Development of dual–release pellets of the non-steroidal anti–inflammatory drug celecoxib

In the current study, once-a-day dual-release pellets of the selective non-steroidal anti-inflammatory drug celecoxib (200 mg) was developed to treat arthritis.

Pellets were prepared where a 100 mg celecoxib, located in the outer layer, was released in an immediate-release (IR) pattern, whereas the remaining 100 mg celecoxib, located in the inner layer, was released in a sustained-release (SR) pattern. Pellets were subjected to four coating- and loading-stages using solid-dispersion and spray-drying including seal-coating, drug-loading, SR-coating, and IR-loading.

Release studies were carried out using dissolution media with a pH range 1.2–12.0. The IR-stage showed a fast release rate, where 47.0% of celecoxib (equivalent to 94 mg) was released within the first hour. Whereas the SR-stage showed a sustained-release pattern up to 16 h. Celecoxib converted from crystalline form to amorphous form during the development of pellets. This in turn improves the aqueous solubility and hence the dissolution of celecoxib.

The results of stability studies showed that pellets were stable at 30 °C/65 %RH and 40 °C/75 %RH for 6 months. The present study demonstrated that celecoxib pellets can be an effective strategy for delivering the poorly-soluble drug celecoxib in a dual-release pattern. More on dual-release pellets