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Entikawei potassium used for curing acute and chronic hepatic disease and preparation method thereof

A technology for chronic liver disease and liver disease, applied in the field of medicine, can solve the problems of low solubility and unfavorable oral preparations to improve the bioavailability of drugs, and achieve the effect of good water solubility

Inactive Publication Date: 2007-10-17
邵长青
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The solubility is very small, which is not conducive to the preparation of oral preparations and the improvement of the bioavailability of drugs

Method used

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  • Entikawei potassium used for curing acute and chronic hepatic disease and preparation method thereof
  • Entikawei potassium used for curing acute and chronic hepatic disease and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1. Entecavir potassium and preparation method thereof

[0025] Take 5g of Entecavir, add 30ml of deionized water, add potassium hydroxide aqueous solution to dissolve, adjust the pH of the solution to 12, add about 50ml of acetone under stirring, after continuing to stir for 30min, let stand for 2 hours, suction filter, filter the precipitate with After washing with acetone for 2-3 times, vacuum-dry at 60°C to obtain off-white solid powder, which is entecavir potassium.

Embodiment 2

[0026] Embodiment two. the preparation of entecavir potassium tablet

[0027] Get 0.5 g of Entecavir Potassium prepared in Example 1, add an appropriate amount of carrier auxiliary materials (such as starch, lactose, polyvinylpyrrolidone, magnesium stearate, etc.), wet granulate, dry and granulate and make 1000 tablets with a tablet machine, Each tablet contains 0.5mg / tablet of active ingredient Entecavir Potassium for oral use.

Embodiment 3

[0028] Example 3. Preparation of Entecavir Potassium Capsules

[0029] Get Entecavir Potassium 1g prepared in Example 1, add an appropriate amount of carrier auxiliary materials (such as starch, lactose, polyvinylpyrrolidone, magnesium stearate, etc.), wet granulation, pack into 1000 empty capsules after drying, make each capsule The active ingredient Entecavir Potassium is 1mg / tablet for oral use.

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Abstract

The present invention relates to a drug potassium entecavir for treating liver disease, which has the following molecular structure, in which n is crystallization water number containing in potassium entecavir, Value range of n being 0-6. The present invention also provides a preparation method of potassium entecavir characterized as carrying out acid and alkaline reaction of entecavir and alkaline compound containing potassium, then adding precipitator for elution, filtering, drying, then potassium entecavir being obtained. The inventive potassium entecavir has merits of high stability, good dissolution, good curative effect and being convenient for clinic use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a potassium salt compound of entecavir, a preparation method thereof and an application thereof in medicine. Background technique [0002] Entecavir (Entecavir) is a 2′-pentanecyclodeoxyguanosine analog, Entecavir is a chiral compound, in which the [1s-(1α, 3α, 4β)] conformation has extremely strong anti-hepatitis B Virus ability, its raw materials and preparations have been listed abroad at present. The molecular structural formula of Entecavir is as follows: [0003] Molecular formula C 12 h 15 N 5 o 3 . water due to entecavir [0004] The solubility is very small, which is not conducive to the preparation of oral preparations and the improvement of the bioavailability of drugs. Contents of the invention [0005] The object of the present invention is to provide a derivative of entecavir with good water solubility, specifically the potassium salt compound of entecavi...

Claims

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Application Information

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IPC IPC(8): C07D473/18A61K31/522A61P1/16A61P31/12
Inventor 邵长青
Owner 邵长青
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