Project's information

Project's title Investigation of production process of Celecoxib - an anti-arthritis and analgesic API
Research hosting institution Institute of Chemistry
Project leader’s name Dr. Ngo Quoc Anh
Project duration 01/01/2011 - 01/01/2012
Project’s budget 400.000.000 VND
Classify Fair
Goal and objectives of the project
  • Develop a celecoxib synthesis process  achieving pharmaceutical standards with production scale of 20g / batch.
  • Test the quality and the toxicity of the product in accordance with current pharmaceutical standards.
  • Synthesize  50g celecoxib .
Main results
  1. Identify the conditions for high performance synthesis process and minimizing the formation of by-products.
  2. Upgrade the celecoxib syhthesis process from  2g / batch scale to 20g/ batch scale, obtaining purified products with no traces detected of the regioisomer isomers and total yield of 70.1%.
  3. Apply the process of 20g/batch scale to synthesize 52g celecoxib with no traces of isomers regioisomer and the overall yield after purification was 70.1%.
  4. Tests five qualities entities based on celecoxib COA of Aarti Drugs Company Limited. Content of celecoxib achieves 98.7% calculated on the anhydrous basis.
  5. LD50 of Celecoxib: 3.09 g / kg body weight.
Novelty and actuality and scientific meaningfulness of the results

Currently celecoxib is protected by intellectural property, but the term of protection will end in 2013. Developing the production process of celecoxib in Vietnam at this time is to actively prepare before the time of switching from branch to generic. Since the product is achieved major commercial success in the pharmaceutical market with global sales of more than $5 billion (retail price in Vietnam about 5,000VND), the successful implementation of this project will contribute to break the monopoly of branch Celebrex ®, develop the domestic production of celecoxib in Vietnam and lower production costs. This will help arthritis patients having the opportunity to access this product in accordance with the economic conditions.

The project also aims to improve some existing problems, such as reaction time, reaction solvent, reaction medium, refined conditions, particularly focusing on the use of the recycled solvent recovered from process in order to increase the economic efficiency of the process.

Products of the project
 
  • Report on the results of the research project, including detailed description of the process, the spectra demonstrating the structure and purity.
  • Report on the quality test results and test of toxicity of the product.
  • 50g products celecoxib.
  • 01 articles: Journal of Chemistry. (2012) T50, 4B, p. 12 - 16.
  • Training of 01 master's students specializing in Pharmaceutical industry.
Recommendations
  • Study the continuous self private process of celecoxib synthesis from 4-methylacetophenon, skipping the diceton purification step.
  • Implement the half long term toxicity test.
  • Optimize the process and submit to the Ministry of Health for permission to use synthetic ingredients celecoxib to produce finished products.