Mechano-Chemical Activation and Stabilization of APIs by co-Milling

Kalt, Matthias and Ros, Angela and Iamartino, Piero and Mercuri, Salvatore and Crivelli, Daniele and Joost, Berndt (2018) Mechano-Chemical Activation and Stabilization of APIs by co-Milling. In: PBP World Meeting, 19.03.2018 - 22.03.2018, Granada, Spain.

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Poor drug dissolution and solubility are often the cause for low bioavailability. Counteracting can include physical modifications of active ingredients by increasing the surface area, solubility and wettability of powder particles with focus on particle size reduction and specific surface area increase or - on the other hand – with focus on the generation of the amorphous state [2]. During milling both the size reduction as well as the induced transition of a crystalline to an amorphous compound can be conducted at the same time. The aim of this work is to study the influence of general milling parameters like stressing energy (SE) and stressing number (SN) on particle size reduction and mechano-chemical activation (MCA) by vibration milling using a small scale mill. As feed particles lactose monohydrate, itraconazole (ITZ), a BSC II class antifungal drug and a blend of itraconazole and HPMC (1:3) were used.

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