Use of the Direct Compression Aid Ludiflash^® for the preparation of pellets via wet extrusion/spheronization

Abstract

Objective: Conventional solid oral dosage forms are unsuitable for children due to problems associated with swallowing and unpleasant taste. Additionally, the limit of tablets lays in the patient adapted dosing. Therefore, the suitability of Ludiflash^®, a direct compression aid for orally disintegrating tablets, was investigated for the preparation of individually dosable pellets.

Materials and methods: Micropellets consisting of Ludiflash^® and small amounts of microcrystalline cellulose were prepared via the wet extrusion/spheronization technique. Paracetamol and ibuprofen were applied as model drugs. The obtained pellets were characterized with respect to drug release and disintegration characteristics, mechanical properties, as well as size and shape.

Results and discussion: Drug loading was possible up to 30% for ibuprofen and even up to 50% for paracetamol. Higher ibuprofen loadings resulted in considerably slowed drug release and higher paracetamol contents yielded in non-spherical pellets. In vitro release studies revealed that more than 80% of the drug was released within 30 and 60 min for paracetamol and ibuprofen, respectively. Drug release rates were highly influenced by the pellet disintegration behavior. Investigations of the release mechanism using the Korsemeyer-Peppas approach suggested Super Case II drug transport for all paracetamol formulations and anomalous drug transport for most ibuprofen formulations. All pellets exhibited a low porosity and friability, as well as a sufficiently high tensile strength, which was significantly influenced by the type of model drug.

Conclusion: Ludiflash^® can be applied as main excipient for the preparation of individually dosable pellets combining fast drug release and a high mechanical stability.

Keywords::

• Fast drug release
• multi-particulate dosage forms
• disintegration
• paracetamol
• ibuprofen

Acknowledgments

The authors thank BASF (Ludwigshafen, Germany) for supplying Ludiflash^® and G.L. Pharma GesmbH for supplying paracetamol and ibuprofen. The authors also thank Ing. E. Prager from Ing. Prager Elektronik GesmbH, Wolkersdorf, Austria, for his assistance with the image analysis of the primary powders and Dr. J. Wagner, FELMI, Graz, Austria for his assistance using the electron microscope. Furthermore, Johannes Hofer, RCPE GmbH, Graz, Austria is acknowledged for his help with the contact angle measurements.

Declaration of interest

The authors report no declarations of interest.