caa a22 4500 445312491 CHVBK 20180317142635.0 cr unu---uuuuu 170323e20111201xx s 000 0 eng 10.1007/s11095-011-0518-2 doi (NATIONALLICENCE)springer-10.1007/s11095-011-0518-2 Overcoming Poor Tabletability of Pharmaceutical Crystals by Surface Modification [Elektronische Daten] [Limin Shi, Changquan Sun] ABSTRACT: Purpose: To test the hypothesis that coating particles with a highly bonding polymer is effective in improving tabletability of poorly compressible drugs. Methods: Micronized acetaminophen (d 90 < 10μm, Form I) was coated with 1%-10% (wt%) hydroxypropyl cellulose (HPC) by spray-drying. Phase nature of acetaminophen powders was identified using powder X-ray diffractometry, SEM, and thermal analysis. Powder tabletability was evaluated on a compaction simulator. Mechanical properties of acetaminophen and HPC were determined by nanoindentation. Results: Spray-drying successfully produced acetaminophen particles enveloped with a layer of HPC but did not cause any detectable phase change of acetaminophen. At 200MPa, physical mixtures containing up to 40% HPC could not be compressed into intact tablets. In contrast, acetaminophen coated with 1% to 10% HPC could form strong tablets (tensile strength was 1.9-7.0MPa) at 200MPa. Under a given compaction pressure, tablet tensile strength increased sharply with the amount of HPC coating. The profoundly improved tabletability of acetaminophen confirmed the effectiveness of the particle coating approach in improving tableting performance of drugs. Conclusions: HPC coating by spray-drying profoundly enhances tabletability of acetaminophen. This strategy is expected to have transformative effects on formulation development of poorly compressible drugs. Springer Science+Business Media, LLC, 2011 acetaminophen nationallicence nanoindentation nationallicence plasticity nationallicence surface engineering nationallicence tabletability nationallicence Shi Limin Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., 55455, Minneapolis, Minnesota, USA aut Sun Changquan Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., 55455, Minneapolis, Minnesota, USA aut Pharmaceutical Research Springer US; http://www.springer-ny.com 28/12(2011-12-01), 3248-3255 0724-8741 28:12<3248 2011 28 11095 https://doi.org/10.1007/s11095-011-0518-2 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11095-011-0518-2 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Shi Limin Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., 55455, Minneapolis, Minnesota, USA aut NATIONALLICENCE 700 1- Sun Changquan Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., 55455, Minneapolis, Minnesota, USA aut NATIONALLICENCE 773 0- Pharmaceutical Research Springer US; http://www.springer-ny.com 28/12(2011-12-01), 3248-3255 0724-8741 28:12<3248 2011 28 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer