Octenyl succinate starch with colon targeting controlled release function and preparation method thereof

A technology of octenyl succinate and octenyl succinic anhydride is applied in the field of natural polymer materials in medicine to achieve the effects of improving colon targeting, increasing added value and good colon targeting controlled release performance

Active Publication Date: 2010-02-24
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, the research work on octenyl succinate starch with colon-targeted and controlled release function has not been reported at home and abroad.

Method used

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  • Octenyl succinate starch with colon targeting controlled release function and preparation method thereof
  • Octenyl succinate starch with colon targeting controlled release function and preparation method thereof
  • Octenyl succinate starch with colon targeting controlled release function and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Weigh 10 g of starch (dry basis), the moisture content of starch is 5%, add 50 mL of organic activator pyridine and mix it in the reaction system to form starch milk with a mass percentage concentration of 20% based on starch dry basis;

[0033] (2) Under the condition of stirring, pass nitrogen gas under the liquid surface for 5 minutes to exhaust the air; control the temperature of the reaction system at 80°C, and activate for 1 hour;

[0034] (3) Control the temperature of the reaction system at 80°C, add 25 mL of octenyl succinic anhydride dropwise; react for 1 h;

[0035] (4) cooling, washing with water and suction filtration three times, washing and suction filtration twice with 70% ethanol by volume, drying in an oven at 40°C, pulverizing, and passing through a 100-mesh sieve to obtain the finished product of octenyl succinate starch.

[0036] The degree of substitution (DS) of the octenyl succinate starch prepared in this example was 0.54, and the content of...

Embodiment 2

[0038] (1) Weigh 10 g of starch (dry basis), the moisture content of starch is 3%, add 50 mL of organic activator dimethyl sulfoxide and mix in the reaction system to form starch milk with a mass percentage concentration of 20% based on starch dry basis;

[0039] (2) Under the condition of stirring, pass nitrogen gas under the liquid surface for 5 minutes to exhaust the air; control the temperature of the reaction system at 85°C, and heat and activate for 0.5h;

[0040] (3) Control the temperature of the reaction system at 100°C, add 30 mL of octenyl succinic anhydride dropwise; react for 5 hours;

[0041] (4) cooling, washing with water and suction filtration three times, washing and suction filtration with 70% ethanol twice by volume percent concentration, oven drying at 40° C., pulverizing, and passing through a 100-mesh sieve to obtain the finished product of octenyl succinate starch.

[0042] The degree of substitution (DS) of the octenyl succinate starch prepared in this...

Embodiment 3

[0044] (1) Weigh 10 g of starch (dry basis), the moisture content of the starch is 2%, add 100 mL of organic activator dimethyl sulfoxide and mix it in the reaction system to form a starch milk with a mass percentage concentration of 10% based on the dry basis of starch;

[0045] (2) Under the condition of stirring, pass nitrogen gas under the liquid surface for 5 minutes to exhaust the air; control the temperature of the reaction system at 95°C, and heat and activate for 3 hours;

[0046] (3) Control the temperature of the reaction system at 110°C, add 37 mL of octenyl succinic anhydride dropwise, and react for 1.5 h;

[0047] (4) cooling, washing with water and suction filtration three times, washing and suction filtration with 70% ethanol twice by volume percent concentration, oven drying at 40° C., pulverizing, and passing through a 100-mesh sieve to obtain the finished product of octenyl succinate starch.

[0048] The degree of substitution (DS) of the octenyl succinate s...

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Abstract

The invention discloses octenyl succinate starch with colon targeting controlled release function and a preparation method and an application thereof. The method comprises the following steps: activating starch and organic activator in the presence of protective gas and adding octenyl succinic anhydride to react for 1-5h, cooling, washing, filtering, drying, smashing and screening the to obtain the product. The obtained octenyl succinate starch has the characteristics of incapable digestion and absorption by the amylase in the upper gastrointestinal tract and capable glycolysis by the microorganism in the colon, good colon targeting controlled release function, high controllability in the degree of substitution, good biocompatibility, and safe and non-toxic properties. The octenyl succinate starch is capable of remarkably increasing the colon targeting of medicaments and has less leakage in the gastrointestinal part by the colon targeting positioning technology, such as time lag and enzymatic triggering, and is capable of controlling the speed and degree of the octenyl succinate starch degraded by the microorganism in the colon through regulating the preparation process on the premise of guaranteeing the colon targeting so as to meet the release requirements of different medicaments.

Description

technical field [0001] The invention belongs to the field of research and development of natural polymer materials in the field of medicine, and in particular relates to a preparation method and application of octenyl succinate starch with a colon-targeted and controlled-release function. Background technique [0002] Oral-colon-targeting-drug-delivery-system (OCTDDS) is a drug delivery system that does not release the drug in the upper gastrointestinal tract after oral administration, but delivers the drug to the ileocecal or colon of the human body. After that, it begins to disintegrate or be released by erosion, so that the drug can exert local or systemic therapeutic effects in the large intestine of the human body. In recent years, the Oral Colon Targeted Drug Delivery System (OCTDDS) has been used to improve the bioavailability of proteins and polypeptides after oral administration and to treat some special diseases, such as ulcerative colitis, Crohn's disease (segment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/16A61K9/20A61P1/00C08B31/04
Inventor 陈玲王雪毓黄帆李晓玺李琳李冰徐鹏丁卫
Owner SOUTH CHINA UNIV OF TECH
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