Antisolvent precipitation of novel xylitol-additive crystals to engineer tablets with improved pharmaceutical performance

Abstract

The purpose of this work was to develop stable xylitol particles with modified physical properties, improved compactibility and enhanced pharmaceutical performance without altering polymorphic form of xylitol. Xylitol was crystallized using antisolvent crystallization technique in the presence of various hydrophilic polymer additives, i.e., polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) at a range of concentrations. The crystallization process did not influence the stable polymorphic form or true density of xylitol. However, botryoidal-shaped crystallized xylitols demonstrated different particle morphologies and lower powder bulk and tap densities in comparison to subangular-shaped commercial xylitol. Xylitol crystallized without additive and xylitol crystallized in the presence of PVP or PVA demonstrated significant improvement in hardness of directly compressed tablets; however, such improvement was observed to lesser extent for xylitol crystallized in the presence of PEG. Crystallized xylitols produced enhanced dissolution profiles for indomethacin in comparison to original xylitol. The influence of additive concentration on tablet hardness was dependent on the type of additive, whereas an increased concentration of all additives provided an improvement in the dissolution behavior of indomethacin. Antisolvent crystallization using judiciously selected type and concentration of additive can be a potential approach to prepare xylitol powders with promising physicomechanical and pharmaceutical properties.

The Novel Use of PVP K30 as Templating Agent in Production of Porous Lactose

“…The crystal form of materials is mainly affected by the crystal habit, which can be modified by the presence of small amounts of a crystal modifier in the crystallization medium. Some hydrophilic polymers, such as PVP and hydroxypropyl cellulose, are commonly used for such a purpose [25,32]. Therefore, we speculate that in this study the hydrophilic polymer PVP K30 acts as a crystal modifier during the spray-drying process, so that porous lactose and Lactose-0 have different crystal types.…”

“…The better flowability of porous lactose could be due to the spheroidal shape and homogeneous particle size distribution. Relatively spheroidal shape and uniform particle size are conducive to improving the flowability and decreasing the values of AR, CI, and HR [31][32][33]. Small particles often led to poor flowability, but porous lactose exhibited the opposite phenomenon.…”

Surface Modifiers on Composite Particles for Direct Compaction

“…Surface modifiers (e.g., hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), and silica, etc.) are often utilized to modify the particle structure, thus, improving the properties of materials with poor DC properties [ 6 , 28 , 30 , 31 , 32 ]. Generally, these materials exhibit excellent properties for DC, such as good compactibility and flowability, fast disintegration, and low hygroscopicity.…”

On-line observation of the crystal growth in the case of the non-typical spherical crystallization methods of ambroxol hydrochloride

“…Among the typical crystallization methods, which usually mean three-solvent systems, the quasi emulsion solvent diffusion technique [11,12] was investigated. As non-typical methods, spherical agglomeration [13,14] (as an antisolvent technique with two solvents [15]) and slow cooling crystallization with an alternating temperature profile [16] were applied. It was revealed, that the non-typical methods are well-applicable to our model drug AMB HCl.…”