Chitosan polymer medicinal auxiliary material with gastric retention and specific drug delivery and preparation method and applications thereof
A chitosan polymer, gastric retention technology, applied in the directions of non-active ingredients medical preparations, drug combinations, pharmaceutical formulations, etc., can solve the problems of difficult positioning release, short action time, strong sustained release, etc. Promotes wound healing, enhances duration of action, and improves solubility
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Embodiment 1
[0039] Preparation of CS-CPBA
[0040] Take 40 mg of CS with a molecular weight of 40,000 and a degree of deacetylation of 80%, add it to 20 mL of pure water containing 40 μL of acetic acid, and stir magnetically for 10 min to dissolve it to obtain solution A. Take 100mg of 3-CPBA, add 20mL of methanol and stir, after fully dissolved, add 20mg of EDC and 20mg of NHS, continue stirring in ice bath for 30min to obtain solution B. Add solution B to solution A at a rate of 6 drops / min, remove the ice bath and react at room temperature for 24 hours to obtain solution C. Transfer solution C to a rotary evaporator, and evaporate at 40°C and -0.1MPa for about 10 minutes until no more bubbles are generated. Put the product after rotary evaporation into a 14000da dialysis bag for dialysis for 48 hours, and change the water every 4 hours. Then put the dialyzed product into an oven at 40° C. to fully dry to obtain CS-CPBA powder.
Embodiment 2
[0042] Preparation of CS-CPBA
[0043] Take 80 mg of CS with a molecular weight of 40,000 and a degree of deacetylation of 80%, add it to 20 mL of pure water containing 20 μL of acetic acid, and stir it magnetically for 10 minutes to dissolve it to obtain solution A. Take 100 mg of 3-CPBA, add 20 mL of acetone and stir, and fully dissolve 40 mg of EDC and 20 mg of NHS were added under ice-bath stirring, and the ice-bath stirring was continued for 30 min to obtain solution B. Add solution B to solution A at a rate of 6 drops / min, remove the ice bath and react at room temperature for 24 hours to obtain solution C. Move solution C to a rotary evaporator, and evaporate at 50°C and -0.1MPa for about 15 minutes until no bubbles are generated. The product after rotary evaporation was put into a 13000da dialysis bag for dialysis for 48 hours, and the water was changed every 6 hours. Then put the dialyzed product into an oven at 50° C. to fully dry to obtain CS-CPBA powder.
Embodiment 3
[0045] Preparation of CS-CPBA
[0046] Take 50 mg of CS with a molecular weight of 50,000 and a degree of deacetylation of 80%, add 25 mL of pure water containing 40 μL of sulfuric acid, and stir magnetically for 15 minutes to dissolve it to obtain solution A. Take 50 mg of 4-CPBA, add 25 mL of methanol and stir, after fully dissolving 40 mg of EDC and 40 mg of NHS were added under ice-bath stirring, and the ice-bath stirring was continued for 30 min to obtain solution B. Add solution B to solution A at a rate of 6 drops / min, remove the ice bath and react at room temperature for 24 hours to obtain solution C. Transfer solution C to a rotary evaporator, and evaporate at 50°C and -0.1MPa for about 10 minutes until no more bubbles are generated. The product after rotary evaporation was put into a 15000da dialysis bag for dialysis for 48 hours, and the water was changed every 8 hours. Then the dialyzed product was freeze-dried to obtain CS-CPBA powder.
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