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Flumazenil liposome injection

A technology of flumazenil and mazenil, which is applied in the directions of liposome delivery, organic active ingredients, nervous system diseases, etc., can solve the problems of poor automatic dispersion uniformity, increase the manufacturing cost, and affect the use effect, etc. The effect of improving quality, improving solubility, and improving efficacy

Inactive Publication Date: 2011-11-23
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation of the emulsion needs to add a large amount of organic co-surfactant, which increases the manufacturing cost; and the automatic dispersion uniformity is poor after dilution during use, which affects the use effect

Method used

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  • Flumazenil liposome injection
  • Flumazenil liposome injection
  • Flumazenil liposome injection

Examples

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preparation example Construction

[0075] On the other hand, the present invention also provides a preparation method of flumazenil liposome injection, specifically comprising the following preparation steps:

[0076] (1) Cholesterol, phosphatidylethanolamine, soybean sterol, and Tween 80 are dissolved in an appropriate amount of buffered saline solution to make blank liposomes;

[0077] (2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0078] (3) under sterile conditions, add flumazenil to the liposome in molten state, add trehalose and PVP under constant stirring;

[0079] (4) Filtrate with a 0.45um microporous membrane, freeze quickly, then return to room temperature, and fill to obtain the flumazenil liposome injection.

[0080] The above-mentioned preparation method, wherein said buffered saline solution is selected from one of phosphate buffered saline, citrate buffered solution, carbonate buffered solution, bor...

Embodiment 1

[0088] The preparation of embodiment 1 flumazenil liposome injection

[0089] The ingredients used and their weights are as follows:

[0090]

[0091] Adopt preparation process to prepare flumazenil liposome injection:

[0092] (1) 120g cholesterol, 150g phosphatidylethanolamine, 30g soy sterol and 10g Tween 80 are dissolved in 3000mlpH in the phosphate buffered saline solution that is 7.2, make blank liposome;

[0093] (2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0094] (3) Under sterile conditions, add 1 g of flumazenil to the liposome in a molten state at 60° C., and add 100 g of trehalose and 150 g of PVP under constant stirring;

[0095] (4) Filtrate with a 0.45um microporous membrane, freeze quickly at -80°C, then return to room temperature, and fill to obtain the flumazenil liposome injection.

Embodiment 2

[0096] The preparation of embodiment 2 flumazenil liposome injection

[0097] The ingredients used and their weights are as follows:

[0098]

[0099]

[0100] Adopt preparation process to prepare flumazenil liposome injection:

[0101] (1) 75g cholesterol, 100g phosphatidylethanolamine, 25g soybean sterol and 20g Tween 80 are dissolved in the phosphate-buffered saline solution of 7.2 in the pH of 3000ml, make blank liposome;

[0102](2) The blank liposomes prepared above were sterilized by circulating steam, and then ultrasonically treated twice, each time for 15 minutes;

[0103] (3) Under sterile conditions, add 0.5 g of flumazenil to the liposome in a molten state at 60° C., and add 30 g of trehalose and 40 g of PVP under constant stirring;

[0104] (4) Filtrate with a 0.45um microporous membrane, freeze quickly at -80°C, then return to room temperature, and fill to obtain the flumazenil liposome injection.

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Abstract

The invention discloses a flumazenil liposome injection and a preparation method thereof. The liposome injection is prepared from flumazenil, cholesterol, phosphatidyl ethanolamine, soyasterol, tween 80, trehalose and polyvinylpyrrolidone in specific proportions by weight. The liposome injection disclosed by the invention has favorable preparation stability, the liposome can not be ruptured due to fusion, ice crystal and the like in the freezing process, and the liposome keeps the same favorable entrapment rate after long-term storage. The flumazenil liposome injection disclosed by the invention improves the solubility of flumazenil, improves the quality of the preparation product, reduces the toxic side effect, increases the retention time of the medicament in systemic circulation, improves the bioavailability of the medicament, obviously improves the curative effect, has a simple preparation method and is suitable for industrialized big production.

Description

technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a flumazenil liposome injection and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] The chemical name of flumazenil is 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-[1,5-a][1,4]benzodiazepine -Ethyl 3-formate, molecular formula C 15 h 14 FN 3 o 3 , the molecular weight is 303.29, and the structural formula is as follows: [0003] [0004] Flumazenil is a white or off-white crystalline powder, almost insoluble in water. [0005] Flumazenil is a 1,4-imidazole benzodiazepine derivative, a benzodiazepine (BZD) receptor antagonist, which can act on the brain BDZ receptor, reverse the central sedative effect of BDZ, and block the BDZ receptor. body without producing the effects of BDZ drugs. Flumazenil can reverse the effects of BDZ and non-BDZ drugs (such as Upiclone and triazolopyridazines) ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/5517A61P25/00
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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