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Prepn process of superfine inhaled glucocorticoid medicine powder

A glucocorticoid and drug technology, applied in the field of ultrafine drug powder, can solve the problems of inability to obtain budesonide with controllable particle size, inability to prepare budesonide, complicated production process, etc. Bioavailability, Efficiency of Dispensing Formulations

Inactive Publication Date: 2007-06-06
BEIJING UNIV OF CHEM TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The method introduced in this patent can prepare crystalline budesonide particles with high purity, but it cannot prepare budesonide with controllable morphology, let alone ultrafine or nano budesonide with controllable particle size
Therefore, in order to obtain budesonide particles suitable for pulmonary inhalation administration, post-processing must be performed, which not only complicates the production process, but also greatly increases the production cost.

Method used

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  • Prepn process of superfine inhaled glucocorticoid medicine powder
  • Prepn process of superfine inhaled glucocorticoid medicine powder
  • Prepn process of superfine inhaled glucocorticoid medicine powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Weigh 2.5g of budesonide raw material, dissolve it with methanol to prepare 100ml of budesonide solution, put it in storage tank 1, weigh 0.21g of tyloxabe, prepare 700mL of tyloxabe solution with deionized water and put it in the storage tank 2. Control the temperature at about 5°C. Under the stirring condition of a magnetic stirrer, quickly pour the methanol solution of budesonide into the aqueous solution of Tyloxabe to obtain milky white budesonide precipitate, continue to stir for 30 minutes, filter and wash , Budesonide dry powder granules were obtained after vacuum drying at 60°C. It can be seen from the scanning electron microscope photo shown in Fig. 3 that the average particle size is 3 μm, and more than 80% of the particles have a particle size of 1-5 μm. It can be seen from the XRD spectrum shown in Figure 4 that what is obtained is crystalline budesonide. In the experiment, the ratio of budesonide solution and aqueous solution was 1:7.

Embodiment 2

[0048] Weigh 2.5g of budesonide crude drug, dissolve with methanol to prepare 100ml of budesonide solution, place it in storage tank 1, weigh 0.25g of hydroxypropyl cellulose, prepare 1000mL of hydroxypropyl cellulose solution with deionized water, place In storage tank 2, control the temperature at about 5°C, and under the stirring condition of a magnetic stirrer, quickly pour the methanol solution of budesonide into the aqueous solution of hydroxypropyl cellulose to obtain a milky white budesonide precipitate, and stir for a period of time Afterwards, filter, wash, and vacuum-dry at 60° C. to obtain budesonide dry powder granules. It can be seen from the scanning electron microscope photo shown in Figure 5 that the average particle size is between 1 and 5 μm. In the experiment, the ratio of budesonide solution and aqueous solution was 1:10.

Embodiment 3

[0050] Weigh 2.5g of budesonide raw material, dissolve it in methanol to prepare 100ml of budesonide solution, place it in storage tank 1, measure 1000mL deionized water with a graduated cylinder and place it in storage tank 2, control the temperature at about 5°C, and stir under magnetic force Under the condition of agitator stirring, the methanol solution of budesonide was quickly poured into deionized water to obtain a milky white budesonide precipitate, which was stirred for a period of time, filtered, washed, and vacuum-dried at 60°C to obtain budesonide dry powder particles. It can be seen from the scanning electron microscope photo shown in Figure 6 that the average particle size is between 1 and 5 μm. In the experiment, the ratio of budesonide solution and aqueous solution was 1:10.

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Abstract

The preparation process of superfine inhaled glucocorticoid medicine powder belongs to the field of medicine micronizing technology. The preparation process includes the following steps: compounding glucocorticoid medicine solution in selected solvent and in the concentration of 70 %-99 % that of corresponding saturation solution at the same temperature; selecting proper counter solvent and compounding counter solvent solution with surfactant of the concentration 0.01-10 wt% as the precipitating phase; mixture the glucocorticoid medicine solution and the precipitant to separate out the medicine at 0-50 deg.c; collecting the re-crystallized slurry, stirring, filtering and vacuum drying at vacuum degree of 0.8-1.0 MPa and temperature of 30-110 deg.c to obtain crystalline powder. The present invention can obtain superfine powder with controllable shape, narrow size distribution and high dispersivity.

Description

technical field [0001] The invention discloses a method for preparing ultrafine inhalation-type glucocorticoid drug powder particles and the ultrafine drug powder prepared by the method, belonging to the field of drug micronization. Background technique [0002] Among the currently known anti-inflammatory anti-asthmatic drugs, glucocorticoids (GCS) have the strongest anti-inflammatory effect, but systemic application of GCS will cause many serious adverse reactions, which limits its application in the treatment of asthma . Inhaled glucocorticoids (IGCS) mainly act on local lung tissue, and can exert a strong anti-inflammatory effect in the airway. Due to the small dosage, they can avoid or reduce systemic side effects. The drug of choice for asthma has a tendency to gradually replace systemic application of GCS. [0003] Currently commonly used IGCS mainly budesonide and beclomethasone dipropionate. The research report on the anti-asthma drug market in 2005 showed that am...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/70A61K45/00A61K31/58A61K31/573A61K47/00A61P29/00A61P11/06A61P11/00
Inventor 陈建峰降立川王哲乐园甄崇礼
Owner BEIJING UNIV OF CHEM TECH