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Flumazenil oil-in-water emulsion for vein and preparation thereof

A technology of oil-in-water emulsion and flumazenil, which is applied in the field of medicine, can solve problems such as poor stability, achieve the effects of improving stability, prolonging the action time, and reducing irritation to blood vessels

Inactive Publication Date: 2010-07-21
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the problem of poor stability of flumazenil injection, the purpose of the present invention is to provide a kind of oil-in-water emulsion of flumazenil to improve its stability

Method used

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  • Flumazenil oil-in-water emulsion for vein and preparation thereof
  • Flumazenil oil-in-water emulsion for vein and preparation thereof
  • Flumazenil oil-in-water emulsion for vein and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of embodiment 1 flumazenil oil-in-water emulsion

[0038] Flumazenil 0.1g

[0039] Corn oil 0.5g

[0040] Soy Lecithin 0.1g

[0041] Palmitic acid 0.5g

[0042] Ditert-butylhydroxytoluene 0.1g

[0043] Glucose 2g

[0044] Absolute ethanol 0.5g

[0045] Water for injection 1000ml

[0046] Preparation Process

[0047] (1) Dissolve 0.1 g of flumazenil in 0.5 g of absolute ethanol, dissolve, add 0.5 g of corn oil, 0.1 g of di-tert-butyl hydroxytoluene and 0.5 g of palmitic acid and mix to obtain an oil phase;

[0048] (2) disperse soybean lecithin 0.1g and glucose 2g in water for injection to obtain an aqueous phase;

[0049] (3) In the case of stirring the water phase at a high speed, pour the oil phase evenly into the water phase to form a colostrum, then transfer it to a high-speed homogenizer to stir and homogenize, and adjust the pH value to 3.9 with phosphoric acid and disodium hydrogen phosphate solution;

[0050] (4) Add 1 g of activated car...

example 2

[0051] The preparation of example 2 flumazenil oil-in-water emulsion

[0052] Flumazenil 0.5g

[0053] Peanut oil 10g

[0054] Hydrogenated Soy Lecithin 5g

[0055] Palmitic acid 5g

[0056] Ditert-butylhydroxytoluene 0.5g

[0057] Mannitol 5g

[0058] Absolute ethanol 2.5g

[0059] Water for injection 5000ml

[0060] The preparation method is the same as Example 1, and the pH value is adjusted to 4.0 with phosphoric acid and disodium hydrogen phosphate solution, and the filling is 5ml / support.

Embodiment 3

[0061] The preparation of embodiment 3 flumazenil oil-in-water emulsion

[0062] Flumazenil 1.0g

[0063] Sesame oil 20g

[0064] Polysorbate 80 10g

[0065] Palmitic acid 10g

[0066] Ditert-butylhydroxytoluene 1.0g

[0067]Sorbitol 10g

[0068] Absolute ethanol 50g

[0069] Water for injection 10000ml

[0070] The preparation method is the same as that of Example 1, and the pH value is adjusted to 3.8 with phosphoric acid and disodium hydrogen phosphate solution, and the filling is 10ml / support.

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Abstract

The invention discloses a Flumazenil oil-in-water emulsion for intravenous injection; the oil-in-water emulsion contains the following ingredients by proportion: 0.1-1 part of Flumazenil, 0.5-20 parts of oil for injection, 0.1-10 parts of emulsifier, 0-10 parts of palmitic acid, 0.1-1 part of di-tert-butyl hydroxy toluene, 0-10 parts of osmotic pressure regulator and 0.5-5 part of absolute ethyl alcohol and 1,000-10,000ml of water for injection. The invention also discloses a preparation method for the emulsion. The emulsion has good stability, long acting time and low toxic and side effect.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an oil-in-water emulsion of flumazenil for intravenous use. Background technique [0002] Flumazenil, chemical name 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-[1,5-a][1,4]benzodiazepine -Ethyl 3-carboxylate, a benzodiazepine receptor antagonist, which specifically blocks its central nervous system effects by competitively inhibiting the reaction between benzodiazepines and their receptors. [0003] According to the literature, flumazenil is a lipophilic drug, the plasma protein binding rate is about 50%, and 2 / 3 of the bound plasma protein is albumin. Flumazenil is widely distributed extravascularly, with a mean volume of distribution (Vss) at steady state of 0.95 L / kg. Flumazenil is mainly metabolized in the liver. The major metabolite in plasma and urine is the carboxylic acid metabolite, which has no benzodiazepine receptor agonist or antagonist activity. Flumazenil is almost c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5517A61P25/20
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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