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High molecular anticarcinogenic prodrug, its preparing method and use

A polymer and anticancer drug technology, applied in the field of medicine and chemical industry

Active Publication Date: 2007-10-03
SICHUAN YINGRUI PHARMA TECH CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After the prodrug was incubated in the pectinase solution for 2h, 35.1% of ketoprofen was released, and after 8h of incubation, 96.2% of ketoprofen was released accumulatively, so pectin can also be used as an ideal prodrug carrier. However, the above reported fruit The use of glue is only a common excipient. At present, there is no report on pectin as a polymer carrier, which is covalently bonded with anticancer drugs to prepare a compound drug.

Method used

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  • High molecular anticarcinogenic prodrug, its preparing method and use
  • High molecular anticarcinogenic prodrug, its preparing method and use
  • High molecular anticarcinogenic prodrug, its preparing method and use

Examples

Experimental program
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Effect test

Embodiment 1

[0084] Example 1: Synthesis of 5-fluorouracil-pectin prodrugs:

[0085] During its preparation, dissolve 15mmol of 5-fluorouracil in a mixed solvent of 30ml of anhydrous pyridine and 50ml of anhydrous sulfolane, control the temperature at 15°C, stir slowly and dropwise add 20ml of anhydrous toluene solution containing 1.4ml (about 16mmol) of oxalyl chloride, dropwise After the addition, control the temperature at 50°C, stir for 4 hours, weigh 1g of pectin and add it to the reaction bottle, control the temperature at 50°C, and stir for 48 hours. After the reaction, add acetone to precipitate, centrifuge, dissolve the precipitate in secondary water, and use The dialysis bag was dialyzed and vacuum-dried at 60°C to obtain the water-soluble 5-fluorouracil-pectin prodrug. Its synthesis process is as follows:

[0086]

[0087] Molecular structure of pectin

[0088]

Embodiment 2

[0089] Embodiment 2: the synthesis of alzyme-pectin prodrug:

[0090] In the preparation process, dissolve 0.2mmol azin in a mixed solvent of 20ml sulfolane and 10ml anhydrous pyridine, control the temperature at 15°C, and slowly add 10ml anhydrous toluene solution containing 0.11ml (about 1.2mmol) oxalyl chloride dropwise with stirring in the dark After the dropwise addition, continue to stir for 4 hours, weigh 0.3g of pectin and add it to the reaction bottle, control the temperature at 30°C, and stir for 48 hours. Dialysis, vacuum drying, to obtain water-soluble alzin-pectin prodrug. Its synthesis process is as follows

[0091]

[0092] (Note: R stands for R 1 represent )

Embodiment 3

[0093] Embodiment 3: daunorubicin-pectin prodrug:

[0094] In the preparation process, dissolve 0.2mmol daunorubicin in a mixed solvent of 20ml sulfolane and 10ml anhydrous pyridine, control the temperature at 15°C, and slowly add 0.1ml (about 1.15mmol) oxalyl chloride containing 10ml anhydrous Toluene solution, after the dropwise addition, continue to stir for 4 hours, weigh 0.3g pectin into the reaction bottle, control the temperature at 30°C, and stir for 48 hours. After the reaction is completed, add acetone to precipitate, centrifuge, and dissolve the precipitate in secondary water. The dialysis bag was dialyzed and vacuum-dried to obtain the water-soluble daunorubicin-pectin prodrug. Its synthesis process is as follows:

[0095]

[0096] (Note: R stands for R 1 represent )

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Abstract

An anticancer high-molecular precursor medicine C-Spacer-P, where P is high- molecular pectin, C is an anticancer medicine containing amino radical or hydroxy radical, and Spacer is the spacing radical, is prepared by bonding the amino or hydroxy of an anticancer medicine with the hydroxy, carboxy, or hydroxymethyl of high- molecular pectin via spacing radical. It is an injection suitable for the solid cancer, and cancerous ascites or hydrothorax.

Description

technical field [0001] The invention relates to a polymer anticancer prodrug and its preparation method and application, belonging to the field of medicine and chemical industry. Background technique [0002] Traditional anticancer drugs are administered orally, intravenously, etc., and then reach a certain blood concentration and distribute throughout the body to produce therapeutic effects. The biggest defect of this treatment method is the lack of selectivity. Most commonly used anticancer drugs have low molecular weight and are easy to diffuse in the body, resulting in relatively even tissue distribution and large toxic and side effects, which seriously affect the anticancer therapeutic value of these drugs. It is generally believed that an ideal targeting vector can solve the above-mentioned shortcomings. At present, the targeting carriers that are being studied at home and abroad and have made some progress mainly include: macromolecular carrier systems, microparticle...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K45/00A61K31/63A61K31/409A61K31/505A61K38/04A61P35/00A61K47/61
Inventor 唐小海成明宋鑫邱宇
Owner SICHUAN YINGRUI PHARMA TECH CO
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