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Vitamin B12 group containing amphiphilic sodium alginate derivative and preparation method and application thereof

A sodium alginate and B12 technology, which is applied in the field of amphiphilic sodium alginate derivatives and its preparation, can solve the problems that have not yet been reported on sodium alginate oral nanoparticles, achieve the enhancement of small intestine targeted absorption performance, and maintain biological activity , The effect of low synthesis reaction temperature

Inactive Publication Date: 2018-12-21
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sodium alginate is often used as a pharmaceutical preparation auxiliary material in the pharmaceutical industry at present, and there is no report of sodium alginate oral nanoparticles in the prior art

Method used

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  • Vitamin B12 group containing amphiphilic sodium alginate derivative and preparation method and application thereof
  • Vitamin B12 group containing amphiphilic sodium alginate derivative and preparation method and application thereof
  • Vitamin B12 group containing amphiphilic sodium alginate derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] (1) According to the ratio of CSAD (the substitution degree of cholesterol group is 15%): dehydrated ethyl acetate = 0.5g: 10mL, add dehydrated ethyl acetate to CSAD, and stir at room temperature at 100 rpm under nitrogen protection Dissolve in 24 hours to obtain CSAD solution;

[0057] (2) According to the ratio of vitamin B12 (VB12): dehydrated ethyl acetate = 0.05g: 3mL, add dehydrated ethyl acetate to VB12 to dissolve;

[0058] (3) According to the ratio of dicyclohexylcarbodiimide: 4-dimethylaminopyridine: dehydrated ethyl acetate = 0.1g: 0.05g: 3mL, dicyclohexylcarbodiimide and 4-dimethylaminopyridine Add dehydrated ethyl acetate to dissolve;

[0059] (4) Slowly add the solution obtained in step 2 and step 3 to the CSAD solution in step 1, and react for 20 hours at 500 rpm under nitrogen protection;

[0060] (5) Precipitate the reaction solution in step 4 with isopropanol, filter, and collect the precipitate;

[0061] (6) Add 10 mL of distilled water to the pre...

Embodiment 2

[0072] (1) According to the ratio of CSAD (the degree of substitution of cholesterol groups is 3%): dehydrated dimethylformamide = 1g: 0.5mL, add dehydrated dimethylformamide to CSAD, under the protection of helium at 500 rev / min, stirred at room temperature for 18 hours and dissolved to obtain a CSAD solution;

[0073] (2) According to the ratio of VB12: dehydrated dimethylformamide = 0.5g: 5mL, add dehydrated dimethylformamide to VB12 to dissolve;

[0074](3) According to the ratio of dicyclohexylcarbodiimide: 4-dimethylaminopyridine: dehydrated dimethylformamide = 0.3g: 0.3g: 1mL, dicyclohexylcarbodiimide and 4-dimethylformamide Add dehydrated dimethylformamide to aminopyridine to dissolve;

[0075] (4) Slowly add the solution obtained in step 2 and step 3 to the CSAD solution in step 1, and react for 2 hours at 100 rpm under the protection of helium;

[0076] (5) Precipitate the reaction solution in step 4 with ethanol, filter, and collect the precipitate;

[0077] (6) ...

Embodiment 3

[0083] (1) According to the ratio of CSAD (the degree of substitution of cholesterol groups is 8%): dehydrated dimethyl sulfoxide = 0.6g: 35mL, add dehydrated dimethyl sulfoxide to CSAD, under the protection of argon at 300 Rotation / min Stir at room temperature for 1 hour to dissolve, and obtain CSAD solution;

[0084] (2) According to the ratio of VB12: dehydrated dimethyl sulfoxide = 0.02g: 1mL, add dehydrated dimethyl sulfoxide to VB12 to dissolve;

[0085] (3) According to the ratio of dicyclohexylcarbodiimide: 4-dimethylaminopyridine: dehydrated dimethyl sulfoxide = 0.5g: 0.1g: 5mL, dicyclohexylcarbodiimide and 4-dimethyl Add dehydrated dimethyl sulfoxide to aminopyridine to dissolve;

[0086] (4) Slowly add the solution obtained in step 2 and step 3 to the CSAD solution in step 1, and react for 48 hours at 400 rpm under the protection of argon;

[0087] (5) Precipitate the reaction solution in step 4 with acetone, filter, and collect the precipitate;

[0088] (6) Add ...

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Abstract

The invention discloses a vitamin B12 group containing amphiphilic sodium alginate derivative and a preparation method and application thereof. Particularly, the derivative is an amphiphilic sodium alginate derivative containing a vitamin B12 group and a cholesteryl group. The derivative has a compound structure formula represented by a formula (I) shown in the description. The vitamin B12 group containing amphiphilic sodium alginate derivative (VB12-CSAD) is prepared through subjecting a cholesteryl containing amphiphilic alginic acid derivative (CSAD) to a reaction with vitamin B12. The reaction conditions of synthesis of the VB12-CSAD are mild, and thus, the maintaining of bioactivity of the vitamin B12 is facilitated; the VB12-CSAD is high in stability in a digestive tract system; thesmall-intestine targeted absorption performance is high, so that the vitamin B12 group containing amphiphilic sodium alginate derivative is advantageously used as an oral-application nano-preparationfor small-intestine targeted absorption and has a relatively good application prospect in the aspect of improving safety and bioavailability of oral application drugs.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, more specifically, to an amphiphilic sodium alginate derivative containing a vitamin B12 group and its preparation method and application. Background technique [0002] Due to the strong acidic environment of gastric acid, the action of enzymes in the digestive system, short half-life, and fast metabolism, it is difficult for some oral drugs to reach the absorption site in the small intestine. In addition, there are problems such as low absorption efficiency in the small intestine, resulting in low bioavailability of these drugs. Low, thus affecting the therapeutic effect (Sun Luyin et al., Medical Review, 2015, 21(20), 3686-3688). [0003] As an emerging drug delivery system, polymer nanoparticles have unique advantages in overcoming the above-mentioned shortcomings of oral drugs. They can not only better protect the stability of drugs in the digestive tract system, but also improve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/04A61K9/51A61K47/36A61K47/26A61K31/546A61K38/28
CPCA61K9/5123A61K9/5161A61K31/546A61K38/28C08B37/0084
Inventor 杨立群邓宇斌李国新赖明华龙玲莉张黎明胡彦锋郭伟洪
Owner SUN YAT SEN UNIV
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