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

Abstract

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.

Nutmeg Essential Oil, Red Clover, and Liquorice Extracts Microencapsulation Method Selection for the Release of Active Compounds from Gel Tablets of Different Bases

“…Powders with higher moisture and irregular form have worse flowability [ 28 ]. In the pharmaceutical industry, powder flowability is a crucial parameter that affects manufacturing efficiency because of layer generation capabilities and content uniformity [ 29 , 30 ]. Consequently, preparing the powders flowability parameter should be a priority to produce quality product.…”

Using Chia Powder as a Binder to Obtain Chewable Tablets Containing Quinoa for Dietary Fiber Supplementation

“…The formulations that exhibited exceptional flow properties, with a value of <15%, were T8, T7, and T6. The other formulations had a reasonable flow rate, or assistance was required, which, in both cases, can be solved with the addition of excipients that help with the fluidity of the powder, for example, a rheology promoter such as silicon dioxide [41]; a diluent to aid filling and compressibility such as microcrystalline cellulose, lactose, or co-processed products [42]; and lubricants such as magnesium stearate [43].…”

“…The granule diameter values were heterogeneous and had a wide range at 996 41,. 439.77, 766.21, 785.51, 579.56, 966.91, 800.44, 446.30, and 1040.71 µm, respectively (Figure…”

Use of Chia as a Binder to Obtain Chewable Tablets Containing Quinoa for Dietary Fiber Supplementation

“…The formulations that exhibited exceptional flow properties, with a value of < 15%, were R8, R7, and R6, respectively. The other formulations have a reasonable flow rate or assistance is required, which in both cases can be solved with the addition of excipients that help with the fluidity of the powder, for example, a rheology promoter such as silicon dioxide [35], a diluent to aid filling and compressibility such as microcrystalline cellulose, lactose or co-processed products [36], and lubricants such as magnesium stearate [37].…”