Inhaled Preparation Of Isoglycyrrhizic Acid Or Salt Thereof, And Use In Preparing Drugs For Treating Respiratory System Diseases

Abstract

The present invention belongs to the field of medicine, relates to an inhaled preparation of isoglycyrrhizic acid or a salt thereof, and in particular relates to an inhaled preparation of magnesium isoglycyrrhizinate and the use thereof in preparing drugs for treating respiratory system diseases.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS[0001]The present application claims priority of Chinese Application No. 201610237175.3, filed on Apr. 15, 2016, and content thereof is incorporated by reference in its entirety into the text of this application.FIELD OF THE INVENTION[0002]The present invention belongs to the field of medicine, relates to an inhaled preparation of isoglycyrrhizic acid or a salt thereof, and in particular relates to an inhaled preparation of magnesium isoglycyrrhizinate and the use thereof in preparing drugs for treating respiratory system diseases.BACKGROUND OF THE INVENTION[0003]Glycyrrhiza is a commonly used medicinal plant, and main active ingredient thereof is glycyrrhizic acid species, namely 18-β glycyrrhizic acid and 18-α glycyrrhizic acid (also known as isoglycyrrhizic acid). Chinese patent ZL02111693.8 discloses a new compound magnesium isoglycyrrhizinate (structure shown in Formula I, with molecular weight of 845); proved by a large number of pharmac...

AI Technical Summary

Benefits of technology

[0068]The inventors unexpectedly discovered that the magnesium isoglycyrrhizinate with medium molecular weight can be prepared into an inhaled preparation, which has a high emptying rate and a high fine particle fraction, and inhalation administration can make magnesium isoglycyrrhizinate rapidly enter the bloodstream in the lung, thereby entering the blood circulation to play a systemic role. Compared with common oral preparations, the bioavailability of magnesium isoglycyrrhizinate inhaled preparation is significantly improved, thereby the dosage and the risk of toxic side effects can be reduced; compared with the injection, the bioavailability of the magnesium isoglycyrrhizinate inhaled preparation is equivalent, but that makes the patient actively or passively receive inhaled preparation, which greatly reduces the pain caused by injection and improves patient compliance. Therefore, the inhaled preparation of the present invention is extremely suitable for sequential use with an injection solution, and the pain and treatment costs brought by injection are reduced while ensuring the efficacy.

Problems solved by technology

Some patients may have jaundice fever and liver enlargement accompanying with liver damage.

Magnesium isoglycyrrhizinate is clinically suitable for treating chronic viral hepatitis and improving liver function abnormalities, but patient compliance is poor since it is administered intravenously.

Although intravenous drip is used for the purpose of timely treatment for patients who cannot be administrated orally, it will inevitably lead to corresponding adverse reactions, such as infusion reaction, vascular stimulation and phlebitis, causing pain to the patients.

Since liver cells are not the only host cells of hepatitis virus, there exists a problem of low bioavailability when using diammonium glycyrrhizinate preparation to treat viral hepatitis, and it has to increase the dosage to achieve the desired therapeutic effect, but the risk of side effects of the drug is also increased at the same time.

As for dry powder inhaled preparation, if the drug particles are highly hygroscopic, aggregation, drug particle enlargement and stratification are very likely to occur during drug preparation and storage, thereby affecting the pulmonary deposition amount of the drug particles, and further affecting the efficacy.

The use of magnesium isoglycyrrhizinate prepared as an inhaled preparation for treating diseases has not been reported, and the molecular weight of magnesium isoglycyrrhizinate is moderate, thus preparing it into an inhaled preparation may present a great challenge.

With the progressive development of airflow limitation, the chronic inflammatory response of the airway and lung caused by harmful particles or gases is increased, and acute exacerbations and complications often affect the severity of the overall disease of the patients.

It is reported that the incidence and mortality of COPD are increasing year by year, and it is now the fourth leading cause of death in the world, seriously jeopardizing the health of the people, and has become an important public health problem due to its heavy social and economic burden.

However, researches have confirmed that the current treatment cannot alleviate the long-term decline tendency in lung function of patients with COPD, especially the effective prevention and treatment for the progressive decline of lung function in stable phase are lacked, and the long-term application of glucocorticoids and β2 receptor agonists inevitably bring some side effects, thus it is still necessary to find better drugs and preparations for the treatment of COPD.

Cough, phlegm and asthma are the three common symptoms of the respiratory system, which are present simultaneously and interact with each other, which not only bring pain to the patients, but also is life threatening.

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