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Multi-component crystalline particles for inhalation therapy

A multi-component crystallization and particle technology, applied in inhalers, drug combinations, drug devices, etc., to reduce the impact of the system, eliminate deposition and accumulation

Inactive Publication Date: 2015-09-30
CIRCASSIA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, WO2005 / 0105043 (Vectura Limited) states that glycopyrronium has serious problems with its stability and that the presence of amorphous or amorphous glycopyrronium bromide species can lead to significant physical instability

Method used

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  • Multi-component crystalline particles for inhalation therapy
  • Multi-component crystalline particles for inhalation therapy
  • Multi-component crystalline particles for inhalation therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1: Glycopyrronium bromide (GB) and formoterol fumarate (FF)

[0064] A methanolic solution of GB / FF was prepared and added to recirculating TBME at room temperature using a crude probe based system at 0.5ml / min addition rate, solution / non-solvent 1 / 20, using 40w ultrasonic power. Immediate recrystallization and formation of a homogeneous slurry was observed in all cases. The material isolated by filtration was crystalline as shown by differential scanning calorimetry (DSC).

[0065] For GB:FF (7.5:1) in MeOH / TBME, the experimental parameters are as follows.

[0066] Solution concentration: 25% (6.8g, in 27ml methanol)

[0067] Volume TBME : 648ml

[0068] Solution-non-solvent ratio: 1 / 24 V / V

[0069] Reaction vessel temperature : 7.4 + / - 0.2 ℃

[0070] Solution adding rate: 0.5ml / min

[0071] Solution adding speed: 0.042m / s

[0072] Solution feeding tube diameter: 0.5mm

[0073] Adding time: 60min

[0074] Recirculation rate: 0.9L / min

[0075] Rec...

Embodiment 2

[0093] Embodiment 2: Glycopyrronium bromide (GB) and salmeterol xinafoate (SX)

[0094] Methanol solutions of GB / SX were prepared at different ratios (4:1, 2:1 and 1:1) and using a crude probe based system using 40W US power at 0.5ml / min addition rate, solution / non-solvent 1 / 20, added to recycle DIPE at room temperature. Immediate recrystallization and formation of a homogeneous slurry was observed in all cases. Material isolated by filtration was crystalline as shown by DSC.

[0095] For GB:SX (2:1) in MeOH / DIPE, the experimental parameters are as follows.

[0096] Solution concentration: 25% (6.8g, in 27ml methanol)

[0097] Volume DIPE : 648 ml

[0098] Solution-non-solvent ratio: 1 / 24 V / V

[0099] Reaction vessel temperature : 7.4 + / - 0.2 ℃

[0100] Solution adding rate: 0.5ml / min

[0101] Solution adding speed: 0.042 m / s

[0102] Solution feeding tube diameter: 0.5mm

[0103] Adding time: 60mins

[0104] Recirculation rate: 2.63L / min

[0105] Recirculatio...

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Abstract

Pharmaceutical Preparations Multi-component crystalline particles and compositions, methods for their preparation, their uses in inhalation therapy and inhaler devices containing said particles are provided, in particular particles comprising glycopyrrolate. The particles can be prepared substantially free of excipients and agents other than active agents or their precursors in the presence of ultrasonic irradiation in a process comprising contacting a solution in a first flowing stream with an anti-solvent in a re-circulating second flowing stream, causing the mixing thereof and collecting crystals that are generated.

Description

field of invention [0001] The present invention relates to the preparation of multicomponent crystalline particles of active agents suitable for inhalation therapy and delivery by oral or nasal inhalation, wherein the particles can be prepared substantially free of excipients and other inactive agents. The invention also provides granules and formulations prepared according to the method of the invention and their use in medicine. Background of the invention [0002] The development of inhaled combination products raises the important pharmaceutical issue of maintaining a controllable ratio of drug components during different stages of drug formulation and drug delivery. Targeted substance mixtures have been obtained using formulated products resulting from physical mixtures of active ingredients. However, co-deposition of active substances from aerosols can lead to inconsistencies in deposition ratios in different regions of the lung despite the use of precisely formulate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61K31/4015A61K31/4196A61P11/00
CPCA61K31/4015A61K31/4196A61K31/137A61K31/40A61K31/138A61K31/167A61P11/00A61P11/06A61P43/00A61K2300/00A61M15/009A61M15/08A61K9/0078A61K9/0075A61K9/008A61M2202/064
Inventor J.伯恩斯D.帕里克S.卡尔基
Owner CIRCASSIA
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