposite particle and a preparation method thereof, and also relates to the application of the composite particle in preparing and treating asthma and chronic obstructive pulmonary disease. Background technique [0002] Pulmonary inhalation administration is the most ideal way to treat lung diseases. After inhalation, the drug can be directly deposited on the lesion, and it can take effect quickly and easily reach a higher local drug concentration in the lung. Compared with systemic administration methods such as intravenous injection and oral administration, pulmonary inhalation can also reduce or even avoid toxic and side effects on other non-drug action sites. The clinical treatment of asthma and chronic obstructive pulmonary disease is also preferably given by the pulmonary inhalation route, and glucocorticoids and β-receptor agonists ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/12A61K47/36A61K47/38A61K45/00A61P11/00A61P11/06A61K31/137A61K31/58A61K31/56A61K31/167A61K31/46
CPCA61K9/0075A61K9/12A61K9/146A61K31/137A61K31/167A61K31/46A61K31/56A61K31/58A61K45/00A61K47/36A61K47/38A61K2300/00
Inventor 寸冬梅杨明世刘婷婷韩美华
Owner SHENYANG PHARMA UNIVERSITY
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