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Colon-targeted pro-drug based on nanometer cellulose carrier and preparation method of colon-targeted pro-drug

A nano-cellulose and colon-targeting technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, anti-tumor drugs, etc., can solve the problems of difficult chemical bonds breaking, no practical application value, and limited targeting activity. The effect of good encapsulation and good drug controlled release performance

Active Publication Date: 2015-04-29
福建省沙县鸿源安生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since most drug units or targeting units cannot be directly connected to macromolecular carriers through chemical reactions, even if it is possible to react, the coupling efficiency will be too low due to the steric hindrance effect of carrier molecular chains or drug molecules, or the targeting will be limited. activity, so it has no practical application value; even if the drug is directly connected to the carrier, the chemical bond formed by the direct connection between the drug and the carrier is difficult to break and the drug cannot be released

Method used

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  • Colon-targeted pro-drug based on nanometer cellulose carrier and preparation method of colon-targeted pro-drug
  • Colon-targeted pro-drug based on nanometer cellulose carrier and preparation method of colon-targeted pro-drug

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Weigh 1 g dry sample of nanocellulose, 0.08 g 4-dimethylaminopyridine (DMAP), 1.5 g alanine, 1.25 g 1-ethyl-(3-dimethylaminopropyl) carbodiimide salt Hydrochloride (EDC·HCl), 0.75 g of fluorenylmethoxycarbonyl chloride (Fmoc-Cl), 50 mL of dimethyl sulfoxide was added, the reactants were mixed evenly, and the reaction was performed under magnetic stirring at room temperature for 20 h. After the reaction was completed, the liquid was removed by centrifugation at 9000 rpm, and then the remaining solid sample was washed with deionized water multiple times, and then washed twice with ethanol solution to obtain an Fmoc-protected amino nanocellulose sample. To remove Fmoc protection, disperse it in 20 mL of 10% (v / v) piperidine / DMF solution, stir for 20 min to remove Fmoc, and obtain amino acid esterified nanocellulose, which is vacuum-frozen at -53°C Dry the sample.

[0021] Weigh 0.1 g dry sample of amino acid esterified nanocellulose, 0.3 g N-hydroxysuccinimide (NHS), 0.3 ...

Embodiment 2

[0023]Weigh 1 g dry sample of nanocellulose, 0.08 g 4-dimethylaminopyridine (DMAP), 1.5 g leucine, 1.25 g 1-ethyl-(3-dimethylaminopropyl) carbodiimide salt Hydrochloride (EDC·HCl), 0.75 g of fluorenylmethoxycarbonyl chloride (Fmoc-Cl), 50 mL of dimethyl sulfoxide was added, the reactants were mixed evenly, and the reaction was performed under magnetic stirring at room temperature for 20 h. After the reaction was completed, the liquid was removed by centrifugation at 9000 rpm, and then the remaining solid sample was washed with deionized water multiple times, and then washed twice with ethanol solution to obtain an Fmoc-protected amino nanocellulose sample. To remove Fmoc protection, disperse it in 20 mL of 10% (v / v) piperidine / DMF solution, stir for 20 min to remove Fmoc, and obtain amino acid esterified nanocellulose, which is vacuum-frozen at -53°C Dry the sample.

[0024] Weigh 0.1 g dry sample of amino acid esterified nanocellulose, 0.5 g N-hydroxysuccinimide (NHS), 0.5 g...

Embodiment 3

[0026] The filter paper was disintegrated in a fiber standard disintegrator at 3000 r / min for 20 minutes to obtain a uniformly dispersed filter pulp, which was freeze-dried for later use. Take 3.0 g of dried filter pulp, stir and disperse in 100 mL of acetic acid solution, and let it stand overnight (15 h) to preactivate the cellulose. Then 1.5 mL of concentrated sulfuric acid was added dropwise as a catalyst, and the suspension was placed in an oil bath at 80 °C and stirred at 300 r / min for 6 h. After reacting for a certain period of time, the reaction system was ultrasonically treated at an ultrasonic frequency of 40 kHz, a power of 250 W, an ultrasonic temperature of 75 °C, and an ultrasonic time of 5 h. After the reaction was completed, the suspension was centrifuged repeatedly with deionized water at 9000 r / min, and then unreacted reagents and by-products were eluted with acetone / ethanol mixture (1 / 1 volume ratio). Finally, the collected maleic anhydride esterified nanoc...

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Abstract

The invention discloses a colon-targeted pro-drug based on a nanometer cellulose carrier and a preparation method of the pro-drug. The colon-targeted pro-drug is prepared by linking a carrier and a drug intermediate through a chemical bond by taking the nanometer cellulose as the carrier and amino acid as a connecting arm. The researches prove that as the particle size of the nanometer cellulose is quite small and the number of reaction activity sites on the surface is large, the drug can be tightly coated. The in-vitro assay researches prove that the pro-drug can effectively achieve colon-targeted drug release to meet the requirements of the colon-targeted drug carrier, and thus can be applied to developing a novel targeted drug for treating a disease at the colon part.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a colon targeting prodrug based on a nanocellulose carrier and a preparation method thereof. Background technique [0002] The colon (colon) is located in the posterior part of the gastrointestinal tract of the body and is the organ involved in various diseases. Common diseases include ulcerative colitis, Crohn's disease, colon cancer, and hemorrhagic colitis. Due to the complex environmental factors of the gastrointestinal tract, conventional oral preparations are generally absorbed or degraded before reaching the colon and rectum, and cannot specifically act on the lesion. Therefore, chemical and pharmaceutical techniques are used to change the physical and chemical properties of the drug. Prepare a colon-targeted drug delivery system, also known as colon-specific drug delivery system (CDDS), so that the therapeutic drug is not released in the stomach and small intesti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61P1/00A61P1/04A61P35/00C08B15/06
Inventor 唐丽荣黄彪李涛卢麒麟陈学榕
Owner 福建省沙县鸿源安生物科技有限公司
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