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Scutellarin prodrug using carboxymethyl chitosan as the carrier and method for preparing the same

A technology of carboxymethyl chitosan and scutellarin, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of ethylene glycol and other problems, and achieve easy realization , improve bioavailability, simple preparation method

Inactive Publication Date: 2008-01-02
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of polyethylene glycol as a prodrug carrier also has obvious disadvantages, and its degradation process will produce ethylene glycol and diethylene glycol, which have certain biological toxicity.

Method used

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  • Scutellarin prodrug using carboxymethyl chitosan as the carrier and method for preparing the same
  • Scutellarin prodrug using carboxymethyl chitosan as the carrier and method for preparing the same
  • Scutellarin prodrug using carboxymethyl chitosan as the carrier and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Carboxymethyl chitosan (0.35 g, 1.5 mmol) prepared from methyl chitosan with a molecular weight of 2000 was dissolved in 100 ml of distilled water and stirred to fully dissolve it. Dissolve scutellarin (0.70 g, 1.5 mmol) in 20 ml of DMF, and add dropwise to the carboxymethyl chitosan solution with a dropping funnel. The above reaction solution was fully stirred, and the solution became light yellow, transparent and clear, and then 0.15 g of DMAP was added. DCC (0.35 g, 1.5 mmol) was dissolved in 10 ml of DMF, dropped into the reaction solution with a dropping funnel, and stirred at 50° C. for 24 hours. After the reaction is finished, filter the filtrate with a slow filter paper, centrifuge the filtrate, put the clear liquid in a pear-shaped bottle, and evaporate to dryness. Wash the light green solid on the wall of the pear-shaped bottle with n-propanol to form a large amount of precipitate, filter it, wash it with n-propanol until the filtrate is colorless, dry the pr...

Embodiment 2

[0037] Carboxymethyl chitosan (0.24 g, 1.0 mmol) prepared from methyl chitosan with a molecular weight of 4000 was dissolved in 80 ml of distilled water and stirred to fully dissolve. Dissolve scutellarin (0.94g, 2.0mmol) in 30ml DMF, and add it dropwise to the carboxymethyl chitosan solution with a dropping funnel. The above mixed solution was stirred sufficiently, and the solution became light yellow, transparent and clear, and then 0.10 g of DMAP was added. DCC (0.24 g, 1.0 mmol) was dissolved in 10 ml of DMF, and dropped into the above mixture with a dropping funnel. The reaction was stirred at 40°C. 120 hours. After the reaction is finished, filter with slow filter paper and centrifuge the filtrate, take the clear part and place it in a pear-shaped bottle, and evaporate to dryness. Wash the light green solid on the wall of the pear-shaped bottle with n-propanol to form a large amount of precipitate, filter it, wash it with n-propanol until the filtrate is colorless, dr...

Embodiment 3

[0039] Carboxymethyl chitosan (1.05 g, 4.5 mmol) prepared from methyl chitosan with a molecular weight of 20,000 was dissolved in 80 ml of distilled water and stirred to fully dissolve. Dissolve scutellarin (2.33g, 5.0mmol) in 30ml DMF, and add it dropwise to the carboxymethyl chitosan solution with a dropping funnel. The above mixed solution was stirred sufficiently, and the solution became light yellow, transparent and clear, and then 0.50 g of DMAP was added. EDC (1.14g, 4.5mmol) was dissolved in 10ml of distilled water, and dropped into the above mixture with a dropping funnel. The reaction was stirred at 25°C. After 192 hours, filter with slow filter paper and centrifuge the filtrate, take the clear part and place it in a pear-shaped bottle, and evaporate to dryness. Wash the light green solid on the wall of the pear-shaped bottle with n-propanol to form a large amount of precipitate, filter it, wash it with n-propanol until the filtrate is colorless, and dry the precip...

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Abstract

The invention provides a kind of scutellarin pro-drug taking carboxymethyl chitose as vector, and the preparation method, which takes carboxymethyl chitose as vector, takes dicyclo hexylcar bodiimide (DCC)as condensing agent, and produces new-type scutellarin pro-drug through reaction between carboxy group of scutellarin and amino of chitose. There are more active carboxy groups on main chain of scutellarin pro-drug, which is favorable for increasing pro-drug water solubility and biological utilization rate of scutellarin. The preparation method is simple and is easy to carry out.

Description

technical field [0001] The invention relates to a macromolecular prodrug and a preparation method thereof, in particular to a scutellarin prodrug and a preparation method thereof. technical background [0002] Scutellarin, also known as scutellarin, is the main component of scutellarin extracted from the plant Erigeron breviscapus of Compositae, and belongs to flavonoids. It has been proven to dilate blood vessels, increase cardiac coronary flow, increase cerebral blood flow, reduce cerebrovascular resistance, improve blood-brain barrier permeability, and resist platelet aggregation caused by adenosine diphosphate. It has been used clinically for many years. Clinically, it is mainly used to treat cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease, angina pectoris and other diseases, with definite curative effect. Its existing preparations include common tablets, injections and injection powders. Oral bioavailability of ordinary tablets...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/7048A61K47/36A61P9/10A61P7/02A61K47/61
Inventor 陈强迟波沈健林思聪
Owner NANJING UNIV
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