Glycopyrronium bromide compound

A technology of glycopyrronium bromide and compounds, which is applied in the field of glycopyrrolate bromide compounds and their clinical applications, and can solve problems such as long patent expiration time

Inactive Publication Date: 2018-04-17
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The starting materials used in this route are easy to obtain, the process operation is simple, and the yield of each step is stable, which is suitable for large-scale industrial production; however, this route involves patent protection in China, and the time before the patent expires is long

Method used

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  • Glycopyrronium bromide compound
  • Glycopyrronium bromide compound
  • Glycopyrronium bromide compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add glycopyrronium bromide into a mixed solvent of acetonitrile-methyl ethyl ether (1:19), heat and stir at 35-42°C until dissolved to obtain a mixed solution of glycopyrronium bromide; cool the solution to 25°C, crystallize at constant temperature, filter, Crystals are obtained after drying.

[0042] Powder X-ray diffraction: use Cu-K radiation, the X-ray powder diffraction (XRPD) collection of patterns of gained glycopyrronium bromide crystal sees attached figure 1 . Differential Scanning Calorimetry: The differential scanning calorimetry spectrum of glycopyrrolate bromide is shown in the attached figure 2

Embodiment 2

[0044] Mix 0.5 g of magnesium stearate and 205 g of lactose monohydrate as a carrier in a three-dimensional mixer for 4 hours, and micronize it into D 90 Less than 5 microns, D 50 Add 0.75 g of glycopyrronium bromide (Example 1) less than 2.5 microns into the above powder, and continue mixing for 1 hour by three-dimensional mixing to obtain inhalable dry powder A; put dry powder A into No. 3 HPMC material with 25 mg aliquots in the capsule.

Embodiment 3

[0046] Magnesium stearate 4.5g, carrier lactose monohydrate 200g, micronized into D 90 Less than 5 microns, D 50 Add 0.79 g of glycopyrronium bromide (Example 1) less than 2.5 microns together into a three-dimensional mixer and mix for 6 hours to obtain inhalable dry powder B; dry powder B is packed into No. 3 capsules of HPMC material with 50 mg aliquots middle.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a glycopyrronium bromide compound. COPD (chronic obstructive pulmonary disease) is a common respiratory disease,morbidity and mortality of the COPD are increasing year by year in China, about 210 million people in the world are affected, and the disease is predicted to be the third leading cause of death in 2020. Glycopyrronium bromide has an improvement effect on patients with the COPD, and the pharmacokinetics of glycopyrronium bromide within one week after treatment reaches a steady state.

Description

technical field [0001] The invention belongs to the field of medical research, in particular to glycopyrronium bromide compounds and their clinical applications. Background technique [0002] Glycopyrronium bromide is also known as glycopyrrolate bromide, stomach Changning. White crystalline powder, odorless, slightly bitter taste. The melting point is 193-194.5°C. Soluble in water, ethanol, soluble in acetonitrile, methanol, slightly soluble in acetone, almost insoluble in chloroform and ether. Made from styrene. Quaternary ammonium anticholinergics have the functions of inhibiting the secretion of gastric juice and regulating gastrointestinal motility. After taking it, it can quickly relieve spasm, resist acid and relieve pain. For gastric and duodenal ulcers, chronic gastritis, gastric acid hypersecretion embolism. The curative effect is similar to or better than propantheline bromide. Preparations include tablets and injections. [0003] Glycopyrronium Bromide is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/12A61K31/40A61P11/00
CPCC07D207/12C07B2200/13
Inventor 易仕旭罗浩刘好胡登稳李云秀
Owner SICHUAN HAISCO PHARMA CO LTD
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