Edaravone liposome injection and new application thereof

A technology of edaravone lipid and injection, applied in liposome injection of edaravone and its preparation, a new application field for the treatment of thrombophlebitis, which can solve the problem that it is difficult to achieve the therapeutic effect and the quality cannot be guaranteed to be stable and stable Sex can not meet the clinical requirements and other problems, to achieve the effect of promoting stability, improving stability and reducing leakage

Inactive Publication Date: 2009-12-16
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Edaravone in solid state is relatively stable, but its aqueous solution is prone to oxidation-reduction reaction and degradation
At present, the edaravone preparation widely used clinically is water injection, by adding L-cysteine ​​and sodium bisulfite as antioxidants in the formula, filling nitrogen gas in the preparation process to improve its stability, However, after long-term storage, the quality cannot be guaranteed to be stable, and degradation will still occur
Patent documents CN1241565C, CN100358520C and CN101288650A respectively describe the preparation method of edaravone freeze-dried powder injection, which mainly improves the solubility. Although some stabilizers are added, the stability after long-term placement still cannot meet the clinical requirements. requirements, it is difficult to achieve its expected therapeutic effect

Method used

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  • Edaravone liposome injection and new application thereof
  • Edaravone liposome injection and new application thereof
  • Edaravone liposome injection and new application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1 Preparation of Edaravone Liposomes

[0069] Prescription (1000 sticks):

[0070] Edaravone 10g

[0071] Dilauroyl Phosphatidylcholine 200g

[0072] Cholesterol 5g

[0073] Polysorbate 80 10g

[0074] Sodium chloride 13.5g

[0075] Acetic acid-sodium acetate buffer solution with a pH value of 5.0 500ml

[0076] Preparation Process

[0077] (1) Dissolve 200g of dilauroylphosphatidylcholine, 5g of cholesterol and 10g of polysorbate 80 in 1000ml of isopropanol, slowly inject 1000ml of 0.01mol / L ammonium sulfate solution under stirring, heat and stir to evaporate the isopropanol, Place in an ice bath and sonicate for 10 minutes to obtain blank liposomes;

[0078] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in 0.9% sodium chloride aqueous solution 1000ml and dialyzes 20 hours, removes the ammonium sulfate in liposome external phase;

[0079] (3) Dissolve 10g of Edaravone in 500ml of water, keep the dialyzed blank liposo...

Embodiment 2

[0088] Example 2 Preparation of Edaravone Liposomes

[0089] Prescription (1000 sticks):

[0090] Edaravone 15g

[0091] Hydrogenated Soy Lecithin 75g

[0092] Cholesterol 45g

[0093] Polysorbate 80 150g

[0094] Mannitol 225g

[0095] Boric acid-borax buffer solution with a pH value of 5.5 800ml

[0096] Preparation Process

[0097] (1) Dissolve 75g of hydrogenated soybean lecithin, 45g of cholesterol and 150g of polysorbate 80 in 1500ml of tert-butanol, slowly inject 1500ml of 0.1mol / L ammonium sulfate solution under stirring, heat and stir to remove tert-butanol, and place in an ice bath Ultrasound for 20 minutes to obtain blank liposomes;

[0098] (2) Place the blank liposome in the dialysis bag, seal it, place the dialysis bag in 1500ml of 10% mannitol aqueous solution and dialyze for 22 hours, remove the ammonium sulfate in the liposome external phase;

[0099] (3) 15g of Edaravone was dissolved in 800ml of water, and the dialyzed blank liposome was incubate...

Embodiment 3

[0112] Example 3 Preparation of Edaravone Liposomes

[0113] Prescription (1000 sticks):

[0114] Edaravone 30g

[0115] Egg Yolk Phosphatidylserine 300g

[0116] Cholesterol 150g

[0117] Polysorbate 80 120g

[0118] Glucose 240g

[0119] Phosphoric acid-disodium hydrogen phosphate buffer solution with a pH value of 6.0 1000ml

[0120] Preparation Process

[0121] (1) Dissolve 300g of egg yolk phosphatidylserine, 150g of cholesterol and 120g of polysorbate 80 in 2000ml of benzyl alcohol, slowly inject 2000ml of 0.15mol / L ammonium sulfate solution under stirring, heat and stir to remove benzyl alcohol, put it in an ice bath and sonicate 10min, get blank liposome;

[0122] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in 5% glucose aqueous solution 3200ml and dialyzes 20 hours, removes the ammonium sulfate in liposome external phase;

[0123] (3) Dissolve 30g of Edaravone in 1000ml of water, keep the dialyzed blank liposomes at 60°C...

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Abstract

The invention discloses an edaravone liposome preparation form. The edaravone liposome injection is prepared from excipients, such as edaravone, phospholipid, cholesterol, polysorbate 80, and the like. The invention further discloses new application of the edaravone liposome injection in treating thrombus type phlebitis.

Description

technical field [0001] The present invention relates to a new dosage form and application of edaravone, in particular to a liposome injection of edaravone and a preparation method thereof, and further relates to its new application in treating thrombophlebitis. Background technique [0002] Thrombophlebitis, also known as venous thrombosis, refers to inflammation of the venous lumen caused by various reasons or accompanied by venous thrombosis, including superficial thrombophlebitis and deep thrombophlebitis. Clinically, it is characterized by pain, swelling of limbs, anterior varicose veins, and palpable cord-like tumors under the skin, and most of them are in the lower limbs. It is a critical and difficult disease clinically. Bring long-term pain to patients, affect life and work ability, even disability. Commonly used non-surgical treatments include thrombolysis, anticoagulation and other treatments, which are easy to cause bleeding, and blood coagulation function needs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4152A61K47/34A61P9/14A61P7/02A61K47/26
Inventor 王明
Owner HAINAN MEILAN SMITH KLINE PHARMA
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