Improved Compaction and Packing Properties of Naproxen Agglomerated Crystals Obtained by Spherical Crystallization Technique

Abstract

Naproxen was crystallized from acetone-water in the presence of different concentrations of hydroxypropylcellulose (HPC). Naproxen particles recrystallized in the presence of HPC exhibited an obvious improvement in their packing, flow, and mechanical properties compared to naproxen recrystallized in the absence of the polymer (control particles). The results showed that the particle size distributions of the treated samples were broader than those obtained when HPC was absent. The agglomerates produced in the presence of 0.25% HPC displayed superior flow characteristics (displaying both a low angle of repose and Carr index) in comparison to samples produced in the presence of other concentrations of HPC. This was attributed to the spherical shape and smooth surface, since the area of contact in the powder bed for spherical agglomerates was smaller than that for other crystal shapes. However it was found that the tensile strength of tablets with the particles isolated in the presence of 1% HPC was increased to a greater extent than tablets produced using the spherical particles. Generally, the tensile strengths of the tablets increased with increasing concentrations of HPC present in the crystallization medium. Differential scanning calorimetry (DSC) and X-ray powder diffraction studies showed that naproxen particles, crystallized in the presence of HPC did not undergo structural modifications.

Design and evaluation of sustained release spherical agglomerates of Fluvastatin sodium by crystallo-co-agglomeration

“…Higher values of tensile strength of agglomerates compared to pure drug crystals indicated improvement in mechanical handling properties of agglomerates (Table 6). High tensile strength of compacts of agglomerates compared to that of pure drug crystals indicated strong interparticulate bonding generated between agglomerated crystals produced by crystalloco-agglomeration in presence of polymers (Maghsoodi et al, 2007).…”

“…Utilization of CCA in designing spherical agglomerates having excellent micromeritic and compression properties with satisfactory mechanical strength has been revealed in various studies. The technique has been successfully utilized for improving processability via enhancement in flow, compaction and packing properties (Maghsoodi et al, 2007;Maghsoodi and Tajalli Bakhsh, 2011). So far the technique has been applied for preparation of directly compressible sustained release agglomerates by few scientists (Jadhav et al, 2010;Gadekar et al, 2011); it is further required to study successful utilization of technique for the same.…”

Recrystallization of Drugs: Significance on Pharmaceutical Processing

“…The nature and amount of these changes count on the recrystallization conditions including the presence of impurities, type of solvents and cooling rates. This view is supported by a variety of papers at molecular level developing the knowledge of solid-state properties such as crystal structure, crystal habit, and polymorphism influence on the mechanical properties of powders in an attempt to identify and modify physical properties of bulk solids of drugs (Liebenberg et al, 1999;Maghsoodi et al, 2007).…”

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“…These findings suggested remarkable improvements in compactibility and packability of spherical agglomerates prepared with polymers due to improved micromeritic properties. [34] The parameters of Heckel plot for the pure drug crystals and agglomerates are depicted in Table 5. The true density was calculated as the density of compacts formed when maximum pressure (here 60 MPa) was applied on the powder/ agglomerates.…”