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Novel nasal mucosa absorption enhancer

A technology of absorption enhancer, nasal mucosa, applied in the field of medicine

Inactive Publication Date: 2013-07-31
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, chitosan is insoluble in water and common organic solvents, and can only be dissolved under acidic conditions, which brings a lot of inconvenience to practical applications.

Method used

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  • Novel nasal mucosa absorption enhancer
  • Novel nasal mucosa absorption enhancer
  • Novel nasal mucosa absorption enhancer

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0021] Example 1: Succinylated chitosan (50kDa) with an amino substitution degree of 63.0% promotes nasal mucosal absorption of ligustrazine phosphate

[0022] Male rats (180g-220g) were placed above the drug storage pool after esophageal intubation. Add 5mL ligustrazine phosphate solution (4.0mg / mL) into the drug storage pool and keep stirring. Finally, 0.1% succinylated chitosan (Mw=50kDa) with an amino substitution degree of 63.0% was added and stirred to dissolve (the control group was not added). The drug solution enters the nasal cavity of the rats through the peristaltic pump from the drug storage pool and then returns to the drug storage pool from the nostrils. Samples are taken from the drug storage pool at different time intervals within 2 hours for content determination. In the same way, the absorption promoting effect of 0.1% chitosan (Mw=50kDa) was investigated, and the results are shown in figure 1 .

example 2

[0023] Example 2: Succinylated chitosan (Mw=50kDa) with an amino substitution degree of 63.0% promotes the nasal mucosal absorption of promethazine

[0024] Male rats (180g-220g) were placed above the drug storage pool after esophageal intubation, and 5mL of promethazine solution (0.35mg / mL) was added to the drug storage pool and stirred continuously, and then passed into a circulating water bath at 37±0.5°C. Finally, 0.1% succinylated chitosan (Mw=50kDa) with an amino substitution degree of 63.0% was added and stirred to dissolve (the control group was not added). The drug solution enters the nasal cavity of the rats through the peristaltic pump from the drug storage pool and then returns to the drug storage pool from the nostrils. Samples are taken from the drug storage pool at different time intervals within 2 hours for content determination. Investigate the absorption promoting effect of 0.1% chitosan Mw=(50kDa) with the same method, the results are shown in figure ...

example 3

[0025] Example 3: The effect of succinylated chitosan (Mw=20kDa) with amino substitution degree of 64.2% on nasal mucosal absorption of isosorbide dinitrate

[0026] Male rats (180g-220g) were placed above the drug storage pool after esophageal intubation, and 5mL of isosorbide dinitrate solution (0.5mg / mL) was added to the drug storage pool and stirred continuously, and then passed into a circulating water bath at 37±0.5°C , and finally add 0.1% succinylated chitosan (Mw=20kDa) with an amino substitution degree of 64.2%, and stir to dissolve (the control group is not added). The drug solution enters the nasal cavity of the rats through the peristaltic pump from the drug storage pool, and then returns to the drug storage pool through the nostrils. Samples are taken from the drug storage pool at different time intervals within 2 hours for content determination. In the same way, the absorption promoting effect of 0.1% chitosan (Mw=20kDa) was investigated, and the results are sho...

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Abstract

The invention belongs to the technical field of medicine, and relates to a utilization of succinylated chitosan as a nasal mucosa absorption enhancer. The nasal mucosa absorption enhancer has advantages of good water-solubility, good absorption enhancing and safe use.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a novel absorption accelerator for nasal mucosa administration preparations. The accelerator has the characteristics of good water solubility, good absorption promotion effect and safe use. Background technique [0002] Nasal drug delivery route has been widely concerned and valued by pharmaceutical researchers due to its characteristics of fast absorption, rapid onset of action, high bioavailability, and small side effects. This is mainly due to the fact that the surface area of ​​the human nasal mucosa is 150 cm 2 , not only the epithelial cells of the mucosal surface in the respiratory area have many villi, which are similar to the villi of the small intestine, which can greatly increase the effective area for drug absorption, but also the subepithelial layer of the nasal mucosa is rich in capillaries and lymphatic capillaries, which can make the drug avoid the first-pass effec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K9/08A61K9/10A61K9/107A61K9/16A61K9/127A61K9/14C08B37/08
Inventor 毛世瑞那丽东
Owner SHENYANG PHARMA UNIVERSITY