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Insensitivity of compaction properties of brittle granules to size enlargement by roller compaction.
J Pharm Sci. 2007 May; 96(5):1445-50.JP

Abstract

Pharmaceutical granules prepared by roller compaction often exhibit significant loss of tabletability, that is, reduction in tensile strength, when compared to virgin powder. This may be attributed to granule size enlargement for highly plastic materials, for example, microcrystalline cellulose. The sensitivity of powder compaction properties on granule size variations impacts the robustness of the dry granulation process. We hypothesize that such sensitivity of compaction properties on granule size is minimum for brittle materials because extensive fracture of brittle granules during compaction minimizes differences in initial granule size. We tested the hypothesis using three common brittle excipients. Results show that the fine (44-106 microm), medium (106-250 microm), and coarse (250-500 microm) granules exhibit essentially identical tabletability below a certain critical compaction pressure, 100, 140, and 100 MPa for spray-dried lactose monohydrate, anhydrous dibasic calcium phosphate, and mannitol, respectively. Above respective critical pressure, tabletability lines diverge with smaller granules exhibiting slightly higher tablet tensile strength at identical compaction conditions. Overall, tabletability of brittle granules is insensitive to granule size enlargement. The results provide a scientific basis to the common practice of incorporating brittle filler to a typical tablet formulation processed by roller compaction granulation.

Authors+Show Affiliations

Pfizer Global Supply Chain, Global Research and Development, Ann Arbor, Michigan 48105, USA.No affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17455348

Citation

Wu, Sy-Juen, and Changquan 'Calvin' Sun. "Insensitivity of Compaction Properties of Brittle Granules to Size Enlargement By Roller Compaction." Journal of Pharmaceutical Sciences, vol. 96, no. 5, 2007, pp. 1445-50.
Wu SJ, Sun C. Insensitivity of compaction properties of brittle granules to size enlargement by roller compaction. J Pharm Sci. 2007;96(5):1445-50.
Wu, S. J., & Sun, C. (2007). Insensitivity of compaction properties of brittle granules to size enlargement by roller compaction. Journal of Pharmaceutical Sciences, 96(5), 1445-50.
Wu SJ, Sun C. Insensitivity of Compaction Properties of Brittle Granules to Size Enlargement By Roller Compaction. J Pharm Sci. 2007;96(5):1445-50. PubMed PMID: 17455348.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Insensitivity of compaction properties of brittle granules to size enlargement by roller compaction. AU - Wu,Sy-Juen, AU - Sun,Changquan 'Calvin', PY - 2007/4/25/pubmed PY - 2007/6/15/medline PY - 2007/4/25/entrez SP - 1445 EP - 50 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 96 IS - 5 N2 - Pharmaceutical granules prepared by roller compaction often exhibit significant loss of tabletability, that is, reduction in tensile strength, when compared to virgin powder. This may be attributed to granule size enlargement for highly plastic materials, for example, microcrystalline cellulose. The sensitivity of powder compaction properties on granule size variations impacts the robustness of the dry granulation process. We hypothesize that such sensitivity of compaction properties on granule size is minimum for brittle materials because extensive fracture of brittle granules during compaction minimizes differences in initial granule size. We tested the hypothesis using three common brittle excipients. Results show that the fine (44-106 microm), medium (106-250 microm), and coarse (250-500 microm) granules exhibit essentially identical tabletability below a certain critical compaction pressure, 100, 140, and 100 MPa for spray-dried lactose monohydrate, anhydrous dibasic calcium phosphate, and mannitol, respectively. Above respective critical pressure, tabletability lines diverge with smaller granules exhibiting slightly higher tablet tensile strength at identical compaction conditions. Overall, tabletability of brittle granules is insensitive to granule size enlargement. The results provide a scientific basis to the common practice of incorporating brittle filler to a typical tablet formulation processed by roller compaction granulation. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/17455348/Insensitivity_of_compaction_properties_of_brittle_granules_to_size_enlargement_by_roller_compaction_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(16)32256-0 DB - PRIME DP - Unbound Medicine ER -