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Oxiracetam liposome injection

A body injection and injection technology, applied in the field of medicine, can solve the problems of encapsulated drug leakage, easy aggregation, fusion, etc., and achieve the effect of small side effects, good solubility, and fast dissolution

Inactive Publication Date: 2010-06-16
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, liposomes are ubiquitous and easy to aggregate and fuse, resulting in the leakage of encapsulated drugs. Therefore, it is not easy to prepare drug liposomes that meet the stability requirements in industry. Those skilled in the field of pharmacy know clearly that in the preparation of drugs Liposomes face various difficulties, all of which are by no means expected to be solved by simple theory, and many difficulties need to be overcome

Method used

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  • Oxiracetam liposome injection
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  • Oxiracetam liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of Oxiracetam Liposomal Injection

[0052] prescription:

[0053] Oxiracetam 100g

[0054] Soy Lecithin 480g

[0055] Cholesterol 320g

[0056] Tween 80 130g

[0057] Sodium chloride 45g

[0058] Phosphate buffer solution 4000g

[0059] Preparation Process:

[0060] (1) Dissolve 480g soybean lecithin, 320g cholesterol and 130g Tween 80 in a mixed solvent of acetone and methanol in a volume ratio of 5000ml of 4:1, mix well, remove the mixed solvent under reduced pressure on a rotary thin film evaporator, and obtain Phospholipid membrane;

[0061] (2) Add 4000 g of disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution with a pH value of 5.0 to the prepared phospholipid film, shake, stir for 30 min, and rotate at 800 r / min to fully hydrate the phospholipid film, and mash it with tissue Machine high-speed homogeneous emulsification 20min, rotating speed is 15000r / min, 0.45μm microporous membrane filtration, makes blank lipo...

Embodiment 2

[0063] Example 2 Preparation of Oxiracetam Liposomal Injection

[0064] prescription:

[0065] Oxiracetam 100g

[0066] Egg Yolk Lecithin 350g

[0067] Cholesterol 120g

[0068] Tween 80 80g

[0069] Glucose 250g

[0070] Citrate buffer solution 4200g

[0071] Preparation Process:

[0072] (1) Dissolve 350g egg yolk lecithin, 120g cholesterol and 80g Tween 80 in a mixed solvent of acetone and methanol in a volume ratio of 3000ml of 4:1, mix well, remove the mixed solvent under reduced pressure on a rotary thin film evaporator, and obtain Phospholipid membrane;

[0073] (2) Add 4200 g of citric acid-sodium citrate buffer solution with a pH value of 6.0 to the prepared phospholipid film, shake, stir for 60 min, and rotate at 400 r / min to completely hydrate the phospholipid film, and use a tissue masher High-speed homogeneous emulsification for 40 minutes, the rotating speed is 15000r / min, and 0.45 μm microporous membrane filtration to obtain a blank liposome suspensi...

Embodiment 3

[0075] Example 3 Preparation of Oxiracetam Liposomal Injection

[0076] prescription:

[0077] Oxiracetam 100g

[0078] Hydrogenated egg yolk lecithin 700g

[0079] Cholesterol 500g

[0080] Tween 80 300g

[0081] Glycerin 500g

[0082] Citrate buffer solution 4000g

[0083] Preparation Process:

[0084] (1) 700g hydrogenated egg yolk lecithin, 500g cholesterol and 300g Tween 80 are dissolved in the mixed solvent of acetone and methanol of 12000ml volume ratio 4: 1, mix well, remove the mixed solvent under reduced pressure on the rotary thin film evaporator, prepare Get phospholipid membrane;

[0085] (2) Add 4000 g of citric acid-sodium citrate buffer solution with a pH value of 5.5 to the prepared phospholipid film, shake, stir for 40 min, and rotate at 600 r / min to completely hydrate the phospholipid film, and use a tissue masher High-speed homogeneous emulsification for 30 minutes, the rotation speed is 15000r / min, and 0.45 μm microporous membrane filtration to...

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Abstract

The invention discloses an oxiracetam liposome injection which is characterized by comprising the following components in parts by weight: 1 part of oxiracetam, 3-18 parts of phospholipid, 1-12 parts of cholesterol, 0.5-7 parts of tween 80 and an appropriate amount of osmotic-pressure regulating agent and buffering solution. The oxiracetam liposome injection has the advantages of good stability, high entrapment rate, small toxic and side effects and simple preparation, and is suitable for clinical requirements.

Description

technical field [0001] The invention relates to an oxiracetam liposome injection, which belongs to the technical field of medicine. Background technique [0002] Oxiracetam, chemical name: 4-hydroxy-2-oxo-1-pyrrolidineacetamide, molecular formula: C 6 h 10 N 2 o 3 Molecular weight: 158.16, it is an analogue of piracetam, which can improve the memory and learning function of patients with senile dementia and memory impairment. Mechanistic research results suggest that oxiracetam can promote the synthesis of phosphorylcholine and phosphorylethanolamine, increase the ratio of ATP / ADP in the brain, and increase the synthesis of protein and nucleic acid in the brain. [0003] Oxiracetam injection was launched in Italy for the first time in December 1987, and it has been widely used in clinical practice in foreign countries. In my country, the demand for this product has increased significantly as the population aging trend continues to accelerate. Patent literature CN1424034...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/4015A61K47/34A61K47/24A61K47/28A61P25/00A61P25/28A61K47/26
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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