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Overcoming poor tabletability of pharmaceutical crystals by surface modification.
Pharm Res. 2011 Dec; 28(12):3248-55.PR

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) < 10 μm, 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 200 MPa, 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 1.9-7.0 MPa) at 200 MPa. 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.

Authors+Show Affiliations

Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota 55455, USA. shilimin02@gmail.comNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.

Language

eng

PubMed ID

21710340

Citation

Shi, Limin, and Changquan Calvin Sun. "Overcoming Poor Tabletability of Pharmaceutical Crystals By Surface Modification." Pharmaceutical Research, vol. 28, no. 12, 2011, pp. 3248-55.
Shi L, Sun CC. Overcoming poor tabletability of pharmaceutical crystals by surface modification. Pharm Res. 2011;28(12):3248-55.
Shi, L., & Sun, C. C. (2011). Overcoming poor tabletability of pharmaceutical crystals by surface modification. Pharmaceutical Research, 28(12), 3248-55. https://doi.org/10.1007/s11095-011-0518-2
Shi L, Sun CC. Overcoming Poor Tabletability of Pharmaceutical Crystals By Surface Modification. Pharm Res. 2011;28(12):3248-55. PubMed PMID: 21710340.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Overcoming poor tabletability of pharmaceutical crystals by surface modification. AU - Shi,Limin, AU - Sun,Changquan Calvin, Y1 - 2011/06/28/ PY - 2011/03/03/received PY - 2011/06/16/accepted PY - 2011/6/29/entrez PY - 2011/6/29/pubmed PY - 2012/4/7/medline SP - 3248 EP - 55 JF - Pharmaceutical research JO - Pharm Res VL - 28 IS - 12 N2 - 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) < 10 μm, 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 200 MPa, 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 1.9-7.0 MPa) at 200 MPa. 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. SN - 1573-904X UR - https://www.unboundmedicine.com/medline/citation/21710340/Overcoming_poor_tabletability_of_pharmaceutical_crystals_by_surface_modification_ L2 - https://doi.org/10.1007/s11095-011-0518-2 DB - PRIME DP - Unbound Medicine ER -