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Ornidazole liposome injection

A technology of ornidazole lipid and injection is applied in the field of pharmaceutical preparations to achieve the effects of protecting form and stability and improving stability

Inactive Publication Date: 2013-05-29
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the challenge in preparing liposomes lies in selecting the appropriate liposome composition and formulation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1 Preparation of Ornidazole Liposomal Injection

[0058] Prescription: (1000 bottles)

[0059]

[0060] Preparation Process:

[0061] (1) Dilauroylphosphatidylglycerol 1500g, soybean sterol 1000g, trehalose 500g and 500g Tween 60 are dissolved in 70% ethanol aqueous solution of 2500ml, mix well, remove the organic solvent under reduced pressure on the rotary thin film evaporator, obtain Lipid membrane;

[0062] (2) Add an appropriate amount of buffer solution to the bottle, shake for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid membrane, and emulsify with a high-speed tissue grinder for 10-15 minutes at a speed of 8000r / min. Filter with a 0.45 μm microporous membrane to obtain a liposome suspension;

[0063] (3) Under sterile conditions, add 500 g of ornidazole to the liposome suspension and shake evenly; then perform gradient homogenization at 100 bar to 800 bar for 5 to 6 times;

[0064] (4) Quickly freeze, then return ...

Embodiment 2

[0065] Example 2 Preparation of Ornidazole Liposomal Injection

[0066] Prescription: (1000 bottles)

[0067]

[0068] Preparation Process:

[0069] (1) Dilauroylphosphatidylglycerol 1000g, soybean sterol 500g, trehalose 500g and 500g Tween 60 are dissolved in 70% ethanol aqueous solution of 2000ml, mix well, remove the organic solvent under reduced pressure on a rotary thin film evaporator, obtain Lipid membrane;

[0070] (2) Add buffer solution to the bottle, shake for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid film, use a tissue masher for high-speed homogeneous emulsification for 10-15 minutes at a speed of 8000r / min, and use 0.45 μm microporous membrane filtration, obtained liposome suspension;

[0071] (3) Under sterile conditions, add 500 g of ornidazole to the liposome suspension and shake evenly; then perform gradient homogenization at 100 bar to 800 bar for 5 to 6 times;

[0072] (4) Quickly freeze, then return to room tem...

Embodiment 3

[0073] Example 3 Preparation of Ornidazole Liposomal Injection

[0074] Prescription: (1000 bottles)

[0075]

[0076] Preparation Process:

[0077] (1) Dilauroylphosphatidylglycerol 750g, soybean sterol 500g, trehalose 250g and 250g Tween 60 are dissolved in 70% ethanol aqueous solution of 1500ml, mix well, remove the organic solvent under reduced pressure on the rotary thin film evaporator, obtain Lipid membrane;

[0078] (2) Add buffer solution to the bottle, shake for 30 minutes at a speed of 400-700r / min to completely hydrate the phospholipid film, use a tissue masher for high-speed homogeneous emulsification for 10-15 minutes at a speed of 8000r / min, and use 0.45 μm microporous membrane filtration, obtained liposome suspension;

[0079] (3) Under sterile conditions, add 250 g of ornidazole to the liposome suspension and shake evenly; then perform gradient homogenization at 100 bar to 800 bar for 5 to 6 times;

[0080] (4) Quickly freeze, then return to room temp...

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Abstract

The invention discloses an ornidazole liposome injection and a preparation method thereof. The liposome injection is prepared from ornidazole, dilauroyl phosphatidylglycerol, soybean sterol, tween 60 and mycose with a specific weight ratio. The liposome injection of the invention has good stability of preparation and can maintain good encapsulation efficiency even after long term storage. Preparation product quality is improved in the invention; retention time is lengthened in a systemic circulation; bioavailability of drugs is improved; toxic and side effects are reduced; The method of preparation is simple and the ornidazole liposome injection and the preparation method thereof are applicable to industrial production.

Description

technical field [0001] The invention relates to a novel injection of ornidazole and a preparation method thereof, in particular to an ornidazole liposome injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Ornidazole is white or slightly yellow crystalline powder, odorless, bitter in taste, gradually turns yellow when exposed to light, relative molecular mass: 219.63, molecular formula: C 7 h 10 ClN 3 o 3 , its chemical name is 1-(3-chloro-2-hydroxypropyl)-2-methyl-5-nitroimidazole; the chemical structure is as follows: [0003] [0004] Ornidazole is a nitroimidazole derivative, which is a powerful drug against anaerobic bacteria and antiprotozoal infection. It is the third-generation nitroimidazole with higher curative effect, shorter course of treatment, better tolerance and wider distribution in the body. derivative. The antimicrobial effect of ornidazole is through the reducti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/4164A61K47/34A61P31/04A61P33/02
Inventor 陶灵刚曹丽梅
Owner HAINAN YONGTIAN PHARMA INST
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