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Injection type pH sepsitive chitin quarternary ammonium salt aquagel and its preparation method

A chitosan quaternary ammonium salt, chitosan technology, applied in the directions of pharmaceutical formulations, inactive medical preparations, drug delivery, etc., can solve the problems of patients' economic burden, inconvenience, application barriers, etc. and safety, high pH responsiveness, and the effect of improving hydrophilicity

Inactive Publication Date: 2006-09-13
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, there are still many shortcomings in the smart hydrogels prepared so far, which limit their clinical application.
First of all, most of the currently prepared smart hydrogels are not injectable, and are usually shaped outside the body, and must be surgically implanted to enter the body, which brings economic burden and physical pain to patients as well as application problems. inconvenient
Second, most of the currently prepared smart hydrogels are not biodegradable or lack biocompatibility.
When the drug is released, it must be removed from the human body through surgery, which also limits the clinical application of hydrogel as a drug carrier
For example, polyacrylamide polymers and their derivatives are currently the most widely studied temperature-sensitive hydrogels, but polyacrylamide polymers are not biodegradable, and their monomers are toxic to the human body. There are great obstacles in the clinical application of glue
In addition, the pH responsiveness of the currently developed pH-sensitive hydrogels is not sensitive enough, and it is difficult to quickly respond to small changes in pH in the body to achieve "on-off" drug release.

Method used

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  • Injection type pH sepsitive chitin quarternary ammonium salt aquagel and its preparation method
  • Injection type pH sepsitive chitin quarternary ammonium salt aquagel and its preparation method
  • Injection type pH sepsitive chitin quarternary ammonium salt aquagel and its preparation method

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Experimental program
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Effect test

Embodiment 1

[0049] Disperse 3.0g of chitosan in 20mL of water and stir at 80°C for 1h. 16.94g of 2,3-epoxypropyltrimethylammonium chloride was dissolved in 15mL of water, and added to the chitosan dispersion. After stirring and reacting at 80° C. for 12 h, the reaction solution was poured into acetone to precipitate, stirred and washed in a refrigerator overnight, and then dried to obtain a white loose product. Characterized by infrared spectroscopy (attached figure 1 ), proving that quaternary ammonium groups are substituted on the chitosan chain to generate chitosan quaternary ammonium salts.

Embodiment 2

[0051] Dissolve 0.50 g of the chitosan quaternary ammonium salt prepared in Example 1 in the lactic acid solution of 8 mL of 0.1 mol / L, and dissolve completely. Cool to 4°C, add 2 mL of 0.25 g / mL sodium β-glycerophosphate solution dropwise with stirring, and stir well to make it evenly mixed. The pH of the resulting solution was 7.4. The mixed solution was heated to 37°C and kept for 60 minutes to fully gel the system. The system is stable at 4°C. Chitosan quaternary ammonium salt solution, chitosan quaternary ammonium salt-β-sodium glycerophosphate mixed solution, the photo of the chitosan quaternary ammonium hydrogel that gelled under 37 ℃ are as attached figure 2 shown.

Embodiment 3

[0053] Dissolve 0.50 g of the chitosan quaternary ammonium salt prepared in Example 1 in the acetic acid solution of 8 mL of 0.1 mol / L, and dissolve completely. Cool to 4°C, add 2 mL of 0.25 g / mL sodium β-glycerophosphate solution dropwise with stirring, and stir well to make it evenly mixed. The resulting solution had a pH of 7.0. The mixed solution was heated to 37°C and kept for 60 minutes to fully gel the system. The system is stable at 4°C.

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Abstract

An injectable pH-sensitive chitosan quaternary ammonium salt hydrogel is prepared through reaction between chitosan and 2.3-epoxypropyl ammonium trimethylchloride, depositing in acetone, washing, baking to obtain chitosan quatemary ammonium salt, dissolving it in acidic solution, dripping the solution of glycerine phosphate while stirring, and heating for gelatinizing.

Description

technical field [0001] The invention relates to an injectable pH-sensitive chitosan quaternary ammonium hydrogel and a preparation method thereof, belonging to the field of pharmaceutical preparations of medical engineering. Background technique [0002] Chitosan is the product of N-deacetylation of chitin, and it is a linear polysaccharide composed of β(1→4)-bonded D-glucosamine residues and N-acetylglucosamine with different numbers and random distribution. . Chitosan has a wider range of uses than chitin because it has free amino groups on its molecular chain and can be dissolved in dilute acid solutions. As a natural cationic biopolymer, chitosan has a wide range of sources, non-toxic, odorless, antithrombotic, antistatic, alkali resistance, film forming, bioadhesion, biocompatibility and biodegradability, and its The degradation products are non-toxic, non-immunogenic and non-carcinogenic. These properties make chitosan a promising biomedical carrier [1] . Chitosan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/36
Inventor 马光辉苏志国吴颉
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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