A novel approach to crystallisation of nanodispersible microparticles by spray drying for improved tabletability

作者：Paluch Krzysztof J; Tajber Lidia; Adamczyk Bozena; Corrigan Owen I; Healy Anne Marie^*

来源：International Journal of Pharmaceutics, 2012, 436(1-2): 873-876.

DOI：10.1016/j.ijpharm.2012.05.074

• Spray drying
• Tabletability
• Specific surface area
• Nanocrystalline microparticles
• Erosion
• Nanosuspension

High-dose API powders which are to be tableted by direct compression should have high compactibility and compressibility. This note reports on a novel approach to the manufacture of crystalline powders intended for direct compaction with improved compactibility and compressibility properties. The poorly compactable API, chlorothiazide, was spray dried from a water/acetone solvent mix producing additive-free nanocrystalline microparticles (NCMPs) of median particle size 3.5 mu m. Tablets compacted from NCMPs had tensile strengths ranging from 0.5 to 4.6 MPa (compared to 0.6-0.9 MPa for tablets of micronised CTZ) at compression forces ranging from 6 kN to 13 kN. NCMP tablets also had high porosities (34-20%) and large specific surface areas (4.4-4.8 m(2)/g). The time taken for tablets made of NCMPs to erode was not statistically longer (p %26gt; 0.05) than for tablets made of micronised CTZ. Fragmentation of NCMPs on compression was observed. The volume fraction of particles below 1 mu m present in the suspension recovered after erosion of NCMP tablets was 34.8 + 3.43%, while no nanosized particles were detected in the slurry after erosion of compacted micronised CTZ.

• 出版日期2012-10-15