Water and oil soluble O-chitosan derivatives and their preparation and use

A chitosan derivative, chitosan technology, applied in the direction of drug combination, organic active ingredients, medical preparations containing active ingredients, etc., to achieve the effect of improving absorption efficiency and obvious weight loss effect

Inactive Publication Date: 2005-03-16
TIANJIN UNIV
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

A kind of water, oil two-soluble O-chitosan derivative that the patent of the present

Method used

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  • Water and oil soluble O-chitosan derivatives and their preparation and use
  • Water and oil soluble O-chitosan derivatives and their preparation and use

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Experimental program
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Embodiment 1

[0018] Embodiment one, the preparation of O-ethylamine hydroxyethyl chitosan

[0019] 1. Radiation degradation of chitosan: Chitosan with a molecular weight of 1.08 million and a degree of deacetylation of 85% is produced by Co 60 The radiation source is irradiated with a radiation dose of 60kGy to obtain chitosan oligomer A with a molecular weight of 100,000-200,000 and a deacetylation degree of 86%.

[0020] 2. Preparation of O-ethylamine hydroxyethyl chitosan:

[0021] 1. the preparation of N-phthaloyl chitosan: 0.83g phthalic acid solution is dissolved in the N, N-dimethylformamide that contains 6ml volume ratio of 5% water, adds 0.3g chitosan, in Stir and heat to 120°C under nitrogen. After reacting for 8 hours, the light brown mixture was cooled to room temperature and then poured into ice water. After filtration, the precipitate was washed with 150 ml of methanol for 1 hour and dried to give 0.444 g of substance B as a light brown powder.

[0022] ②Preparation of O-...

Embodiment 2

[0024] Embodiment two, O-2'-hydroxypropyl-N, the preparation of N-dimethyl octadecyl ammonium chloride chitosan

[0025] 1. The radiation degradation of chitosan: carry out by the first step in embodiment one

[0026] 2. Preparation of N, N dimethyl octadecyl tertiary amine chitosan:

[0027] 1. the preparation of N-phthaloyl chitosan: carry out by the first process in the second step in the embodiment one

[0028] ②Synthesis of N,N dimethyl octadecyl tertiary amine hydrochloride

[0029] Prepare 0.1mol / l dilute hydrochloric acid, add it dropwise to 5.95g N, N dimethyl octadecadecyl amine with a constant pressure funnel, control the pH value of the system to 4-11, stir and react in a water bath at room temperature for about 2 hours, and then freeze-dry The milky white cream hydrochloride C.

[0030] ③Reaction of hydrochloride and epichlorohydrin

[0031] Add 1ml of epichlorohydrin dropwise to 3.3g of C, and react in a water bath at room temperature for 6-24 hours to obtain...

Embodiment 3

[0034] Embodiment three, the therapeutic effect of water and oil two-soluble O-chitosan derivatives on obese rats

[0035] 1. Feed preparation and establishment of nutritional obesity model: Synthetic feed was selected as the basic animal feed, and whole egg powder, lard, cholesterol, milk powder and white sugar were added to the basic feed to adjust the energy, cholesterol and fat in the feed A high-fat feed was formulated and fed continuously for 6 weeks to form a nutritionally obese rat model.

[0036] 2. Animal grouping and research methods: After the model was successfully constructed, 70 obese animals were randomly divided into 7 groups according to body weight, 10 animals in each group. The diets fed to each group were as follows:

[0037] ① Obese mice control group (group C): fed with basic feed;

[0038] ②O-ethylamine hydroxyethyl chitosan (EAHECS) weight loss experimental group (TA1-3): TA1 group: basal feed + 2.5% EAHECS, TA2: basal feed + 5% EAHECS, TA3: basal fe...

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Abstract

Water and oil soluble O-chitosan derivatives, their preparation and use thereof, wherein the synthesized chitosan upper substitutive derivative comprises o-ethlamine hydroxide ethyl chitosan and 0-2' -hydroxylpropyl -N, N-dimethyl octadecyl ammonium chloride chitosan, which is prepared through the reaction of N-phthaloyl chitosan with chlorohydrin, chlorethamin hydrochlorate and N,N dimethyl octadecyl amine hydrochlorate and epichlorohydrin in dimethyl carbinol medium.

Description

technical field [0001] The invention relates to a water- and oil-soluble O-chitosan derivative and its preparation and application. It belongs to the preparation and application technology of water- and oil-soluble O-chitosan derivatives. Background technique [0002] Chitosan, the only alkaline polysaccharide found so far in nature, has been proven to have a significant adsorption effect on fat, and has begun to be used in the latest weight-loss drugs. In Japan, chitosan weight-loss drugs have developed rapidly and have become the mainstream of weight-loss drugs. The Japanese Ministry of Health and Welfare allocated 6 billion yen to some medical universities in 1985 as the cost of basic research and application development of chitin. The Japanese chitosan health product "Jiu Duo Shan" entered the Chinese market in 1996, and got back 1 billion yuan from China in one year, equivalent to 14.3 billion yen, which was 2.3 times the funding allocat...

Claims

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Application Information

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IPC IPC(8): A61K31/722A61P3/04C08B37/08
Inventor 刘晓非庄旭品姚炳佳姚康德
Owner TIANJIN UNIV
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