• Journal of Pharmaceutical Investigation
• /
• v.41 no.1
• /
• pp.45-50
• /
• 2011

Nonclassical pathway of crystallization has been utilized to modify the properties and morphologies of inorganic and organic/inorganic materials. In here, the polymer-directed crystallization method has been applied to the pharmaceutical active ingredient to assess the applicability for as a particle engineering tool. The polymer-directed crystallization was successful to modifying the crystal size, habit and morphology, but it was not effective to discover the novel polymorphs of Sibutramine (SB). SB was selected as a model drug and polyacrylic acid (PAA), polyethylene imine (PEI) and chitosan (CHI) were added as a crystallization pathway modifier. SB was crystallized via drowning crystallization using methanol or ethanol as a solvent and water as a non-solvent. The significant interactions between polymer and the drug were confirmed by measuring the solubility of the drug in presence of polymer during the crystallization. The crystal forms of SB are characterized by X-ray diffraction (XRD), scanning electron microscope (SEM) and optical microscope (OM). The polymer-directed crystallization seems to be able to modify the crystal properties of pharmaceutical active ingredient, which is critical in determining the bioavailability, processability, and stability.

• Polymer(Korea)
• /
• v.33 no.2
• /
• pp.124-130
• /
• 2009

In presence of a polymer, the crystallization of low MW organic materials can be stopped at an intermediary step, where mesocrystals can be identified. A mesocrystal is defined as a superstructure of nanoparticles having polymer-adsorbed crystal faces on the scale of several hundred nanometers to micrometers. This study examined the effects of water soluble polymers and relevant parameters on the formation of guanosine-5'-monophosphate mesocrystals. It was observed in OM and SEM that GMP obtained in a polymer solution had a unique particle morphology different from the typical one of GMP. XRD analysis indicated that the polymer-directed crystallized GMP had a different polymorph of GMP. This result shows that the crystal structure of GMP can be changed by polymers. It was observed in TGA analysis that the polymer-directed crystallized GMP had a different water content, indicating a different type of hydrate.