Improving the Powder Properties of an Active Pharmaceutical Ingredient (Ethenzamide) with a Silica Nanoparticle Coating for Direct Compaction into Tablets

To improve the powder properties of active pharmaceutical ingredients (APIs), we coated APIs with silica nanoparticles using a dry process that allowed for direct compression into tablets. The dry coating performed with different apparatuses (a batch-type high-speed shear mixer (Mechanomill) and a c...

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Bibliographic Details
Published in:	Powders Vol. 1; no. 4; pp. 231 - 242
Main Authors:	Tadauchi, Tatsuki, Yamada, Daiki, Koide, Yoko, Yamada, Mayumi, Shimada, Yasuhiro, Yamazoe, Eriko, Ito, Takaaki, Tahara, Kohei
Format:	Journal Article
Language:	English
Published:	MDPI AG 21-11-2022
Subjects:	Comil dry coating ethenzamide powder flowability silica nanoparticles
Online Access:	Get full text
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Summary:	To improve the powder properties of active pharmaceutical ingredients (APIs), we coated APIs with silica nanoparticles using a dry process that allowed for direct compression into tablets. The dry coating performed with different apparatuses (a batch-type high-speed shear mixer (Mechanomill) and a continuous conical screen mill (Comil)) and properties of the resulting dry-coated APIs were compared. Ethenzamide (ETZ), which has low powder flowability, was selected as the host particle to be improved and the colloidal silicas Aerosil 200 and R972 were used as the guest particles. Both coating processes and types of silica nanoparticles improved the powder flowability (angle of repose) of ETZ under unstressed conditions. Inverse gas chromatography demonstrated that dry coating with silica nanoparticles reduced the surface free energy and improved the homogeneity of the surface energy distribution of ETZ particles. Under the stress conditions of a shear cell test, the Mechnomill-based treatment improved the powder flowability of ETZ from that of untreated ETZ; however, the Comil-based treatment did not improve the flowability. The mechanical shear force exerted by Comil was apparently insufficient for interactions between host and guest particles. However, the properties of tableted ETZ were enhanced even when the silica nanoparticles were coated using Comil.
ISSN:	2674-0516 2674-0516
DOI:	10.3390/powders1040016