Low-density amorphous carrier particles and its preparation method and application

A carrier particle, amorphous technology, which is applied in the directions of non-active medical preparations, pharmaceutical formulations, non-active components of polymer compounds, etc., can solve problems such as poor fluidity, achieve good fluidity, improve the effective deposition rate of drugs, The effect of high thermodynamic stability

Active Publication Date: 2021-03-02
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Carrier-free powder aerosol is composed of a certain dose of drug micropowder alone. Due to the unique physiological structure of the respiratory tract, the particle size of the drug micropowder is generally required to be 0.5-5 μm. The drug with this particle size is affected by the physical and chemical properties of the drug itself, such as electrostatic attraction. poor liquidity

Method used

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  • Low-density amorphous carrier particles and its preparation method and application
  • Low-density amorphous carrier particles and its preparation method and application
  • Low-density amorphous carrier particles and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Erythritol and hydroxypropyl-β-cyclodextrin were mixed according to different mass ratios (100:0, 80:20, 70:30, 60:40, 40:60, 30:70, 20:80, 0: 100) dissolved in water, respectively prepared into a solution with a concentration of 50mg / ml (the total concentration of erythritol and hydroxypropyl-β-cyclodextrin), and then using a spray dryer to spray dry the above solution to prepare carrier particles, The conditions of spray drying are as follows: the inlet air temperature is 130°C, the outlet air temperature is 85°C, the pump liquid rate is 7ml / min, the nozzle diameter is 0.71mm, the atomization pressure is 120Kpa, and the air flow rate is 0.60m 3 / h. The erythritol carrier particles obtained under these conditions were evaluated or characterized as follows.

[0061] (1) Density measurement: bulk density and tap density are important properties of dry powder inhalation formulations. The specific method is: put a certain amount of powder (about 100mg) of known mass into...

Embodiment 2

[0084] Dissolve small molecule sugar alcohols (trehalose, raffinose, erythritol, xylitol, lactose) and hydroxypropyl-β-cyclodextrin in water at a mass ratio of 40:60, and prepare concentrations of 50mg / ml (the total concentration of small molecular sugar alcohol and hydroxypropyl-β-cyclodextrin), then adopt a spray dryer to spray dry the above solution to prepare carrier particles. The conditions of spray drying are as follows: the inlet air temperature is 130°C, outlet air temperature 85°C, pump liquid rate 7ml / min, nozzle diameter 0.71mm, atomization pressure 120Kpa, air flow 0.60m 3 / h.

[0085] (1) See Table 2 for the particle size, bulk density, crystal form, and glass transition temperature (Tg) of different composite carrier particles after spray drying (the test method is the same as in Example 1). The results showed that the particle size of the composite carrier particles prepared by spray drying with different small molecule sugar alcohols and hydroxypropyl-β-cyclo...

Embodiment 3

[0097] Small molecular sugar alcohol (raffinose or erythritol) and hydroxypropyl-β-cyclodextrin are dissolved in water at a mass ratio of 40:60, and the concentration is respectively prepared to be 50mg / ml (small molecular sugar alcohol and The total concentration of hydroxypropyl-β-cyclodextrin) solution, and then use a spray dryer to spray dry the above solution to prepare carrier particles. The conditions of spray drying are as follows: the inlet air temperature is 130°C, and the outlet air temperature is 85°C , the pump liquid rate is 7ml / min, the nozzle diameter is 0.71mm, the atomization pressure is 120Kpa, and the air flow rate is 0.60m 3 / h. Then the carrier particles were equally divided into 3 parts, and two of them were placed under accelerated stability conditions (40° C., 75% RH) for 5 days and 10 days respectively. Then the raffinose and erythritol carrier particles on day 0 and the raffinose and erythritol carrier particles after being placed under accelerated ...

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Abstract

The invention relates to a low-density amorphous carrier particle, its preparation method and application. The amorphous carrier particle is prepared by spray-drying a small molecule sugar alcohol, hydroxypropyl-β-cyclodextrin and a solvent, and the small molecule sugar alcohol is selected from trehalose, raffinose, erythritol At least one of xylitol, sorbitol and lactose; the mass ratio of the small molecule sugar alcohol and hydroxypropyl-β-cyclodextrin is 90:10-10:90. The amorphous carrier particle of the present invention has the characteristics of low density, stable amorphous state, high physical and chemical stability, good fluidity, and insensitivity to humidity. Using it as a dry powder inhaler carrier can effectively improve the atomization and The delivery performance can effectively improve the effective deposition rate of the dry powder inhaler, greatly improve the bioavailability and efficacy of the drug in the lungs, and reduce the storage environment requirements of the dry powder inhaler.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a low-density amorphous carrier particle and a preparation method and application thereof. Background technique [0002] The pulmonary drug delivery system (PDDS) delivers granular drugs to the lungs through a special drug delivery device and enters the human body in a non-invasive manner, which can effectively achieve targeted pulmonary drug delivery, systemic drug delivery and Macromolecular drug delivery. There are 300-400 million alveoli in the lungs, and the area of ​​the respiratory tract is as high as 70-140m 2 area, and the thickness of alveolar epithelial cell wall or capillary wall is only 0.5-1 μm, the distance of drug exchange is very short, the membrane permeability is high, the absorption speed is fast, and the drug can easily penetrate the alveoli, so that the active ingredient can be delivered quickly; The submucosal alveolar capillary networ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/26A61K47/40A61K9/72
CPCA61K9/0075A61K9/1623A61K9/1652
Inventor 李革赵紫玉张雪娟廖秋莹崔影彤陈航平
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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