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Slow-release aerogel and indomethacin-loaded slow-release aerogel

A technology of indomethacin and airgel, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., to achieve the effect of mild conditions, high loading efficiency, and easy volatilization

Active Publication Date: 2018-05-04
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But there is no patent report on the slow release of indomethacin and the application of loading materials
The use of biodegradable porous hydrogels to load indomethacin, which can not only increase its loading rate, but also achieve its controlled release technology has not been reported yet.

Method used

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  • Slow-release aerogel and indomethacin-loaded slow-release aerogel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] (1) Disperse 1g of nanocellulose raw material in 0.1M acetic acid buffer solution (pH=4.5) to obtain a 1% viscous solution, add 0.8g of sodium periodate, stir well, react at 40°C for 10h, add ethyl alcohol The reaction was terminated with 2 ml of diol, and then subjected to a large amount of water dialysis treatment for 2 days to obtain purified aldylated nanocellulose. After freeze-drying treatment, white formylated nano-cellulose is obtained. The whole reaction was carried out in a three-neck flask, which was wrapped with black paper to avoid light.

[0035] (2) Add the aldylated nanocellulose (0.5 g dry weight) of step (1) into a mixed solvent composed of 9 mL DMSO and 1 mL water, soak to make the material fully swell, and then add 0.5 mL of lysine solid g, reacted at 50°C for 4 hours, the color of the material changed from colorless to brown. After the reaction material dropped to room temperature, 0.5g of sodium borohydride alcohol solution was added, and a large ...

Embodiment 2

[0043] Step (1) is with embodiment 1.

[0044] (2) Add the aldylated nanocellulose (0.5 g dry weight) of step (1) into a mixed solvent composed of 9 mL DMSO and 1 mL water, soak to make the material fully swell, and add 1.0 g of lysine solid , reacted at 60°C for 8 hours, the color of the material changed from colorless to brown. After the reaction material dropped to room temperature, 0.5g of sodium borohydride alcohol solution was added, and a large amount of hydrogen gas could be seen. The purpose of sodium borohydride is to make the imine group The group (C=N) is reduced to an amino group. Finally, the product solution was dialyzed with a large amount of deionized water to obtain lysine-modified nanocellulose.

[0045] (3) disperse the lysine-modified nanocellulose (0.4g of dry weight) of step (2) in the aqueous solution containing 1.6g cationic guar gum and 0.2g polyvinyl alcohol, stir at high speed, obtain viscous White solution, add aqueous solution of sodium hydroxid...

Embodiment 3

[0050] Step (1) is with embodiment 1.

[0051] (2) Add the aldylated nanocellulose (0.5 g dry weight) of step (1) into a mixed solvent composed of 9 mL DMSO and 1 mL water, soak to make the material fully swell, and add 0.25 g of lysine white solid g, reacted at 30°C for 4 hours, the color of the material changed from colorless to brown. After the reaction material dropped to room temperature, 0.5g of sodium borohydride alcohol solution was added, and a large amount of hydrogen gas could be seen. The purpose of sodium borohydride was to make the imine produced The group (C=N) is reduced to an amino group. Finally, the product solution was dialyzed with a large amount of deionized water to obtain lysine-modified nanocellulose.

[0052] (3) disperse the lysine-modified nanocellulose (0.2g of dry weight) of step (2) in the aqueous solution containing 2g cationic guar gum and 0.2g polyvinyl alcohol, stir at high speed, obtain viscous white solution, add an aqueous solution of so...

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Abstract

The invention belongs to the technical field of medicine slow release and high molecular materials and discloses slow-release aerogel and indomethacin-loaded slow-release aerogel. The slow-release aerogel is prepared by the following steps: taking nanocellulose and sodium periodate to be subjected to oxidization reaction to obtain aldehyde nanocellulose; then dispersing the aldehyde nanocelluloseinto a solvent and adding lysine to react to obtain lysine modified nanocellulose; dispersing the obtained product into a water solution of cationic guar gum and polyvinyl alcohol; then adding an alkaline catalyst and a macromolecular crosslinking agent in sequence; standing and crosslinking at 25 to 70 DEG C and carrying out polymerization reaction for 6 to 24h to obtain aerogel; neutralizing theaerogel, immersing and washing, freezing and drying to obtain the slow-release aerogel. The slow-release aerogel is immersed into an ammonia water solution of indomethacin and is subjected to swelling and adsorption; after the adsorption is balanced, a product is taken out and dried to obtain the indomethacin-loaded slow-release aerogel. According to the slow-release aerogel and the indomethacin-loaded slow-release aerogel, the lysine modified nanocellulose is added and the loading rate and the slow release speed of the prepared aerogel on the indomethacin are adjustable.

Description

technical field [0001] The invention belongs to the technical field of drug sustained release and polymer materials, and in particular relates to a sustained release aerogel and a sustained release aerogel loaded with indomethacin. Background technique [0002] Indomethacin is a lipophilic, nonsteroidal anti-inflammatory drug (for its molecular structure see figure 1 ), which has obvious antipyretic and inflammatory pain relief effects, and is commonly used in the treatment of acute and chronic rheumatoid arthritis, gouty arthritis and cancer pain (Western medicine carcinoid pain medicine). Indomethacin causes obvious adverse reactions, such as nausea, vomiting, abdominal pain, diarrhea, ulcers, and sometimes gastric bleeding and perforation. Therefore, it is desired to reduce the frequency of taking the drug, prolong the action time of the drug, realize the slow release of the drug, and increase the patient's tolerance. Due to the poor solubility of indomethacin, its solu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08L5/14C08L1/08C08L71/02C08J3/075C08J3/24C08B15/02C08B15/06A61K31/405A61K47/38A61K47/36A61K47/32A61K9/00A61P29/00A61P35/00A61P19/02A61P19/06
CPCA61K9/0087A61K31/405A61K47/32A61K47/36A61K47/38C08B15/02C08B15/06C08J3/075C08J3/246C08J2305/14C08J2401/08C08J2471/02
Inventor 万小芳刘宝联柴欣生李友明陈广学
Owner SOUTH CHINA UNIV OF TECH
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