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

A chitosan quaternary ammonium salt, chitosan technology, applied in the direction of pharmaceutical formulations, drug delivery, etc., can solve the problems of patients' economic burden, inconvenience, application obstacles, etc., to improve utilization rate and safety, and high pH responsiveness , Improve the effect of hydrophilicity

A chitosan quaternary ammonium salt, chitosan technology, applied in the direction of pharmaceutical formulations, drug delivery, etc., can solve the problems of patients' economic burden, inconvenience, application obstacles, etc., to improve utilization rate and safety, and high pH responsiveness , Improve the effect of hydrophilicity

CN1830420BInactive Publication Date: 2012-07-25INST OF PROCESS ENG CHINESE ACAD OF SCI
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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

Examples

Experimental program
Comparison scheme
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

The present invention discloses an injectable pH-sensitive chitosan quaternary ammonium salt hydrogel and a preparation method thereof, belonging to the medicine engineering pharmaceutic preparation field. The method adopts the chitosan hyamine and the glycerophosphate to prepare the injectable pH-sensitive chitosan quaternary ammonium salt hydrogel. The preparation method comprises the following steps: (1) the chitosan and the 2.3-epoxypropyl ammonium trimethylchloride are reacted at the reaction temperature, are deposited using acetone, washed, and dried to obtain chitosan hyamine; (2) the prepared chitosan hyamine is dissolved into an acid solution; (3) glycerophosphate is added dropwise into the chitosan hyamine acid solution to obtain uniform and clear mixed solution while stirring; (4) the temperature is rised to a gelatinization temperature, and an uniform and transparent chitosan hyamine hydrogel is obtained after keeping constant temperature. The hydrogel can happen gelatinization at a room temperature, and responds to the internal pH value variation to swelling, dissolve and realize intelligent release of the embedding drugs.

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

Patent Timeline
25 Jul 2012
Publication
CN1830420B
IPC
A61K47/36; A61K9/00
Inventors
马光辉; 苏志国