A novel approach to crystallisation of nanodispersible microparticles by spray drying for improved tabletability.
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 μm. 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 (4.4-4.8m(2)/g). The time taken for tablets made of NCMPs to erode was not statistically longer (p>0.05) than for tablets made of micronised CTZ. Fragmentation of NCMPs on compression was observed. The volume fraction of particles below 1 μm 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.
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, College Green, Dublin 2, Ireland.
Krzysztof J
KJ
Paluch
Lidia
L
Tajber
Bożena
B
Adamczyk
Owen I
OI
Corrigan
Anne Marie
AM
Healy
D002740:Chlorothiazide / Q000737:chemistry*; D003460:Crystallization; D003890:Desiccation; D004339:Drug Compounding / Q000379:methods*; D010316:Particle Size; D016062:Porosity; D011312:Pressure; D013499:Surface Properties; D013607:Tablets; D013718:Tensile Strength
D013607:Tablets; D002740:Chlorothiazide