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Increasing dissolution rate of celecoxib using eutectic mixture formation

Other Titles
 Celecoxib의 용출율 증가를 위한 공융혼합물의 제조 
 Lee, Benjamin Joon 
Issue Date
Dept. of Pharmacy/석사
Eutectic mixture is a mixture composed of specific proportion of more than two components and shows same melting point. In pharmaceutics, the technique or concept usually used for making water insoluble drug or active pharmaceutical ingredient (API) to water soluble drug by mixing with water soluble excipients. As solubility increases, bioavailability is also increased in case of BCS class II drug.In this experiment, celecoxib (CEL), which is COX-2 selective inhibitor of NSAIDs, is used as a model BCS class II drug. The purpose of this experiment is to enhance dissolution rate by creating eutectic mixture with appropriate excipients.Four excipients (Adipic acid (ADI), citric acid (CIT), nicotinamide (NIC), and saccharin (SAC)) were selected through screening of excipients process via solvent evaporation method and DSC analysis. The selected excipients were used to create pure eutectic mixture via phase diagram of eutectic point. In this step, only CEL-ADI (50:50 in weight ratio) and CEL-SAC (90:10 in weight ratio) systems could successfully make eutectic mixtures. Dissolution rate of CEL-ADI and CEL-SAC were evaluated and results showed that CEL-ADI has hugely increased dissolution rate compared with CEL and CEL-SAC. To confirm the dissolution study result and to remove variables related with particle size, contact angle were measured. Even in similar or larger size, CEL-ADI showed the fastest dissolution. PXRD, NMR, Raman and FT-IR results shows that no chemical bonds were generated. It confirmed that the mixture was not salt, hydrate or co-crystal. Increasing dissolution rate without chemical interactions is caused by increasing wettability and surface area of CEL in eutectic mixture.The result illustrated increasing dissolution rate and bioavailability while maintaining chemical/biological characteristic of celecoxib only by researching on proportions of low molecular excipients. This method and concept will lead to easy, simple, and economical formulation design.
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