Development of Delayed-Release Pellets of Ibuprofen Using Kollicoat® MAE 100P via Hot-Melt Extrusion Technology

Abstract

Purpose

The present work was intended to develop the ibuprofen-Kollicoat^® MAE 100P delayed-release pellets using hot-melt extrusion technology, which exhibits pH-dependent solubility. Ibuprofen irritates the gastric lining, so its release in the gastric environment is not desired. Conventionally, Kollicoat^® MAE 100P has been used as an enteric coating polymer, and we have explored its application using hot-melt extrusion technology in our work.

Methods

Three different drug loadings were processed at various extrusion temperatures using HME to produce pellets of uniform size. DSC was performed to study the drug’s state, the polymer’s thermal behavior, and drug-polymer miscibility. An in vitro drug release study was performed in 0.1N HCl followed by pH 6.8 phosphate buffer to understand the ability of the polymer to impede the release of ibuprofen in the stomach. Furthermore, the lead batch was characterized by DSC, FTIR, HS-PLM, and optical microscopy to study the interaction between the drug and polymer.

Results

The thermogram of the pellets indicated no drug-polymer immiscibility. This work also demonstrates proof of the plasticizing ability of ibuprofen. Drug release studies showed less than 1.5% drug release in 0.1N HCl in 2 h, and complete drug release was obtained in the next 2 h in pH 6.8 phosphate buffer, indicating the delayed-release characteristics of the pellets.

Conclusion

This work proves that Kollicoat^® MAE 100P could be used in modified-release dosage forms to attain the delayed-release pellets.