Improved inhalable agglomerates

A technology of aggregates and drugs, applied in the field of medicine, can solve the problems of unfavorable drug clinical applications, side effects, and decreased efficiency of drug delivery to the lungs

Pending Publication Date: 2022-04-15
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In a preferred embodiment, in order to allow glycopyrronium bromide, one of the APIs, to be preferentially delivered to the large airways where muscarinic receptors are located, the crystal particle size of glycopyrronium bromide is significantly larger than that of other drugs, but this also leads to The decrease in the efficiency of drug delivery to the lungs is partly due to increased deposition in the oropharynx, which may cause potential side effects that are not conducive to the clinical application of the drug (AAPS PharmSciTech(2019) 20:103)

Method used

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  • Improved inhalable agglomerates

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] The preparation of embodiment 1 micronization active agent particle

[0120] The active agent is micronized using the MCONE pulverizer of Italian DEC company, and parameters such as crushing pressure, feeding pressure and feeding speed are limited according to the task requirements, so as to obtain the active agent particles with the target particle size. The particle size was measured using a SYMPATEC particle size analyzer with a 4 bar dispersion pressure. The particle size results are shown in Table 1 and Table 2.

[0121] Table 1 API particle size distribution

[0122]

[0123]

[0124] Table 2 API particle size distribution

[0125] X10(μm) X50(μm) X90(μm) fluticasone furoate 0.52 1.98 4.43 Glycopyrrolate 0.61 1.83 3.71 indacaterol acetate 0.68 1.93 3.68

Embodiment 2 3

[0126] The preparation of embodiment 2 three-component inhalation dry powder A

[0127] Disperse 40 g of distearoylphosphatidylcholine (DSPC) and 3.72 g of calcium chloride dihydrate in hot deionized water (T=70° C.), using an ULTRA-TURRAX TM high-shear mixer (T-25 model )8000rpm for 3 minutes. Subsequently, an appropriate amount of PFOB was added dropwise to the resulting DSPC / CaCl while shearing and mixing. 2 In the dispersion, the resulting DSPC / CaCl 2 The / PFOB dispersion was subjected to high-pressure homogenization for three rounds to obtain a blank carrier emulsion. The resulting emulsion is spray-dried on a BüCHI B-290 micro-spray dryer, spray-drying parameters: inlet temperature = 120°C, peristaltic pump speed: 5-7rpm (~ 2mL / min), fan frequency: 100%, atomizer flow Velocity = 60 cm (rotameter), to obtain porous carrier particles, the particle size of the carrier particles is shown in Table 3.

[0128] Table 3 particle size distribution of porous carrier particles ...

Embodiment 3 3

[0132] The preparation of embodiment 3 three-component inhalation dry powder B

[0133] Porous carrier particles were prepared by a method similar to that of Example 2, except that the target amount of fluticasone furoate was dispersed in hot deionized water together with distearoylphosphatidylcholine (DSPC) and calcium chloride dihydrate. The resulting porous carrier particles comprise fluticasone furoate as a core embedded in a porous phospholipid interface layer.

[0134] Weigh the indacaterol acetate, glycopyrronium bromide and drug-containing porous carrier in Table 1 that have been micronized, spray-dry them on a BüCHI B-290 micro-spray dryer after high-shearing in perfluorooctylbromide antisolvent, and enter Temperature=140°C, peristaltic pump speed: 5-7rpm (~2mL / min), fan frequency: 100%, atomizer flow rate=46cm (rotameter), and inhalation dry powder B was obtained.

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Abstract

The present invention relates to improved inhalable agglomerates. In particular, the present invention relates to active agent particles comprising porous support particles and micronized active agent particles. By reasonably controlling the particle size of the active agent, the preparation has excellent pulmonary delivery efficiency and can be used for inhalation treatment of pulmonary diseases.

Description

technical field [0001] The disclosure belongs to the field of medicine, and relates to a dry powder pharmaceutical preparation for pulmonary delivery and a preparation method. Background technique [0002] Active pharmaceutical ingredients (APIs) useful in the treatment of respiratory diseases are formulated for administration, typically by inhalation of portable inhalers. The two most common types of portable inhalers are pressurized metered dose inhalers (pMDIs) and dry powder inhalers (DPIs). [0003] The vast majority of dry powder inhalers rely on the patient's inspiratory force to fluidize and disperse the drug particles. For effective drug deposition in the lung, it is widely accepted that particles must have an aerodynamic diameter between 1 μm and 5 μm. Accordingly, APIs are typically micronized to obtain fine particles with a mass median diameter in this size range. Unfortunately, finely micronized drug particles generally exhibit poor powder flowability, fluidi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/16A61K45/06A61K47/24A61K47/02A61K31/56A61P11/00A61K31/4704A61K31/40
Inventor 陆绘孙姣潘凯孙琼李金宇杨玉霞赵平
Owner JIANGSU HENGRUI MEDICINE CO LTD
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