Nasal use gel containing active component of methyl astragaloside

A technology of astragaloside IV and active ingredients, which is applied in the field of medicine and can solve problems such as difficulty in exerting drug effects, slow onset of effect, and inability of patients to administer medicines independently

Inactive Publication Date: 2007-07-25
TIANJIN INSTITUTE OF PHARMA RESEARCH
View PDF0 Cites 16 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 c

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Astragaloside IV nasal gels were prepared with different hydrophilic gel materials. See Table 1 for formulation (w / w%).

[0030] Table 1. Prescriptions of astragaloside IV nasal gels with different hydrophilic gel materials

[0031] Prescription 1

[0032] Dissolve the preservative in the above prescription 1 in an appropriate amount of distilled water, add carbomer and stir for about 24 hours to make it fully swell. In addition, grind astragaloside drug powder and moisturizer evenly, slowly add it to the carbomer solution, use 1mol / L sodium hydroxide solution to neutralize and adjust the pH to 6.0, and make a gel. The preparation method of prescriptions 2 to 4 is that the hydrophilic material is fully swollen in a certain amount of water to form a blank matrix, and then the solution or suspension of astragaloside IV and other additives is fully mixed to form a drug-containing gel. The preparation of prescriptions 5 and 6 is to add a certain amount of polo...

Embodiment 2

[0034] Carbomer 934P is used as the hydrophilic gel material, and ethanol, propylene glycol, Transcutol P, Labrasol, polyethylene glycols, polysorbates, and cyclodextrins are used as solubilizers. The formulation prescription is shown in Table 2.

[0035] Table 2. Prescription of astragaloside IV nasal gel preparation

[0036] Prescription 1

[0037] Grind the carbomer in the above prescription with glycerin, add distilled water dissolved in preservatives and stir for about 24 hours to fully swell. In addition, after the drug is dissolved with a solubilizer, it is slowly dropped into the carbomer solution, and the pH is adjusted to form a gel. Example 3

Embodiment 3

[0038] Carbomer 934P is used as the hydrophilic gel material, propylene glycol is used as the solubilizer, and glycocholate sodium salt, lysophosphatidylcholine, saponin, and taurocholate sodium salt are used as absorption promoters. The preparation prescription is shown in Table 3.

[0039] Table 3. Prescription of astragaloside IV nasal gel preparation

[0040] Prescription 1

[0041] Grind the carbomer in the above prescription with glycerin, add distilled water dissolved in preservatives and absorption enhancers and stir for about 24 hours to fully swell. In addition, after the drug is dissolved with a solubilizer, it is slowly dropped into the carbomer solution, and the pH is adjusted to form a gel.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/7048A61K36/481A61K9/00A61P9/04
Inventor 王亚静李章才
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap