Novel preparation approach with a 2-step process for spherical particles with high drug loading and controlled size distribution using melt granulation: MALCORE®
A novel approach for preparing drug-containing particles (DCPs) with controlled size distribution and high drug loading was developed using melt granulation. This approach comprises two steps. First, melting component adsorbed particles (MAs) were prepared by mixing and heating the melting components with a porous carrier using a high shear granulator. Second, DCPs were prepared by layering the drug on MAs using a fluidized bed rotor granulator. The time taken for both steps was within 30 min. Adding the polymer in the second step remarkably increased the viscosity of the mixture of melting components and the polymer.
Highlights
- • Novel two-step approach for making drug-containing particles using melt granulation.
- • Particle size distribution control by adsorbing melting component into porous carrier.
- • Spherical particles with high amounts of loaded drug was prepared.
- • The viscosity of the mixture of SA and AMCE increased by heating.
- • Particle characteristics and manufacturing time unaffected by manufacturing scale.
Therefore, DCPs could be successfully loaded with a high amount of drug (70% w/w). The particle size distribution of the DCPs was narrow, and it depended on that of the MAs. The flowability of the DCPs was excellent, and the sphericity was close to 1. A unique particle formulation mechanism was suggested based on the observation of DCPs using scanning electron microscopy. The manufacturing time and DCP characteristics were not affected by the manufacturing scale. In conclusion, we have successfully developed a highly efficient novel approach for preparing optimal DCPs through melt granulation, named “Melt Adsorption and Layering with Porosity Core” (MALCORE®).
About this article: Naoki Yoshihara, Ryota Kimata, Takayuki Terukina, Takanori Kanazawa, Hiromu Kondo,
Novel preparation approach with a 2-step process for spherical particles with high drug loading and controlled size distribution using melt granulation: MALCORE®, Advanced Powder Technology, Volume 33, Issue 2, 2022, 103409,
ISSN 0921-8831, https://doi.org/10.1016/j.apt.2021.103409. (https://www.sciencedirect.com/science/article/pii/S0921883121006063)