Amino-containing cellulose grafted copolymer capable of regulating gastrointestinal smooth muscle

A technology of cellulose grafting and copolymers, which is applied in the direction of drug combination, medical preparations containing active ingredients, digestive system, etc., and can solve problems such as strong side effects and cardiovascular and cerebrovascular diseases

Inactive Publication Date: 2012-09-26
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these drugs are easily absorbed into the blood, easily interact with blood vessel walls, cause cardiovascular and cerebrovascular diseases, and produce strong side effects, so some of these drugs are withdrawn from the market or restricted in use

Method used

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  • Amino-containing cellulose grafted copolymer capable of regulating gastrointestinal smooth muscle
  • Amino-containing cellulose grafted copolymer capable of regulating gastrointestinal smooth muscle
  • Amino-containing cellulose grafted copolymer capable of regulating gastrointestinal smooth muscle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1: prepare the amino group-containing cellulose graft copolymer of the present invention

[0054] Weigh 0.1 g of hydroxypropyl cellulose (Sigma-aldrich) with a weight-average molecular weight of 80,000 and a molar substitution degree of 3.5, add it to 50 mL of deionized water, blow nitrogen gas, and dissolve it completely in a constant temperature oil bath at 40°C. Adjust the pH of the solution to 1.5 with concentrated nitric acid, add 1.96g of 2-methacryloyloxyethylphosphorylcholine, and stir to make it fully dissolved. Then add 5 mL of cerium ammonium nitrate aqueous solution (0.008 g / mL), continue to blow nitrogen, then seal, and react for 2 hours. Hydroquinone was added to terminate the reaction. Add 10 mL of sodium hypochlorite aqueous solution (0.01 g / mL) to oxidize for 10 minutes. The reaction mixture was precipitated, filtered, dialyzed, and dried to obtain a cellulose graft copolymer containing amino groups: hydroxypropyl cellulose grafted poly-2-m...

Embodiment 2

[0056] Embodiment 2: prepare the amino group-containing cellulose graft copolymer of the present invention

[0057] The specific implementation steps are as in Example 1, except that the weight-average molecular weight of hydroxypropyl cellulose is 60,000, and the molar substitution degree is 2; the weight-average molecular weight of the cellulose graft copolymer containing amino groups obtained is 100,000 .

[0058] figure 2 It can be seen from the hydrogen nuclear magnetic spectrum that the degree of polymerization of the side chain of the prepared copolymer is m=3.

Embodiment 3

[0059] Example 3: Use of the copolymer of the present invention in regulating gastrointestinal smooth muscle

[0060] Step (1): Preparation of aqueous solution of amino-containing cellulose graft copolymer: Weigh 9 parts, each 2.56 mg, of hydroxypropyl cellulose grafted poly-2-methacryloyl prepared in Example 1 Oxyethylphosphorylcholine was dissolved in different volumes of distilled water to obtain amino group-containing cellulose graft copolymer aqueous solutions with different concentrations as shown in the table below.

[0061]

[0062] Step (2): Preparation of isolated rat jejunum and colon longitudinal smooth muscle strips: the healthy rats were killed by cervical dislocation, and the jejunum (10 cm from the duodenum) and colon (2 cm from the ileocecal) were quickly taken to prepare Longitudinal muscle strips were fixed in smooth muscle grooves. Low calcium, low potassium, atropine and 5-HT4 receptor antagonists were used to induce the low contraction state of the smo...

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Abstract

The invention relates to an amino-containing cellulose grafted copolymer ( represented by formula (I)), a preparation method and an application of the copolymer, as well as a compound containing the copolymer. In the formula I, R1, R2 and R3 are the same as or different from each other, each is selected from H, CH3, -COOH, -CH2OH, -CH2CH2OH and/or -CH2CH(CH3)OH, respectively, one in R1, R2 and R3 is -CH3 when the other two are different, or one in R1, R2 and R3 is -COOH when the other two are different; R4 is H or CH3; R5 is the group containing amino; n is the degree of polymerization of cellulose of the main chain structural unit of the copolymer, and the value of n is determined according to the used cellulose derivative. The cellulose copolymer provided by the invention is capable of regulating gastrointestinal smooth muscle, unlikely to be degraded by gastrointestinal enzymes, and absorbed less or un-absorbed, so that not only the initial treating effect is held but also the gastrointestinal part is regulated, and thus the side effect is minimized.

Description

technical field [0001] The invention relates to a cellulose graft copolymer material containing an amino group, its preparation method and its use for regulating gastrointestinal smooth muscle, and also relates to a cellulose graft copolymer containing an amino group combination. Background technique [0002] Irritable bowel syndrome (irritable bowel syndrome, IBS) is a common chronic functional gastrointestinal disease, with abdominal pain, abdominal discomfort, accompanied by abnormal bowel habits and stool properties as the main symptoms, it persists or intermittent attacks, and lack of Abnormalities in morphological and biochemical markers that explain symptoms. According to epidemiological surveys, the prevalence of IBS in Western countries is above 10%, and the prevalence in Chinese communities exceeds 10.5%. Although the prognosis of IBS is good, it affects the work and life of patients to varying degrees due to its recurrent attacks, and directly or indirectly cons...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F251/02A61K31/785A61P1/00
Inventor 康宏亮刘瑞刚叶冬梅黄勇
Owner INST OF CHEM CHINESE ACAD OF SCI
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