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Glucan-containing pharmaceutical composition and preparation method thereof

A technology of dextran and composition, which is applied in the field of dextran-containing pharmaceutical composition and its preparation, and can solve the problems of large toxic side effects and cytotoxicity

Active Publication Date: 2013-04-17
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Doxorubicin is a broad-spectrum antineoplastic drug that has effects on a variety of tumors. However, it can produce a wide range of biochemical effects on the body, has strong cytotoxicity to normal cells, and has large toxic and side effects.

Method used

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  • Glucan-containing pharmaceutical composition and preparation method thereof
  • Glucan-containing pharmaceutical composition and preparation method thereof
  • Glucan-containing pharmaceutical composition and preparation method thereof

Examples

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preparation example Construction

[0036] like figure 1 As shown, the preparation method of the above-mentioned glucan-containing pharmaceutical composition comprises the following steps:

[0037] S10, prepare dextran-polyethyleneimine, and the dextran and polyethyleneimine are connected by a urethane bond.

[0038] The preparation method of dextran-polyethyleneimine comprises the following steps:

[0039] Step 1. Dissolve dextran, 4-dimethylaminopyridine and 4-nitrophenyl chloroformate (PNC) in a mass ratio of 1:0.02~0.05:0.2~0.5. In a mixed solution of dimethyl sulfoxide and pyridine, react in an ice bath for 2 to 6 hours, drop the reaction dropwise into a mixed solution of ethanol and ether to form a precipitate, collect the precipitate by centrifugation, wash with ether, and dry in vacuo Dextran-4-nitro-p-phenylchloroformate is obtained.

[0040] The molecular weight of dextran can be 6000-70000. Dextran has the advantages of low price, good biocompatibility, and biodegradability. When the glucan-conta...

Embodiment 1

[0065] Dissolve 0.3 g of dextran with a molecular weight of 6000 in 12 mL of a mixed solution of dimethyl sulfoxide and pyridine with a volume ratio of 1:1, add 11.28 mg of 4-dimethylaminopyridine and 93 mg of 4-nitro-p-phenylchloroformic acid The ester was reacted in an ice bath for 4 hours. After the reaction, the reaction was dropped into a mixed solution of 120 mL of ethanol and ether to form a precipitate. The precipitate was collected by centrifugation, washed with ether, and dried in vacuo to obtain DEX-PNC.

[0066] The DEX-PNC aqueous solution was added dropwise to an aqueous solution of PEI with a molecular weight of 2000, the molar ratio of PEI and dextran was 1:20, and the reaction was carried out under stirring conditions for 24 hours. In the aqueous solution, a dialysis membrane with a molecular weight cutoff of 3500 was used. Dialyzed for 2 days, filtered and freeze-dried to obtain DEX-PEI.

[0067] Dissolve 5 mg of DOX in 1 mL of DMF solution, add cis-aconitic ...

Embodiment 2

[0073] Dissolve 0.3 g of dextran with a molecular weight of 40,000 in a 1:1 volume ratio of 10 mL of a mixed solution of dimethyl sulfoxide and pyridine, add 20.8 mg of 4-dimethylaminopyridine and 112.08 mg of 4-nitro-p-phenyl chloride Formate, reacted in an ice bath for 2 hours. After the reaction, the reaction was dropped into a mixed solution of 200 mL of ethanol and ether to form a precipitate. The precipitate was collected by centrifugation, washed with ether, and dried in vacuo to obtain DEX-PNC.

[0074] The DEX-PNC aqueous solution was added dropwise to an aqueous solution of PEI with a molecular weight of 600, the molar ratio of PEI and dextran was 1:10, and the reaction was carried out under stirring conditions for 12 hours. In the aqueous solution, a dialysis membrane with a molecular weight cut-off of 3500 was used. Dialyzed for 4 days, filtered and freeze-dried to obtain DEX-PEI.

[0075] Dissolve 5 mg of DOX in 1 mL of DMF solution, add cis-aconitic anhydride acc...

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Abstract

The invention discloses a glucan-containing pharmaceutical composition which comprises glucan-polyethyleneimine and a pharmaceutically active component activated by cis-aconitic acid anhydride. Glucan and polyethyleneimine are bonded through urethane bonds, cis-aconitic acid anhydride and the pharmaceutically active component are bonded through amide bonds, and the pharmaceutically active component activated by cis-aconitic acid anhydride and glucan-polyethyleneimine are bonded through amide bonds which are jointed between cis-aconitic acid anhydride and polyethyleneimine. After entering a human body, the glucan-containing pharmaceutical composition forms a shell-core structure, can not be identified by the reticuloendothelial system, and gradually concentrates at the site of a tumor mass. Under the acidic conditions of the tumor site, the amide bonds between the pharmaceutically active component activated by cis-aconitic acid anhydride and polyethyleneimine are broken to release a large amount of the pharmaceutically active component, while the release of the pharmaceutically active component at other sites is extremely low, thus, the toxicity to the health cells is reduced, and the toxic or side effect is reduced. The invention discloses a preparation method of the glucan-containing pharmaceutical composition mentioned above.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a glucan-containing pharmaceutical composition and a preparation method thereof. Background technique [0002] Dextran (DEX) has good biocompatibility, biodegradability, and no immunogenicity, which enables micelles to escape the recognition of the reticuloendothelial system, so that they can circulate in the blood system for a long enough time , it is increasingly favored by the advantages of high permeability and retention effect at the tumor site into tumor cells. Polyethyleneimine (PEI), as a cationic polymer, has the advantages of low cost and good stability, and can be effectively used for non-viral gene carriers. Doxorubicin is an anti-tumor antibiotic that can effectively inhibit the synthesis of RNA and DNA, so as to achieve the effect of treating cancer. Doxorubicin is a broad-spectrum antitumor drug, which has effects on a variety of tumors. However, it can produce ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00C08G81/00C08B37/02
Inventor 蔡林涛王碧刘朋龚萍石碧华易虎强岳彩霞
Owner SHENZHEN INST OF ADVANCED TECH
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