Preparation for modified chitosan metal complexes micro-sphere used for carrying medicament and preparation for the modified chitosan

A chitosan derivative and chitosan technology, applied in the field of medicine, can solve problems such as poor solubility, low biological activity, and limited application range, and achieve the effects of low cost, good slow-release performance, and increased solubility

Inactive Publication Date: 2008-01-16
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, natural chitosan has a large molecular weight, and its compact crystal structure, insoluble in common solven

Method used

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  • Preparation for modified chitosan metal complexes micro-sphere used for carrying medicament and preparation for the modified chitosan
  • Preparation for modified chitosan metal complexes micro-sphere used for carrying medicament and preparation for the modified chitosan

Examples

Experimental program
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Example Embodiment

[0029] Example 1

[0030] The preparation of modified chitosan α-ketoglutarate condensed chitosan (KCTS) is as follows: Weigh a dry sample of chitosan (CTS), swell it with distilled water, add α-ketoglutarate, filter, and use NaOH solution Adjust the pH to 4-5, continue the reaction in a 35-38℃ water bath, add sodium borohydride, adjust the pH=6.5-7.0 with dilute HCl solution, continue the reaction for 20-28h, pour the reaction mixture into 90-97% ethanol to terminate the reaction , KCTS is separated out, filtered under reduced pressure, washed, the product is transferred to a Soxhlet extractor for continuous extraction for 6-9 hours, and dried to obtain a white powdery solid α-ketoglutarate chitosan (KCTS).

[0031] Using chitosan molecule on C 2 Free amino-NH 2 The macromolecule reaction with α-ketoglutaric acid can synthesize the functional polymer α-ketoglutarate chitosan (KCTS) with Schiff base group. The solubility of the prepared KCTS has been improved to a certain extent, ...

Example Embodiment

[0032] Example 2

[0033]The preparation of modified chitosan hydroxylamine α-ketoglutarate chitosan (HKCTS) is: 0.5-1.0g KCTS is dissolved in water, and the pH of the polymer solution is adjusted to 4.0- with 0.1mol / L hydrochloric acid solution. 5.0 Add 0.74-1.48g of dicyclohexylcarbodiimide (DCCI) slowly to the mixture under stirring, after 2-3 hours of reaction, add 5.0-10.0g of hydroxylamine hydrochloride, and further react for 1 hour under stirring; then use sodium hydroxide Adjust the pH value to 9.0-10.0, and stir at room temperature for more than 20-28 hours until the reaction mixture is terminated when HKCTS precipitation occurs in a mixture of 10-20ml concentrated hydrochloric acid and 250-300ml acetone. After filtering and washing, the obtained polymer was dried overnight at room temperature.

[0034] The solubility of the prepared HKCTS is greatly improved, and it can be completely dissolved in water, soluble in 2% NaOH and 10% ammonia. HKCTS introduces -CONHOH group, ...

Example Embodiment

[0035] Example 3

[0036] (1). Accurately weigh 1.000g of KCTS (prepared), add it to 20.00mL of 0.1mol / L NaOH solution, fully swell or dissolve for 30min, and stir evenly;

[0037] (2) Accurately weigh 1.000g of oral theophylline drug, add it to the above system, stir for 1 hour at a constant temperature of 40℃, and obtain a milky white viscous polymer solution;

[0038] (3), accurately weigh 1.8gZnSO 4 ·7H 2 O is made into ZnSO with a concentration of 18mg / mL 4 ·7H 2 O aqueous solution 100.00mL;

[0039] (4) Slowly add the milky white viscous polymer solution to 18mg / mL ZnCl 2 In 100.00 mL of the aqueous solution, adjust the pH of the system to about 6, keep constant temperature and stirring in a water bath for more than 9 hours, that is, a large number of white polymer microspheres are generated;

[0040] (5) Carry out vacuum suction filtration, and the filtrate is washed 2-3 times with distilled water and a small amount of absolute ethanol successively, and vacuum-dried at 35°C...

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Abstract

Disclosed are the preparation of a modified chitosan metal complex microsphere used for drug-loading and the preparation of the modified chitosan. The invention provides a preparation method of a modified chitosan which has good solubility, high biological activity and can reduce the dependence to PH value during drug release, and provides a preparation method of a chitosan derivative based metal complex microsphere for drug-loading. The micorshpere prepared by the invention can be used for drug-loading, and is characterized in improving the drug releasing and simple preparation process.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the preparation of a novel modified chitosan and the preparation of the modified chitosan derivative metal complex drug-loaded microspheres. Background technique [0002] In recent years, the application of chitosan in the pharmaceutical field has attracted more and more attention. It can be used as an adjuvant for pharmaceutical preparations, such as research on the encapsulation of pharmaceutical preparations such as controlled release, sustained release, and targeting; Sugar has active groups such as amino groups. These active groups can be chemically bonded with various drugs to generate polymer drugs and reduce the side effects of anticancer drugs on the human body, and chitosan, the degradation product of chitosan, has a certain Anti-cancer effect; in addition, chitosan itself can also be used as medicine and health care products. The Japanese government has invested 6 billi...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61K9/14A61K47/36
Inventor 黄可龙丁萍刘素琴刘艳飞王蔚玲李桂银
Owner CENT SOUTH UNIV
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