11/2 water citicoline sodium compound and pharmaceutical composition preparation

A technology of citicoline sodium and its compound, which is applied in the field of chemical engineering and pharmaceutical crystallization, can solve the problems of high moisture absorption, poor stability, and backward preparation technology, and achieve the effects of not easy to absorb moisture, stable properties, and wide application prospects

Inactive Publication Date: 2019-01-08
刘兆娟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, compared with similar foreign products, citicoline sodium prepared by the above-mentioned method in China has some quality gaps such as high hygroscopicity, high impurities, and poor stability, and these gaps are mainly due to the backward preparation process.
The existence of these problems leads to poor product quality and instability between batches on the one hand, and also leads to increased production costs and waste of raw materials to a certain extent.

Method used

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  • 11/2 water citicoline sodium compound and pharmaceutical composition preparation
  • 11/2 water citicoline sodium compound and pharmaceutical composition preparation
  • 11/2 water citicoline sodium compound and pharmaceutical composition preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 1 1 / 2 Preparation of Cytocholine Sodium Compound

[0030] Preparation process: Add 200 mL of purified water into the reactor, weigh 100.2 g of crude citicoline sodium into the reactor, and stir until dissolved at room temperature. Add 0.3g of activated carbon to it, stir and adsorb for 30min, filter and decarbonize, adjust the pH to 1.5 with 1mol / L hydrochloric acid, stir well, control the temperature at 15-20°C, slowly add 100mL of ethanol to the above solution, wait until the ethanol is added dropwise After completion, add 0.5g of seed crystals, control the temperature at 5-8°C, let stand for crystallization for 1.5h, and filter; wash the filtrate with 80mL×2 ethanol, and vacuum-dry at 60°C for 2.5h to obtain 1 1 / 2 Hydrocytoline Sodium Compound 99.6g.

[0031] Infrared spectrum at wavenumber 3414.8cm -1 , 3204.3cm -1 , 1654.2cm -1 , 1612.0cm -1 , 1487.3cm -1 , 1380.0cm -1 , 1234.2cm -1 , 1135.3cm -1 , 1072.2cm -1 , 1014.3cm -1 ,833.2cm -1 ...

Embodiment 2

[0036] Example 2 1 1 / 2 Preparation of Cytocholine Sodium Compound

[0037] Preparation process: Add 250 mL of purified water into the reactor, weigh 100.3 g of crude citicoline sodium into the reactor, and stir until dissolved at room temperature. Add 0.3g of activated carbon to it, stir and adsorb for 30min, filter and decarbonize, adjust the pH to 2.0 with 1mol / L hydrochloric acid, stir well, control the temperature at 20-25°C, slowly add 100mL of ethanol to the above solution, wait until the ethanol is added dropwise After completion, add 0.6g of seed crystals, control the temperature at 8-10°C, let stand for crystallization for 1h, and filter; wash the filtrate with 80mL×2 ethanol, and vacuum-dry at 70°C for 2h to obtain 1 1 / 2 Cytophosphacholine Sodium Compound 99.5g.

[0038] The infrared spectrum has a wavenumber of 3414.5cm -1 , 3204.1cm -1 , 1654.3cm -1 , 1612.2cm -1 , 1487.4cm -1 , 1380.3cm -1 , 1234.5cm -1 , 1135.4cm -1 , 1072.4cm -1 , 1014.6cm -1 ,...

Embodiment 3

[0043] Example 3 1 1 / 2 Preparation of hydrocytoline sodium pharmaceutical composition preparation

[0044] Take the citicoline sodium compound prepared in Example 2, and use this raw material to prepare citicoline sodium injection, the specification is 2ml: 0.1g.

[0045] prescription:

[0046]

[0047] Preparation Process:

[0048] 1. Liquid preparation:

[0049] (1) Add 80% water for injection of the total amount in the liquid distribution tank;

[0050] (2) Add 1 of the prescription amount under the stirring state 1 / 2 Cytocholine Sodium, stir to dissolve completely;

[0051] (3) adjust the pH value to 7.0~7.5 with 0.2mol / L sodium hydroxide solution;

[0052] (4) Add water for injection to the full amount;

[0053] (5) Add activated carbon with a total volume of 0.05% (w / v), stir and adsorb for 15 minutes;

[0054] (6) Coarse filtration and decarburization of the solution: filter through a 0.45 μm filter;

[0055] 2. Intermediate detection: detect the pH va...

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Abstract

The invention discloses a 11/2 water citicoline sodium compound and a preparation method of the 11/2 water citicoline sodium compound, wherein each molar of citicoline sodium contains 11/2 molar of water. The citicoline sodium compound is prepared by dissolving a crude product of citicoline sodium into purified water, stirring, dissolving; adding an activated carbon, decarburizing; regulating thepH by using an acid, stirring evenly; slowly adding ethyl alcohol dropwise, adding a seed crystal after finishing adding dropwise, controlling the temperature, leaving to stand, crystalizing, filtering, washing a filtered material with ethyl alcohol, and drying in vacuum. The 11/2 water citicoline sodium compound is low in hygroscopicity and impurity content and good in stability, and has a broader application prospect. Meanwhile, the invention further discloses a pharmaceutical composition preparation of the 11/2 water citicoline sodium compound. The pharmaceutical composition preparation ofthe 11/2 water citicoline sodium compound is better in stability compared with the previous preparation.

Description

technical field [0001] The invention belongs to the technical field of chemical engineering pharmaceutical crystallization and relates to a 1 / 2 Aquacytoline sodium compound and its pharmaceutical composition preparation. Background technique [0002] Citicoline Sodium (Citicoline Sodium) is the abbreviation of cytosine nucleoside diphosphocholine, which 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 molecular weight is 510.31, and the CAS number is 33818-15-4. Clinically, it is mainly used for head trauma and brain surgery accompanied by 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, and treating nerve damage and consciousness caused by acute stroke and surgery. It has obvious clinical therapeutic ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/06A61K31/7068A61P25/00A61P25/28A61P25/16A61P27/06A61P1/18
CPCC07H19/10
Inventor 刘兆娟
Owner 刘兆娟
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