Check patentability & draft patents in minutes with Patsnap Eureka AI!

Ciclesonide and formoterol fumarate dry powder inhaler composition

A dry powder inhaler, formoterol fumarate technology, applied in the field of ciclesonide formoterol dry powder inhaler and its preparation, can solve the problem of unfavorable dry powder inhaler configuration, serious particle agglomeration, easy to generate static electricity, etc. question

Active Publication Date: 2017-06-23
TIANJIN JINYAO GRP
View PDF12 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ciclesonide and formoterol fumarate dry powder inhaler composition
  • Ciclesonide and formoterol fumarate dry powder inhaler composition
  • Ciclesonide and formoterol fumarate dry powder inhaler composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Invention Example 1 Preparation of Ciclesonide Monohydrate by Supercritical Method

[0047] (1) Prepare ciclesonide solution 1: Dissolve 5g ciclesonide completely in a mixed solution of 200ml acetone and 20ml water at 50°C;

[0048] (2) Connect the ciclesonide solution 1 configured in step (1) to the solution pump 2, and control the working pressure to 10MPa;

[0049] (3) Carbon dioxide feed: the CO in the 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;

[0050] (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 5cm; En...

Embodiment 2

[0055] Invention Example 2 Preparation of Ciclesonide Monohydrate

[0056] 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%, which is confirmed to be ring crystals. 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

[0057] Invention Example 3 Preparation of Ciclesonide Monohydrate

[0058] 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°.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a ciclesonide and formoterol fumarate dry powder inhaler composition, which consists of (A) ciclesonide or a monohydrate thereof, and (B) formoterol fumarate or a hydrate and a pharmaceutically acceptable carrier thereof, 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 a glucocorticoid and a β2-receptor agonist, in particular to a ciclesonide formoterol dry powder inhaler 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 and β2-receptor agonists are currently the most common drugs for the treatment of asthma. 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 other countries and regions. The company also studied Ciclesonide Nasal Spray Suspension, and in 2008 Ciclesonid...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/58A61K31/167A61K9/72A61P11/06C07J71/00
CPCA61K9/0075A61K31/167A61K31/58A61K47/10A61K47/18A61K47/26C07J71/0031A61K2300/00
Inventor 王淑丽韩昆颖
Owner TIANJIN JINYAO GRP
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com