Adefovir dipivoxil liposome injection and its preparing method

A technology of ester lipid and liposome is applied in the field of liposome injection preparation containing adefovir dipivoxil and its preparation, and can solve the problems of instability of adefovir dipivoxil, nephrotoxicity, low bioavailability and the like , to overcome the low bioavailability, reduce toxic and side effects, and improve the efficacy of

Inactive Publication Date: 2010-06-16
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] One of the purposes of the present invention is to provide a kind of adefovir dipivoxil liposome injection preparation for the instability of adefovir dipivoxil, low bioavailability and nephrotoxicity, including adefovir dipivoxil liposome Injection and adefovir dipivoxil liposome powder injection;

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Embodiment 1: the preparation of adefovir dipivoxil liposome injection

[0069] Weigh 3g of adefovir dipivoxil, 20g of soybean lecithin and 7g of cholesterol and put them in a round bottom flask, add an appropriate amount of ethanol to the above mixture to completely dissolve into a clear solution, put it in a constant temperature water bath (75°C) and dry it under reduced pressure to form a film, add Dissolve the film in 1000ml of water for injection, homogenize it with an ultrasonic instrument or a high-pressure homogenizer pump, filter it with a microporous membrane, and pack it in ampoules (or vials), so that each bottle contains 6 mg of adefovir dipivoxil. Sterilize to obtain the liposome for adefovir dipivoxil injection.

Embodiment 2

[0070] Embodiment 2: the preparation of adefovir dipivoxil liposome injection

[0071] Weigh 1g of adefovir dipivoxil, 30g of egg yolk lecithin and 30g of cholesterol and put them in a round bottom flask, add an appropriate amount of chloroform to the above mixture to completely dissolve into a clear solution, put it in a constant temperature water bath (75°C) and dry it under reduced pressure to form a film, add Dissolve the film in 1000ml of water for injection, homogenize it with an ultrasonic instrument or a high-pressure homogenizer pump, filter it with a microporous membrane, and pack it in ampoules (or vials), so that each bottle contains 2 mg of adefovir dipivoxil, Sterilize to obtain the liposome for adefovir dipivoxil injection.

example 3

[0072] Example 3: Preparation of Adefovir dipivoxil liposome injection

[0073] Weigh 3g of adefovir dipivoxil, 30g of egg yolk lecithin, 30g of cholesterol and F 68 Put 27g in a round-bottomed flask, add an appropriate amount of chloroform to the above mixture to completely dissolve into a clear solution, place in a constant temperature water bath (75°C) and dry under reduced pressure to form a film, add 1000ml of water for injection to dissolve the film, and use an ultrasonic machine to ultrasonically pulverize or high-pressure homogenate Homogenize with a pump, then filter with a microporous membrane, pack in ampoules (or vials) so that each bottle contains 2 mg of adefovir dipivoxil, and sterilize to obtain liposomes for injection of adefovir dipivoxil.

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Abstract

The present invention relates to adefovir dipivoxil liposome injection and its preparation process. The adefovir dipivoxil liposome injection contains adefovir dipivoxil in 0.01-1 wt%, lipoid for preparing liposome in 0.05-15 wt% and / or pharmaceutically acceptable carrier.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, especially a liposome injection preparation containing adefovir dipivoxil and a preparation method thereof. Background technique [0002] Adefovir Dipivoxil is the prodrug of adenine phosphate compound Adefovir, which is converted into Adefovir by hydrolysis in vivo. Adefovir is a nucleotide of adenosine monophosphate that competes with the natural substrate deoxyadenosine triphosphate for the DNA polymerase of hepatitis B virus. After entering the viral DNA chain, it causes the suspension of its DNA chain synthesis, thereby hindering the replication of the virus. Broad-spectrum antiviral activity. Adefovir can treat hepatitis B virus resistant to lamivudine, and combined therapy with lamivudine can effectively control the resistance to lamivudine. [0003] Adefovir dipivoxil is a solid substance with various crystal forms and amorphous forms that is insoluble in water, and it often degrades with...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K9/127A61K9/14A61P31/14A61P1/16
Inventor 陈建明叶正良张广明王国成赵颖
Owner TIANJIN TASLY PHARMA CO LTD
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