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Nifuratel liposome solid preparation

A technology of nifuratel fat and solid preparations, which is applied in the direction of liposome delivery, antifungal agents, medical preparations of non-active ingredients, etc., to achieve the effects of improving quality, long distribution time, and reducing toxic and side effects

Inactive Publication Date: 2012-01-11
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, the preparation of liposomes requires selection of appropriate liposome components and preparation methods, which requires a large number of experimental screenings and has certain difficulties

Method used

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  • Nifuratel liposome solid preparation
  • Nifuratel liposome solid preparation
  • Nifuratel liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The preparation of embodiment 1 nifuratel liposome capsule

[0045] Prescription (1000 capsules):

[0046]

[0047] Preparation Process:

[0048] (1) Dissolve 100g of nifuratel, 150g of sphingomyelin, 150g of egg phosphatidylcholine, 75g of cholesterol, 125g of Tween 40 and 15g of vitamin E in 1600ml of dichloromethane, place in a pear-shaped flask and evaporate under reduced pressure Remove methylene chloride, add 1500ml ether to dissolve after forming a uniform film on the wall of the flask;

[0049] (2) Add 500ml of buffer solution to the above solution to form a two-phase system, and sonicate in a water bath until a stable emulsion is formed;

[0050] (3) The above-mentioned emulsion is decompressed and rotary evaporated to form a colloidal state, and an appropriate amount of buffer solution is added, and the rotary evaporation is continued to remove ether;

[0051] (4) process 3 minutes with high-shear dispersing emulsifier, under nitrogen environment constan...

Embodiment 2

[0055] The preparation of embodiment 2 nifuratel liposome capsules

[0056] Prescription (1000 capsules):

[0057]

[0058]

[0059] Preparation Process:

[0060] (1) Dissolve 100g of nifuratel, 300g of sphingomyelin, 300g of egg phosphatidylcholine, 100g of cholesterol, 200g of Tween 40 and 20g of vitamin E in 4000ml of dichloromethane, place in a pear-shaped bottle and evaporate under reduced pressure Remove dichloromethane, add 3000ml ether to dissolve after forming a uniform film on the wall of the flask;

[0061] (2) Add 800ml of buffer solution to the above solution to form a two-phase system, and sonicate in a water bath to form a stable emulsion;

[0062] (3) The above-mentioned emulsion is decompressed and rotary evaporated to form a colloidal state, and an appropriate amount of buffer solution is added, and the rotary evaporation is continued to remove ether;

[0063] (4) process 3 minutes with high-shear dispersing emulsifier, under nitrogen environment con...

Embodiment 3

[0067] The preparation of embodiment 3 nifuratel liposome sheet

[0068] Prescription (1000 tablets):

[0069]

[0070] Preparation Process:

[0071] (1) Dissolve 200g of nifuratel, 200g of sphingomyelin, 200g of egg phosphatidylcholine, 100g of cholesterol, 100g of Tween 40 and 20g of vitamin E in 3000ml of dichloromethane, place in a pear-shaped bottle and evaporate under reduced pressure Remove methylene chloride, add 2500ml ether to dissolve after forming a uniform film on the wall of the flask;

[0072] (2) Add 1000ml of buffer solution to the above solution to form a two-phase system, and sonicate in a water bath until a stable emulsion is formed;

[0073] (3) The above-mentioned emulsion is decompressed and rotary evaporated to form a colloidal state, and an appropriate amount of buffer solution is added, and the rotary evaporation is continued to remove ether;

[0074] (4) process 3 minutes with high-shear dispersing emulsifier, under nitrogen environment constan...

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Abstract

The invention discloses a nifuratel liposome solid preparation and its preparation method, which is characterized in that the solid preparation comprises the following components by weight: 100 parts of nifuratel, 100-300 parts of sphingomyelin, 100-300 parts of egg phosphatidylcholine, 50-100 parts of cholesterol, 50-200 parts of tween 40, 10-20 parts of vitamin E and 75-150 parts of other pharmaceutical common auxiliary materials. The invention employs an anti-phase evaporation method for preparing nifuratel liposome solid which substantially raises the biological availability and stability of nifuratel, raises the product quality of the preparation, minimizes the toxicity and side effect, enhances the curative effect and greatly serves for the clinical application.

Description

technical field [0001] The invention relates to a pharmaceutical liposome solid preparation, in particular to a nifuratel liposome solid preparation and a preparation method thereof, and belongs to the field of pharmaceutical preparations. Background technique [0002] Nifuratel (Nifuratel), chemical name: 5-[(methylthio)methyl]-3-[(5-nitrofuryl methylene)amino]-2-oxazolidinone, molecular formula C 10 h 11 N 3 o 5 S, molecular weight 285.28, structural formula: [0003] [0004] Nifuratel is a nitrofuran derivative and is a broad-spectrum antibiotic, especially for common pathogens of gynecological infections such as Gram-positive and negative bacteria, trichomonas, mold, chlamydia and mycoplasma. It is clinically used to treat vulva, vaginal infection, leucorrhea increase and urinary system infection, digestive tract amoebiasis and giardiasis caused by bacteria, trichomonas, mold and candida. [0005] Patent document CN101199474A discloses a kind of nifuratel gel an...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/422A61K47/28A61K47/24A61K47/26A61K47/22A61P31/04A61P31/10A61P33/02
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA