Inhalation ueclidinium bromide solution preparation and preparation method thereof

A technology of umeclidinium bromide and solution, which is applied in the field of pharmaceutical preparations, can solve the problems of irritation, inability to achieve drug delivery, tracheal spasm adverse reactions, etc., and achieve the effects of reducing irritation, preparation safety, and increasing compliance

Pending Publication Date: 2022-02-18
INCREASEPHARM TIANJIN INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The currently marketed inhalation preparation of umeclidinium bromide is a powder aerosol. The powder aerosol needs to rely on the patient's large inspiratory flow rate to start the nebulization. The patient cannot achieve drug delivery under normal breathing conditions, so it is not suitable for children and the elderly. and other patients with difficulty breathing on their own initiative
At present, there is no inhalation solution preparation on the market. Chinese patent CN110292559A discloses umeclidinium bromide atomized inhalation solution, and its prescription composition includes umeclidinium bromide, surfactant, isotonic regulator, metal ion complexing agent, pH buffer, pH adjuster, water; it is recorded in the patent that the osmotic regulator can be selected from mannitol, and mannitol is an activator of bronchospasm, which can easily cause bronchospasm and cause adverse reactions, and the metal ion complexing agent can be selected from ethylenediaminetetraacetic acid Disodium, disodium edetate is an important complexing agent, which is used to complex metal ions and separate metals. It can also be used as an antioxidant synergist, stabilizer and softener. Stimulates the upper respiratory tract

Method used

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  • Inhalation ueclidinium bromide solution preparation and preparation method thereof
  • Inhalation ueclidinium bromide solution preparation and preparation method thereof
  • Inhalation ueclidinium bromide solution preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0042] prescription composition

[0043] name composition Umeclidinium Bromide 20mg citric acid 0.11g Sodium citrate Adjust pH to 4.5 Sodium chloride 7.8g Add water for injection to 1000ml

[0044] Preparation:

[0045] Measure 800ml (80% of prescription quantity) of water for injection at room temperature, drop into prescription quantity sodium chloride, citric acid successively, drop into umeclidinium bromide after stirring and dissolving, continue stirring to dissolve, add sodium citrate to adjust pH value to 4.5 , after stirring evenly, make up to the full amount with a solvent, filter with a 0.22 μm filter membrane or filter element, fill into a 1ml ampoule bottle, seal it, and get ready.

Embodiment 2

[0047] prescription composition

[0048] name composition Umeclidinium Bromide 40mg Dilute hydrochloric acid Appropriate amount sodium bicarbonate Adjust pH to 6.0 Sodium chloride 8.7g Add water for injection to 1000ml

[0049] Preparation:

[0050] Measure 700ml of water for injection at 40°C (70% of the prescribed amount), put into the prescribed amount of sodium chloride, stir and dissolve, add dropwise dilute hydrochloric acid until the pH value reaches 3.0, stir evenly, put in umeclidinium bromide and stir to dissolve, put in carbonic acid Adjust the pH value to 6.0 with sodium hydrogen, stir evenly, make up to the full amount with a solvent, filter with a 0.22 μm filter membrane or filter element, fill it into a 2ml ampoule bottle, and seal it.

Embodiment 3

[0052] prescription composition

[0053] name composition Umeclidinium Bromide 60mg citric acid 0.25g Sodium citrate Adjust pH to 5.0 glucose 48g Add water for injection to 1000ml

[0054] Preparation:

[0055] Measure the water for injection 800ml (80% of prescription quantity) of 60 ℃, drop into prescription quantity glucose and citric acid successively, stir and make dissolving, drop into umeclidinium bromide, after stirring makes dissolving, drop into sodium citrate and adjust pH value to 5.0, Stir evenly, make up to full amount with solvent, filter with 0.22μm filter membrane or filter element, fill into 2ml ampoules, seal, and get ready.

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Abstract

The invention provides an inhalation umeclidinium bromide solution, a preparation method and application thereof, the inhalation solution comprises an active substance, a solvent and auxiliary materials, the single dose specification of the inhalation solution is 1-5ml, and the active substance in the single dose specification is 20-100 micrograms of umeclidinium bromide; the solvent is sterile injection water; the auxiliary materials comprise an isoosmotic adjusting agent and a pH adjusting agent; the adding amount of the isoosmotic adjusting agent is such that the inhalation solution has a weight gram molecule osmotic concentration of 240-400mOsmol / kg; the pH regulator is added so that the pH value of the inhalation solution preparation is 4.0-6.0. The device for combining the ullidinium bromide solution for inhalation with an atomized aerosol can provide a medicine dosage form of the ullidinium bromide for inhalation, which is convenient to use, safe, effective and good in stability, and an administration system.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a umeclidinium bromide solution for inhalation, a preparation method and application thereof. Background technique [0002] Chronic obstructive pulmonary disease (COPD) is a chronic respiratory disease characterized by incompletely reversible airflow limitation, with a large number of patients and a high mortality rate. According to the World Health Organization (WHO), there are currently 600 million people suffering from this disease worldwide, and it will become the third leading cause of death in the world by 2020. [0003] According to the "2013 Chinese Medical Association Guidelines for the Diagnosis and Treatment of Chronic Obstructive Pulmonary Disease", the treatment drugs include: bronchodilators, glucocorticoids, phosphodiesterase-4 (PDE-4) and other drugs. Bronchodilators are the main treatment for controlling COPD symptoms. They can relax bronchial smooth muscle, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/72A61K47/26A61K47/02A61K47/12A61K47/04A61K31/439A61P11/00
CPCA61K9/0078A61K9/08A61K47/26A61K47/02A61K47/12A61K31/439A61P11/00
Inventor 胡杰扈靖都暖王永福
Owner INCREASEPHARM TIANJIN INST CO LTD
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