Ciclesonide azelastine compound composition

A technology of azelastine and azelastine hydrochloride, which is applied in the direction of active ingredients of heterocyclic compounds, drug combination, drug delivery, etc., and can solve the problems of not obtaining crystal form III of ciclesonide

Inactive Publication Date: 2017-05-24
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

By repeating Example 8 of WO2008062450, it was found that ciclesonide crystal form I was obtained, but ciclesonide crystal form III was not obtained

Method used

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  • Ciclesonide azelastine compound composition
  • Ciclesonide azelastine compound composition
  • Ciclesonide azelastine compound composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Invention Example 1 Preparation of Ciclesonide Monohydrate by Supercritical Method

[0057] (1) Preparation of ciclesonide solution 1: 5 g of ciclesonide was completely dissolved in a mixed solution of 200 ml of acetone and 20 ml of water at 50° C.;

[0058] (2) The ciclesonide solution 1 configured in step (1) is connected to the solution pump 2, and the working pressure is controlled to be 10MPa;

[0059] (3) Carbon dioxide feeding: the CO in the steel cylinder is input into the supercritical fluid anti-solvent equipment system through the booster pump 8, and enters the crystallization kettle 4, the flow rate is controlled at 10ml / min, the starting temperature is controlled at 50°C, and the pressure is 10MPa;

[0060] (4) The ciclesonide solution 1 configured in the above step (1) is rapidly sprayed into the crystallization kettle 4 through the nozzle 3 in the supercritical fluid antisolvent equipment system by the solution pump 2, and the flow control is 1.5ml / min, a...

Embodiment 2

[0065] Invention Example 2 Preparation of Ciclesonide Monohydrate

[0066] 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 crystal was 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

[0067] Invention Example 3 Preparation of Ciclesonide Monohydrate

[0068] 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 relates to a ciclesonide azelastine compound composition. The ciclesonide azelastinenasal spray composition contains (A) ciclesonide monohydrate, and (B) azelastine or salt thereof and a pharmaceutically acceptable carrier, wherein the ciclesonide monohydrate exists in a crystal form.

Description

[0001] Technical field: [0002] The invention relates to a compound composition of glucocorticoid hormone and antihistamine, in particular to a compound composition of ciclesonide monohydrate and azelastine. It belongs to the field of pharmaceutical technology. [0003] Background technique: [0004] The human nasal cavity is an effective organ for the absorption of pharmacologically active ingredients. Since the 1980s, with the continuous improvement of the level of science and technology, new preparations that exert the local or systemic therapeutic effect of pharmacologically active components through nasal mucosa absorption—collectively referred to as the research and development progress of Nasal Drug Delivery System (Nasal Drug Delivery System) fast. [0005] Nasal Spray (Nasal Spray) is a new formulation for nasal administration developed in recent years. The pharmacologically active components and adjuvant solutions (or suspensions) are filled in a container that ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/55A61K9/12A61P11/02A61P37/08
CPCA61K31/58A61K9/0043A61K9/12A61K31/55A61K2300/00
Inventor 李静王淑丽韩昆颖金玉鑫
Owner TIANJIN JINYAO GRP
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