Nasal use gel containing active component of methyl astragaloside

Abstract

A nasal gel with high biologic utilization rate contains proportionally astragaloside A, hydrophilic gel chosen from carbomer and cellulose derivative, pH regulator, humectant, antiseptic agent, solubilizer and co-solvent.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nasal gel of the active ingredient of astragaloside IV and a preparation method thereof. technical background [0002] Astragalus is one of the most commonly used traditional Chinese medicines with a long history and wide clinical application. Traditional Chinese medicine believes that astragalus is warm in nature and sweet in taste, and has the functions of invigorating qi and raising yang, solidifying the surface and antiperspirant, detoxifying and promoting muscle growth, reducing swelling and diuresis. Astragaloside IV is a monomeric compound extracted from the traditional Chinese medicine Astragalus membranaceus. In recent years, a large number of studies have shown that astragaloside IV can be used in the prevention and treatment of cardiovascular system diseases, especially in the treatment of chronic heart failure. Compared with the digitalis drugs commonl...

AI Technical Summary

Problems solved by technology

As one of the main active ingredients, astragaloside IV has extremely poor water solubility and poor gastrointestinal mucosal transport permeability, which seriously affects the key process of dissolution and absorption of ordinary oral administration. The average oral bioavailability of astragaloside IV has been calculated Only 2.2%, it is difficult to exert the drug effect under the oral route

Taking conventional oral preparations such as tablets and capsules cannot meet the needs of medication at all

[0003] In view of the many limitations of oral dissolution and absorption, it seems advisable to use injection administration, and there are also patent reports on astragaloside IV injection poles. Additives such as solubilizing and co-solvents solve the problem of insoluble in water, coupled with the shortcomings of the injection itself, it is still inevitable to introduce some more practical problems: 1. The use of harmful solubilizing and co-solvents will bring unnecessary toxic and side effects; 2. Astragaloside IV has poor water solubility, and it is difficult to meet the effective dose by subcutaneous, intramuscular or intravenous injection. However, the input volume is generally large when administered by intravenous infusion, which will increase the burden on the heart of patients with heart failure. 3. Patients with chronic heart failure have a long course of disease, and most of them are unwilling to undertake hospitalization. Long-term infusion will increase the psychological burden and medical burden of patients, and at the same time, patients cannot self-administer medication, which brings a lot of inconvenience; 4. The fear of injection pain plagues most patients, and this phenomenon is more serious if the medication cycle is longer; 5. There are many unsafe factors in the injection itself, such as allergic reactions, pyrogen reactions, etc.

[0006] However, due to the small volume of administration in the nasal cavity, for adults, the maximum amount of liquid medicine that can be accommodated in each nostril is only 0.2ml, which is very difficult to prepare its nasal solution for astragaloside IV with poor water solubility. Difficulties

At the same time, the nasal cavity removes foreign matter quickly, the effective absorption of nasal drops is small, the effect is poor, the throat is irritating, and there are many pathological changes in the nasal mucosa after repeated use.

[0007] Commonly used nasal sprays have the disadvantages of inaccurate or inconvenient control of dosage

Inhalants, especially dry powder inhalers, tend to have a long-term swelling process, large space transfer steric hindrance, and relatively slow onset of action