Preparation method of Citicoline Sodium

Citicoline sodium (also known as sodium cytidine 5′-diphosphocholine or CDP-choline) is a nootropic compound commonly used in the treatment of cognitive disorders, stroke rehabilitation, and to support brain health. The preparation of citicoline sodium generally involves a chemical synthesis process that requires careful handling of reagents and solvents in a controlled environment.

Here’s an overview of a typical synthesis route for citicoline sodium:

1. Preparation of Cytidine and CMP (Cytidine Monophosphate):

  • Step 1: Start with cytidine, a nucleoside composed of cytosine and ribose sugar.
  • Step 2: Cytidine is reacted with phosphorylating agents (such as phosphoric acid or similar reagents) to create Cytidine Monophosphate (CMP).
Preparation method of Citicoline Sodium-Xi'an Lyphar Biotech Co., Ltd

2. Reaction with Choline:

  • Step 3: The CMP is then reacted with a source of choline (such as choline chloride) to form Cytidine 5′-Diphosphocholine (CDP-choline).

This step typically uses phosphoric acid or a phosphorylation catalyst to create the diphosphate bond between cytidine and choline.

3. Formation of Citicoline Sodium:

  • Step 4: After the formation of CDP-choline, the compound is treated with sodium hydroxide (NaOH) or sodium carbonate (Na2CO3) to form the sodium salt of CDP-choline, also known as Citicoline Sodium.

4. Purification:

  • Step 5: The resulting citicoline sodium may be purified by techniques like precipitation, filtration, or chromatography to ensure the removal of any residual reagents or by-products.

5. Drying and Final Processing:

  • Step 6: The purified citicoline sodium is then dried, typically using a vacuum dryer or a similar controlled method to remove any remaining solvents. It is often processed into a powder form for use in pharmaceutical preparations.

Quality Control:

  • Throughout the process, quality control tests, including spectroscopy (UV-Vis, NMR) and HPLC (High-Performance Liquid Chromatography), are often used to ensure the purity and correct molecular structure of the product.
Preparation method of Citicoline Sodium-Xi'an Lyphar Biotech Co., Ltd

The synthesis of citicoline sodium is generally done on an industrial scale and requires precise control of reaction conditions, including temperature, pH, and reagent concentrations.

For commercial pharmaceutical formulations, citicoline sodium is commonly found in tablets, capsules, or injectable solutions.

Note: This process is a simplified version of the synthesis and may vary depending on specific protocols used in different laboratories or industrial settings.