Ursodeoxycholic acid entecavir acidamide and preparation method and use thereof

A technology of ursodeoxycholic acid and oxycholic acid, which is applied in the field of treatment of hepatitis B virus infection, can solve the problems of large side effects and low curative effect

Inactive Publication Date: 2008-03-05
曾昭斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, interferon treatment for 1 year, the HBeAg conversion rate can reach 33%, but the side effects are relatively large, and the curative effect on Asians is slightly lower. The curative effect and safety of pegylated interferon are better than ordinary interferon; The biggest probl

Method used

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  • Ursodeoxycholic acid entecavir acidamide and preparation method and use thereof
  • Ursodeoxycholic acid entecavir acidamide and preparation method and use thereof
  • Ursodeoxycholic acid entecavir acidamide and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: Preparation of ursodeoxycholic acid entecavir amide

[0029] Reaction formula:

[0030]

[0031] Operation steps Put 100mL DMF into the beaker, add (10mmol, 4.0g) ursodeoxycholic acid and (10mmol, 1.4ml) triethylamine under stirring, cool the temperature of the reaction solution to -15°C under stirring, then add ( 15mmol, 2mL) isobutyl chloroformate. After stirring for 2 minutes, a solution of entecavir (10 mmol, 2.8 g) and triethylamine (15 mmol, 2.2 mL) dissolved in 40 ml of DMF was added, and the temperature of the reaction solution was maintained at -15 ° C. After stirring the reaction mixture for 30 min, it was left at room temperature for 1 hour. Filter to remove triethylamine chloride therein, then distill and concentrate the filtrate under reduced pressure, add the concentrate to 400ml of ethanol and heat it appropriately to dissolve, filter and discard the insoluble matter, wash the filtrate twice with an appropriate amount of chloroform solut...

Embodiment 2

[0036] Embodiment 2: the preparation tablet of pharmaceutical composition:

[0037] Element

[0038] Preparation method: grind the raw materials and auxiliary materials separately, pass through a 100-mesh sieve, and set aside. Dissolve an appropriate amount of sodium carboxymethyl starch in water to obtain a 2% sodium carboxymethyl starch solution as a binder. Mix the main and auxiliary materials thoroughly. Use 2% sodium carboxymethyl starch solution as a binder to make a suitable soft material, pass through a 30-mesh sieve to granulate, dry the wet granules at about 60°C, pass through a 30-mesh sieve for granulation, add magnesium stearate and mix well . Determine the drug content in the granules, calculate the theoretical tablet weight, and compress the tablet. Take an appropriate amount of LE film coating agent, add it to 75% ethanol solution, stir to disperse it evenly, and obtain 7% LE film coating solution. Measure the tablet core content and dissolution ...

Embodiment 3

[0039] Embodiment 3: the preparation of pharmaceutical composition

[0040] Element

[0041] Preparation method: respectively pulverize the main drug and auxiliary materials in the prescribed amount through an 80-mesh sieve, and set aside. Get sodium carboxymethyl starch and add water to make 2% sodium carboxymethyl starch solution as a binder. The main ingredient and auxiliary materials are uniformly mixed in equal amounts, added with 2% sodium carboxymethyl starch solution, passed through a 20-mesh sieve to granulate, dried at 55°C, and granulated at 20-mesh to obtain dry granules. Add the dry particles to 100-mesh micronized silica gel and mix well. Put in capsules and get ready.

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PUM

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Abstract

The present invention relates to one kind of new compound, entecavir amido ursodesoxycholate, its preparation process, medicine composition with the compound as active component and the application of the compound in preventing and treating hepatitis B.

Description

field of invention [0001] The present invention relates to a new compound ursodeoxycholic acid entecavir amide, a preparation method thereof, a pharmaceutical composition using the compound as an active ingredient, and an application of the compound in treating hepatitis B virus infection. Background of the invention [0002] According to the World Health Organization estimates: there are currently about 350 million people in the world who are infected with HBV, and some of these infected people can develop liver cirrhosis and liver cancer. Of these 350 million people, 75% live in Asia, and there are 120 million HBV-infected people in China alone. According to WHO data, more than 500,000 people die from liver cirrhosis and primary liver cancer every year, and 80% of liver cancers are caused by hepatitis B. According to the survey data from 1992 to 1995, there are about 30 million chronic hepatitis B patients in my country. According to the latest data from the Ministry of ...

Claims

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Application Information

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IPC IPC(8): C07J43/00A61K31/58A61K9/48A61K9/20A61K9/19A61P1/16A61P31/12
Inventor 曾昭斌丁武孝朱靖华
Owner 曾昭斌
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