Budesonide nanocrystal, preparation method and application in atomization inhalation administration

A nanocrystal, atomization inhalation technology, applied in nanotechnology, nanotechnology, nano-optics and other directions, can solve the problems of clogging the vibrating mesh, not recommended, etc., to improve compliance, relieve asthma symptoms, and achieve the effect of small medication volume

Inactive Publication Date: 2017-11-24
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the mesh size of the vibrating mesh nebulizer is in the micron range (such as 3-8 μm), the particle size of the drug in the existing budesonide nebulized inhalation suspension (Pulmicort) is mostly 1-5 μm, Vibrating mesh nebulizer mist is not recommended for nebulized drug delivery due to possible clogging of vibrating mesh

Method used

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  • Budesonide nanocrystal, preparation method and application in atomization inhalation administration
  • Budesonide nanocrystal, preparation method and application in atomization inhalation administration
  • Budesonide nanocrystal, preparation method and application in atomization inhalation administration

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Embodiment 1

[0033] The preparation of embodiment 1 budesonide nanocrystal

[0034] Dissolve 0.5 g of budesonide in 20 ml of ethanol, filter through a 0.22 μm microporous membrane to obtain sterile solution 1, and pre-cool to 0°C for later use;

[0035] Dissolve 0.2g of Tween 80 in water for injection, filter through a 0.22μm microporous membrane to obtain sterile solution 2, and pre-cool to 0°C for later use;

[0036] Add the pre-cooled solution 1 to the pre-cooled solution 2 at -15°C under stirring, continue to stir for 4 minutes, collect budesonide nanocrystals after centrifugation, and wash with a small amount of water for injection to obtain the budesonide Ned nanocrystals.

Embodiment 2

[0037] The preparation of embodiment 2 budesonide nanocrystals

[0038] Dissolve 5 g of budesonide in 50 ml of ethanol, filter through a 0.22 μm microporous membrane to obtain sterile solution 1, and pre-cool to 3°C for use;

[0039] Dissolve 2 g of Poloxamer 188 in water for injection, filter through a 0.22 μm microporous membrane to obtain sterile solution 2, and pre-cool to 3°C for use;

[0040] Add the pre-cooled solution 1 to the pre-cooled solution 2 at -20°C under stirring, continue stirring for 4 minutes, collect budesonide nanocrystals after centrifugation, and wash with a small amount of water for injection to obtain the budesonide Ned nanocrystals.

Embodiment 3

[0041] Example 3 Budesonide atomized inhalation nanosuspension

[0042] The prescription of budesonide nebulized inhalation nanosuspension is as follows:

[0043]

[0044] Preparation method:

[0045] Dissolve the prescribed amount of Tween 80, sodium chloride, and EDTA-2Na in water for injection, adjust the pH to 4.0 with dilute hydrochloric acid, and filter through a 0.22 μm microporous membrane to obtain a sterile solution;

[0046] Add budesonide nanocrystals to the above sterile solution, and add water for injection to a prescribed volume of 1000ml;

[0047] The above-mentioned nanocrystal suspension is divided into low-density polyethylene small tubes, sealed, and 0.2ml per tube is obtained.

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Abstract

The invention discloses a budesonide nanocrystal, a preparation method and application in atomization inhalation administration. The preparation method of the budesonide nanocrystal comprises the following steps: (1) dissolving budesonide into ethanol, filtering with a 0.22 [mu]m micro-porous membrane to obtain solution 1 and pre-cooling the solution 1 to the temperature of 0-3 DEG C; (2) dissolving a dispersing agent or a stabilizing agent into water for injection, filtering with a 0.22 [mu]m micro-porous membrane to obtain solution 2 and pre-cooling the solution 2 to the temperature of 0-3 DEG C for later use; and (3) stirring at the temperature of (-15)-(-20) DEG C, adding the pre-cooled solution 1 into the pre-cooled solution 2, stirring for 3-5 min and collecting budesonide nanocrystals used for preparing budesonide nano-suspension for atomization inhalation. The budesonide nanocrystals can be better distributed on the surface of a bronchus or a lung and have the beneficial effects of rapidly taking effect and rapidly relieving an asthma symptom; the nano-suspension can be atomized by a vibration net-type atomizer, so that the drug use area is small, the atomization treatment time is short, and the drug utilization ratio is high; and therefore, the drug taking compliance of patients can be improved, and the side effects of drugs can be reduced.

Description

technical field [0001] The invention relates to a budesonide preparation. technical background [0002] As my country's population aging process accelerates and environmental pollution intensifies, the incidence of respiratory diseases, mainly asthma and chronic obstructive pulmonary disease (COPD), has increased significantly. Inhalation administration can directly deliver the drug to the bronchi and lungs. While improving the therapeutic effect, it can greatly reduce the oral dosage and reduce the systemic side effects of the drug. Therefore, it is currently the preferred route of administration for the treatment of asthma and COPD. [0003] Since asthma is a chronic airway inflammatory disease involving a variety of inflammatory cells, anti-inflammation is the key to the maintenance treatment of asthma, and inhaled glucocorticoids are one of the first-choice treatments for long-term maintenance treatment of asthma. [0004] Budesonide is a glucocorticoid with highly effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/58B82Y20/00A61K9/72A61K9/10A61P11/06A61P11/00
CPCC07J71/0031A61K9/0078A61K9/10A61K47/10A61K47/26B82Y20/00C07B2200/13
Inventor 王健侯惠民康彬丁云娜
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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