Maleic acid cinepazide liposome injection and new application thereof

A technology of cinepazide maleate and cinepazide lipid, which is applied in the field of liposome preparations to achieve the effects of reducing drug toxicity, leakage, and drug side effects

Inactive Publication Date: 2011-02-16
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a kind of stable cinepazide maleate injection, promptly adopt the combination of certain content excipient and active ingredient, make the cinepazide maleate lipid of the present invention by pH value gradient method Body injection, thus, well solved the problem that cinepazide maleate injection exists in the prior art

Method used

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  • Maleic acid cinepazide liposome injection and new application thereof
  • Maleic acid cinepazide liposome injection and new application thereof
  • Maleic acid cinepazide liposome injection and new application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of cinepazide maleate liposomes

[0042] Prescription (1000 sticks):

[0043]

[0044] Preparation Process

[0045] (1) Dissolve 320g of soybean lecithin, 48g of cholesterol and 240g of polysorbate 80 in 2000ml of n-butanol, slowly inject 2000ml of 0.03mol / L ammonium sulfate solution under stirring, heat and stir to remove n-butanol, put it in an ice bath and ultrasonically 20min, get blank liposome;

[0046] (2) Blank liposome is placed in dialysis bag, seals, and dialysis bag is placed in 0.9% sodium chloride aqueous solution 1500ml and dialyzes 22 hours, removes the ammonium sulfate in liposome external phase;

[0047] (3) Dissolve 40g of cinepazide maleate in 800ml of water, heat the dialyzed blank liposome at 60°C, slowly add the aqueous solution of cinepazide maleate under stirring, continue to keep warm for 20min, add 0.9 500ml of aqueous sodium chloride solution and 500ml of acetic acid-sodium acetate buffer solution with a pH valu...

Embodiment 2

[0051] Example 2 Preparation of cinepazide maleate liposomes

[0052] Prescription (1000 sticks):

[0053]

[0054] Preparation Process

[0055] (1) Dissolve 480g of hydrogenated soybean lecithin, 400g of cholesterol and 320g of polysorbate 80 in 3000ml of benzyl alcohol, slowly inject 3000ml of 0.1mol / L ammonium sulfate solution under stirring, heat and stir to remove benzyl alcohol, put it in an ice bath and ultrasonically for 20min , to obtain blank liposomes;

[0056] (2) Place the blank liposome in the dialysis bag, seal it, place the dialysis bag in 1500ml of 10% glycerol aqueous solution and dialyze for 22 hours, remove the ammonium sulfate in the liposome external phase;

[0057] (3) Dissolve 80g of cinepazide maleate in 1000ml of water, heat the dialyzed blank liposome at 60°C, slowly add the aqueous solution of cinepazide maleate under stirring, continue to keep warm for 30min, add 10 500ml of aqueous solution of % glycerol and 500ml of potassium dihydrogen...

Embodiment 3

[0065] Example 3 Preparation of cinepazide maleate liposomes

[0066] Prescription (1000 sticks):

[0067]

[0068] Preparation Process

[0069] (1) Dissolve 1600g dioleoylphosphatidylcholine, 640g cholesterol and 960g polysorbate 80 in 6000ml isopropanol, slowly inject 6000ml of 0.5mol / L ammonium sulfate solution under stirring, heat and stir to evaporate isopropanol, Place in an ice bath and sonicate for 10 minutes to obtain blank liposomes;

[0070] (2) Blank liposome is placed in the dialysis bag, seals, and the dialysis bag is placed in 5% glucose aqueous solution 2250ml and dialyzes for 22 hours, removes the ammonium sulfate in the liposome external phase;

[0071] (3) Dissolve 320g of cinepazide maleate in 1500ml of water, heat the dialyzed blank liposome at 60°C, slowly add the aqueous solution of cinepazide maleate under stirring, continue to keep warm for 20min, add 5 750ml of aqueous glucose solution and 500ml of citric acid-sodium citrate buffer solution ...

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Abstract

The invention relates to maleic acid cinepazide liposome injection and new application thereof. The invention discloses the maleic acid cinepazide liposome injection and a preparation method thereof. The maleic acid cinepazide liposome injection mainly comprises the following components according to parts by weight: 1 part of maleic acid cinepazide, 1 to 13 parts of phospholipid, 0.6 to 6 parts of cholesterol and 2 to 10 parts of polysorbate 80. The preparation has favorable curative effect in treating blood vessel type migraine.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a cinepazide maleate liposome injection and a preparation method thereof, and a new application of the preparation in treating vascular migraine. Background technique [0002] Vascular migraine (abbreviated as migraine) is one of the common acute headaches, which is caused by paroxysmal vasomotor dysfunction and temporary changes in certain body fluid substances. The etiology is still unknown, and there is often a family history, and it is more common in women. Its clinical manifestations are: short-term impairment of brain function such as visual hallucinations and hemianopia before the onset, followed by unilateral headache, which is throbbing throbbing pain, tingling pain or dull pain. When it is severe, it is accompanied by dizziness, sweating, nausea and vomiting, palpitations, constipation and other symptoms, which last for about several hours. Generally, the recurrence interval ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/496A61K47/34A61P25/06A61K47/26
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST
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