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A kind of ciclesonide formoterol tiotropium bromide compound dry powder inhalation composition

A dry powder inhaler, tiotropium bromide technology, applied in the field of β2-receptor agonist and anticholinergic drug compound dry powder inhaler, glucocorticoid, can solve the problem of easy to generate static electricity, serious particle agglomeration, unfavorable dry powder inhalation Dosage configuration and other issues to achieve the effect of easy crushing and high lung deposition rate

Active Publication Date: 2021-01-29
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] When using ciclesonide crystal form II as the active ingredient to prepare dry powder inhalers, many difficulties were found, for example: static electricity is easily generated when ciclesonide crystal form II is crushed, and the particle agglomeration is serious, which is not conducive to the configuration of dry powder inhalers
In addition, the lung deposition rate of the configured ciclesonide dry powder inhaler is not ideal
[0007] When using ciclesonide crystal form II as the active ingredient to prepare dry powder inhalers, many difficulties were found, for example: ciclesonide crystal form II is easy to generate static electricity when crushed, and the particles agglomerate seriously, which is not conducive to the configuration of dry powder inhalers
In addition, the lung deposition rate of the configured ciclesonide dry powder inhaler is not ideal

Method used

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  • A kind of ciclesonide formoterol tiotropium bromide compound dry powder inhalation composition
  • A kind of ciclesonide formoterol tiotropium bromide compound dry powder inhalation composition
  • A kind of ciclesonide formoterol tiotropium bromide compound dry powder inhalation composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Invention Example 1 Preparation of Ciclesonide Monohydrate by Supercritical Method

[0046] (1) Prepare ciclesonide solution 1: Dissolve 5g ciclesonide completely in a mixed solution of 200ml acetone and 20ml water at 50°C;

[0047] (2) Connect the ciclesonide solution 1 configured in step (1) to the solution pump 2, and control the working pressure to 10MPa;

[0048] (3) Carbon dioxide feed: the CO in the steel cylinder 2 Input the supercritical fluid anti-solvent equipment system through the booster pump 8, enter the crystallization kettle 4, control the flow rate at 10ml / min, control the starting temperature at 50°C, and the pressure at 10MPa;

[0049] (4) The ciclesonide solution 1 configured in the above step (1) is rapidly sprayed into the crystallization kettle 4 through the solution pump 2 through the nozzle 3 in the supercritical fluid anti-solvent equipment system, the flow control is 1.5ml / min, and the nozzle temperature is 50°C , its spraying distance is 5...

Embodiment 2

[0054] Invention Example 2 Preparation of Ciclesonide Monohydrate

[0055] Take 5g of ciclesonide and add 100ml of ethanol, 10ml of water, and 10ml of acetonitrile into the mixed solution and heat to 50°C, heat filter to remove insoluble matter, cool to 30°C (if crystals are precipitated, take the supernatant), Then add the seed crystals prepared in Example 1 of the invention, heat and stir for 30 minutes, a large amount of crystals are precipitated, cooled to 0-5°C, filtered, and dried. The dried crystals are analyzed by TG-DTA, and the weight loss is about 3.1%. Sonide monohydrate. The obtained crystals were subjected to X-ray powder diffraction measurement, and the measured characteristic peak positions were 2θ=5.1°, 9.0°, 11.2°, 12.8°, 15.0°, 16.2°, 16.9°, 20.7°, 21.8°, 24.3°, 29.1° °, 32.7°.

Embodiment 3

[0056] Invention Example 3 Preparation of Ciclesonide Monohydrate

[0057] Take 5g of ciclesonide and add 100ml of ethanol, 10ml of water, and 15ml of acetonitrile into the mixed solution and heat to 50°C, heat filter to remove insoluble matter, cool to 30°C (if crystals are precipitated, take the supernatant), Then add the seed crystals prepared in Example 1 of the invention, heat and stir for 30 minutes, a large amount of crystals are precipitated, cooled to 0-5°C, filtered, and dried. The dried crystals are analyzed by TG-DTA, and the weight loss is about 3.1%. Sonide monohydrate. The obtained crystals were subjected to X-ray powder diffraction measurement, and the measured characteristic peak positions were 2θ=5.1°, 9.0°, 11.2°, 12.8°, 15.0°, 16.2°, 16.9°, 20.7°, 21.8°, 24.3°, 29.1° °, 32.7°.

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Abstract

The invention discloses a ciclesonide, formoterol fumarate and tiotropium bromide compound dry powder inhaler composition, which consists of (A) ciclesonide or a monohydrate thereof, (B) formoterol fumarate or a hydrate thereof, (C) tiotropium bromide or a hydrate thereof, and a pharmaceutically acceptable carrier, wherein the carrier is a mixture of a carrier A, a carrier B and a carrier C.

Description

technical field [0001] The invention relates to a compound dry powder inhaler of glucocorticoid, β2-receptor agonist and anticholinergic drug, in particular to a compound dry powder inhaler of ciclesonide, formoterol and tiotropium bromide and a preparation method thereof. Background technique [0002] Dry powder inhaler is a kind of preparation for respiratory tract administration. In recent years, dry powder inhalers have developed rapidly due to their advantages of targeting, high efficiency, quick-acting, less toxic and side effects, and no pollution. Glucocorticoids, β2-receptor agonists, and anticholinergic drugs are currently the most common drugs for the treatment of asthma and chronic pulmonary obstruction. Ciclesonide is a new type of glucocorticoid, developed by Altana Company of Germany. In 2004, ciclesonide aerosol was approved for marketing in Australia for the treatment of asthma, and then it was successively launched in the United States, Europe, Japan and o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/58A61K31/167A61K31/46C07J71/00A61K9/72A61K9/14A61P11/06A61P11/00
CPCA61K9/0075A61K9/145A61K31/167A61K31/46A61K31/58C07B2200/13C07J71/0031A61K2300/00
Inventor 王淑丽韩昆颖
Owner TIANJIN JINYAO GRP
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