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Citicoline sodium liposome solid preparation

A technology of citicoline sodium and liposome preparation, which is applied in the field of citicoline sodium liposome solid preparation and its preparation method, and achieves the effects of simple preparation process, improved product quality and low cost

Inactive Publication Date: 2011-06-01
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Although the prior art teaches that citicoline can be made into liposomes to promote passage through the blood-brain barrier, its bioavailability still meets the actual clinical needs. How to increase the level of citicoline by selecting appropriate excipients? The bioavailability of choline liposomes remains an urgent need

Method used

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  • Citicoline sodium liposome solid preparation
  • Citicoline sodium liposome solid preparation
  • Citicoline sodium liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 citicoline sodium liposome

[0051] prescription:

[0052] Citicoline Sodium 100g

[0053] Egg Yolk Lecithin 100g

[0054] Dioleoylphosphatidylglycerol 300g

[0055] Sodium deoxycholate 40g

[0056] Octadecylamine 20g

[0057] Preparation Process:

[0058] (1) 100g egg yolk lecithin and 300g dioleoylphosphatidylglycerol and 40g sodium deoxycholate and 20g octadecylamine are dissolved in a mixed solvent of acetone and dichloromethane with a volume ratio of 1:1 in 2000ml, and placed in The organic solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0059] (2) Add 1000 ml of acetic acid-sodium acetate buffer solution having a pH value of 5.3 dissolved with 100 g of citicoline sodium to fully hydrate the phospholipid film, mix the solution evenly, and heat it at 70° C. for 60 minutes of ultrasonic treatment;

[0060] (3) Spray-dry the solution obtained in the above step (2)...

Embodiment 2

[0082] The preparation of embodiment 2 citicoline sodium liposomes

[0083] prescription:

[0084] Citicoline Sodium 100g

[0085] Egg yolk lecithin 250g

[0086] Dioleoylphosphatidylglycerol 750g

[0087] Sodium deoxycholate 200g

[0088] Octadecylamine 100g

[0089] Preparation Process:

[0090] (1) 250g egg yolk lecithin and 750g dioleoylphosphatidylglycerol and 200g sodium deoxycholate and 100g octadecylamine are dissolved in a mixed solvent of acetone and dichloromethane with a volume ratio of 1:1 in 4000ml, placed in The organic solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0091] (2) Add 2000 ml of acetic acid-sodium acetate buffer solution with 100 g of citicoline sodium at a pH value of 5.3 to fully hydrate the phospholipid film, mix the solution evenly, and conduct ultrasonic treatment for 60 minutes at a temperature of 50° C.;

[0092] (3) Spray-dry the solution obtained in the above step (2...

Embodiment 3

[0100] The preparation of embodiment 3 citicoline sodium liposome granules

[0101] Prescription (1000 bags)

[0102] Citicoline Sodium Liposome (calculated as Citicoline Sodium) 100g

[0103] Sucrose 650g

[0104] Mannitol 500g

[0105] Orange flavor 15g

[0106] Povidone K30 10g

[0107] Preparation Process:

[0108] (1) Pulverize the liposome containing 100g citicoline sodium, cross 80 mesh sieves, and set aside;

[0109] (2) Pulverize the sucrose, pass through an 80-mesh sieve, mix, and set aside;

[0110] (3) Mix 650g sucrose, 500g mannitol and 100g citicoline sodium liposome evenly, add 50% ethanol solution 200ml of 5% povidone K30 containing 15g orange essence to make soft material, cross 20 mesh sieves and granulate , dried at 60°C, granulated through a 18-mesh sieve;

[0111] (4) Subpackage the dried granules to obtain citicoline sodium liposome granules.

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Abstract

The invention relates to a citicoline sodium liposome solid preparation which is mainly prepared from citicoline sodium, phospholipid, an additive and other pharmaceutic adjuvants, wherein the citicoline sodium accounts for 1 part by weight, the phospholipids accounts for 2-12 parts by weight, and the additive accounts for 0.5-8 parts by weight. The liposome solid preparation prepared by the invention has the advantages that the stability of the active ingredient citicoline sodium is greatly improved, the valid period of product is prolonged, and phospholipid absorption is cooperated with the curative activity of the citicoline sodium, thus the bioavailability is improved, the product quality of the preparation is improved, and toxic and side effects are reduced.

Description

technical field [0001] The invention relates to a citicoline sodium liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Citicoline sodium is the abbreviation of cytosine nucleoside diphosphocholine. It is the precursor of phospholipid phosphatidylcholine and the necessary coenzyme for the synthesis of lecithin. Its molecular formula is C 14 h 25 N 4 NaO 11 P 2 , the structural formula is: [0003] [0004] Citicoline is an amorphous, hygroscopic powder that has therapeutic uses, eg as a brain-protective or neuroprotective agent. Citicoline sodium is mainly used clinically for head trauma and brain surgery with disturbance of consciousness, acute disturbance of consciousness after cerebral infarction, promoting the recovery of upper limb function in stroke patients with hemiplegia, and acute pancreatitis. In particular, citicoline is beneficial for patients with ischemic stroke, brai...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/00A61K9/16A61K9/20A61K9/48A61K31/7068A61P25/00A61P25/02A61P25/28A61P1/18
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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