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Hydrophilic polymer-boxwood extract conjugate and its medicine composition

A technology of hydrophilic polymers and conjugates, which is applied in the direction of drug combinations, steroids, pharmaceutical formulations, etc., can solve the problems of poor blood, short half-life, easy crystallization, etc., to improve stability and water solubility, prolong The effect of the active cycle

Inactive Publication Date: 2008-11-19
JENKEM TECH CO LTD TIANJIN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its solubility is poor, and it is currently limited to oral tablets. Because of the addition of acid components to aid in dissolution, injections for injection are prone to crystallization in biological body fluids, causing unnecessary problems, such as high toxicity and poor blood.
And its half-life in the organism is short, and the duration is not long, and oral preparations need to be taken several times a day to ensure the curative effect

Method used

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  • Hydrophilic polymer-boxwood extract conjugate and its medicine composition
  • Hydrophilic polymer-boxwood extract conjugate and its medicine composition
  • Hydrophilic polymer-boxwood extract conjugate and its medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Synthesis of amido-bonded polyethylene glycol acetic acid and cycloevergreen boxine D

[0061]

[0062] 5 grams of methoxypolyethylene glycol acetic acid (mPEG-O-CH 2 -COOH, Mw5000), 0.25 grams of Cyclophylline D (D 1 ), 0.2 g of 4-dimethylaminopyridine (DMAP) was dissolved in 50 ml of anhydrous dichloromethane, and 0.32 g of dicyclohexylcarbodiimide (DCC) was added. Stir overnight under nitrogen protection, excess solvent is removed by rotary evaporation, and 20 ml of 1,4-dioxane is added to the residue. The precipitate was removed by filtration and the filtrate was partially concentrated by rotary evaporation. 100 mL of isopropanol was added to the residue, and the product was collected by filtration and dried in vacuo. N,N'-dimethoxypolyethylene glycol acetic acid-cycloevergreen boxine D amide (1) was obtained, yield: 4.2 g (83%), melting point: 57-59°C.

Embodiment 2

[0064] Synthesis of Polyethylene Glycol Polycarboxy-Oligopeptide and Cycloevergreen Echrysene D Bonded with Amide Group

[0065]

[0066] The method is the same as in Example 1, except that methoxypolyethylene glycol acetic acid is replaced with methoxypolyethylene glycol-glutamic acid dipeptide (Mw10500). Methoxypolyethylene glycol glutamic acid dipeptide-cycloevergreen boxine D amide (2) was obtained, yield: 0.9 g (90%), melting point: 58-59°C.

Embodiment 3

[0068] Synthesis of Amide-Bonded Polyglutamic Acid and Cycloevergreen Box D

[0069]

[0070] The method is the same as in Example 1, except that methoxypolyethylene glycol acetic acid is replaced by polyglutamic acid (Mw5000). Polyglutamic acid-cycloevergreen boxine D amide (3) was obtained, yield: 0.9 g (90%).

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Abstract

The invention relates to a hydrophilic polymer-boxwood alkaline extractive or a combination of a derivative thereof which is shown in a general formula (1), wherein, P is the hydrophilic polymer, which is selected from polyethylene glycol, polyglutamic acid, polyaspartic acid, polypropylene glycol, polyvinyl alcohol, polypropylene morpholine and a copolymer thereof; n is an integer, which does not exceed the total quantity of hydroxyl group and amino group on the D; L is a linking group, which is selected from groups formed by ester group, carbonate group, amide group, amide ester group, ether group, urethane group and acetal; D is the boxwood alkaline extractive or the derivative thereof, which is selected from groups formed by cyclovirobuxine D, cycloprotobuxine A, cycloprotobuxine C, cyclovirobuxine C and derivatives thereof. The combination improves the water solubility of boxwoods, and prolongs the cycle half-life thereof in the organism.

Description

[0001] This application is a divisional application submitted on November 05, 2004 with the title of "hydrophilic polymer-boxwood extract combination and its pharmaceutical composition" and application number 200480029778.X. field of invention [0002] The present invention relates to a combination of hydrophilic polymer and boxwood extract and a pharmaceutical composition comprising the combination. Background technique [0003] Boxwood extract generally refers to boxwood alkaloids such as Cyclovirobuxine D (Cyclovirobuxine D, also known as Boxwood Ning), Cycloprotobuxine A (Cycloprotobuxine A), Cycloprotobuxine C (Cycloprotobuxine C), and Cycloviroxine C. Active substances of small molecules such as Cyclovirobuxine C. [0004] Boxwood is a plant in the boxwood family, Buxus microphyllum, which is produced in the south of the Yangtze River. "Compendium of Materia Medica" records that it is mainly used to promote qi and blood circulation, dispel dampness and dredge collater...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/57A61K9/10C07J53/00A61K31/56C08G65/329C08G65/333
CPCC08G65/329A61K31/56C07J53/00C08G65/33303C08H8/00A61P9/00A61P9/10
Inventor 朱德权嵇世山
Owner JENKEM TECH CO LTD TIANJIN
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