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Deoxypodophyllotoxin medicine-containing pharmaceutical composition and preparation method and preparation thereof

A technology of deoxypodophyllotoxin and pharmaceutical preparations, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve problems such as the inability to make glycoside derivatives

Active Publication Date: 2015-03-11
ZHEJIANG JIANFENG PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no hydroxyl group at the 4-position of DPT, so it cannot be made into glycoside derivatives

Method used

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  • Deoxypodophyllotoxin medicine-containing pharmaceutical composition and preparation method and preparation thereof
  • Deoxypodophyllotoxin medicine-containing pharmaceutical composition and preparation method and preparation thereof
  • Deoxypodophyllotoxin medicine-containing pharmaceutical composition and preparation method and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0091] Preparation method 1 of HA-CA amphiphilic hyaluronic acid copolymer, the reaction equation is as follows figure 1 :

[0092] Sodium hyaluronate was dialyzed against deionized water for 24 hours. After lyophilization, hyaluronic acid (5 mg, 1 mmol carboxyl) was dissolved in 1 mL deionized water.

[0093] Dissolve 10g of 5β-cholanic acid (CA) in 50mL of methanol, add 1.80mL of concentrated hydrochloric acid, seal the container with a film, and react at a constant temperature of 60°C under magnetic stirring for 6 hours, add excess distilled water to form a white precipitate, wash with water 3 times, and dry in vacuum to obtain Methyl cholanoate in white powder form.

[0094] Dissolve 9 g of methyl cholanoate in 50 mL of DMF, slowly add EDA (0.9 μmol), and react with magnetic stirring for 6 hours, then react at a constant temperature of 130°C for 6 hours under magnetic stirring, add excess distilled water to form a white precipitate, wash with water 3 times, and dry in va...

Embodiment 2

[0098] Preparation method 2 of HA-CA amphiphilic hyaluronic acid copolymer, the reaction equation is as follows figure 2 :

[0099] Sodium hyaluronate was dialyzed against deionized water for 24 hours. After lyophilization, hyaluronic acid (400 mg, 1 mmol carboxyl group) was dissolved in 5 ml deionized water, and 650 μl (1 mmol) tetrabutylammonium hydroxide (TBA) was added and stirred at 60° C. overnight.

[0100] Under the condition of stirring at 60°C, 120 mg of HA-TBA was dissolved in 12 ml of dimethyl sulfoxide (DMSO), and then 5β-cholanic acid (CA, 39.8 mg, 98.8 μmol),) EDC (72.8 mg, 379.8 μmol) and NHS (43.7 mg, 379.7 μM). After each reagent was dissolved, the reaction was stirred overnight at 40°C. The reacted system was fully dialyzed in methanol, methanol / water (1 / 1), pure water (containing 12.5 mg / ml of sodium chloride) and pure water successively, each dialyzing for 12 hours. After sufficient dialysis to remove the organic solvent, freeze-dry to obtain white po...

Embodiment 3

[0103] The preparation method three of HA-CA amphiphilic hyaluronic acid copolymer, the reaction equation is as follows image 3 :

[0104] The hyaluronic acid-5β-cholanic acid prepared by the method shown in Example 1 was dissolved in formamide, EDC was added, reacted at room temperature, and then NHS was added to prepare a reaction solution; then Dissolve in DMF, and slowly drop into the reaction solution prepared above to react to prepare the hyaluronic acid-5β-cholanic acid. The reacted system was fully dialyzed in methanol, methanol / water (1 / 1), pure water (containing 12.5 mg / ml of sodium chloride) and pure water successively, each dialyzing for 12 hours. After sufficient dialysis to remove the organic solvent, freeze-dry to obtain white powder HA-CA, which is stored at low temperature until use.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to a deoxypodophyllotoxin medicine-containing pharmaceutical composition and a preparation method and a preparation thereof. The deoxypodophyllotoxin medicine-containing pharmaceutical composition comprises a deoxypodophyllotoxin medicine and hyaluronic acid-5 beta cholanic acid, and the hyaluronic acid-5 beta cholanic acid coats the deoxypodophyllotoxin medicine in micellar form. The invention also discloses the preparation method and application of the pharmaceutical composition. The deoxypodophyllotoxin medicine-containing pharmaceutical composition has excellent tumor targeting property and good safety, reduces the toxic and side effects, improves the curative effect, can be used for intravenous injection, and has good application prospect in tumor target drug application system research and tumor treatment.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical composition containing deoxypodophyllotoxins, a preparation method and a preparation thereof. Background technique [0002] The 2014 World Cancer Report shows that cancer is one of the main "killers" of people's death in both developed and developing countries. Nearly half of the new cancer cases occurred in Asia, most of which were in China, which ranked first in the world in terms of new cancer cases. Currently, chemotherapy, surgery, and radiotherapy are the main means of treating cancer. Chemotherapy is a treatment method that uses chemical drugs to kill tumor cells, inhibit the growth and reproduction of tumor cells, and promote the differentiation of tumor cells. However, conventional chemotherapy drugs have almost no selectivity for tumor tissues and cells, so while killing tumor cells, they also kill normal cells and immune (resistance) cells to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K31/496A61K9/14A61K47/36A61P35/00C08B37/08
Inventor 蒋晓萌陈小元殷之武黄金龙朱雷张力文
Owner ZHEJIANG JIANFENG PHARM CO LTD
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