Fine grade engineered microcrystalline cellulose excipients for direct compaction: Assessing suitability of different dry coating processes

被引:15
作者
Chen, Liang [1 ,2 ]
He, Zizhou [1 ]
Kunnath, Kuriakose [1 ]
Zheng, Kai [1 ]
Kim, Sangah [1 ]
Dave, Rajesh N. [1 ]
机构
[1] New Jersey Inst Technol, New Jersey Ctr Engn Particulates, Newark, NJ 07102 USA
[2] Biogen, Prod & Tech Dev, 225 Binney St, Cambridge, MA 02142 USA
基金
美国国家科学基金会;
关键词
Dry coating; Tableting; Particle engineering; Excipients; Direct compression; Process development; TABLET TENSILE-STRENGTH; CONICAL SCREEN MILL; FLOW PROPERTIES; FUNCTIONAL-PROPERTIES; PROCESS VARIABLES; BULK-DENSITY; POWDER; SILICA; PARTICLES; ADHESION;
D O I
10.1016/j.ejps.2020.105408
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Recent work showed that contrary to conventional wisdom, fine surface engineered excipients outperform their larger counterparts in blends of highly loaded blends of cohesive drug powders in terms of their packing, flowability and tablet tensile strength. Here, two continuous devices, fluid -energy mill (FEM) and conical mill (Comil), are compared with LabRAM, a batch device used in previous work, for nano -silica dry coating of microcrystalline cellulose (MCC) excipients, 20 and 30 ?m. Coated MCCs from all three devices had higher bulk densities and flow function coefficients (FFCs) compared with Avicel PH -102. Silica coating quality was best with LabRAM, but also good with FEM and Comil, although Comil was less effective for the finer MCC. However, the better coating quality of LabRAM had a downside of having poorer compaction properties. The most sur- prising outcome was that multi -component blends of 17 wt% coated MCC with 60 wt % Ibuprofen 50 had higher bulk density, higher or similar flowability, higher tablet tensile strength, and comparable Ibuprofen dissolution from tablets, compared to those with Prosolv 50, a silicified excipient. The FEM dry coated MCC blends, having only 0.17 wt% silica, performed the best, having desirable bulk density, FFC, and tensile strength that could facilitate high-speed direct compression tableting. In summary, considering that achieving best coating quality need not be the primary objective, FEM may be the best option for producing desired sized dry coated fine excipients.
引用
收藏
页数:10
相关论文
共 38 条
[1]  
Block LawrenceH., 2009, Pharmacopeial Forum, V35, P1026
[2]   Insight Into a Novel Strategy for the Design of Tablet Formulations Intended for Direct Compression [J].
Capece, Maxx ;
Huang, Zhonghui ;
Dave, Rajesh .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2017, 106 (06) :1608-1617
[3]   Controlled Release from Drug Microparticles via Solventless Dry-Polymer Coating [J].
Capece, Maxx ;
Barrows, Jason ;
Dave, Rajesh N. .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 104 (04) :1340-1351
[4]  
Carlin B., 2008, Pharmaceutical Dosage Forms: Tablets, Volume 2: Rational Design and Formulation, V2, P173
[5]   The relationship between attractive interparticle forces and bulk behaviour in dry and uncharged fine powders [J].
Castellanos, A .
ADVANCES IN PHYSICS, 2005, 54 (04) :263-376
[6]   Profoundly Improving Flow Properties of a Cohesive Cellulose Powder by Surface Coating with Nano-silica Through Comilling [J].
Chattoraj, Sayantan ;
Shi, Limin ;
Sun, Changquan Calvin .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2011, 100 (11) :4943-4952
[7]   Direct Compression Tablet Containing 99% Active Ingredient-A Tale of Spherical Crystallization [J].
Chen, Hongbo ;
Aburub, Aktham ;
Sun, Changquan Calvin .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2019, 108 (04) :1396-1400
[8]   Surface engineered excipients: III. Facilitating direct compaction tableting of binary blends containing fine cohesive poorly-compactable APIs [J].
Chen, Liang ;
He, Zizhou ;
Kunnath, Kuriakose T. ;
Fan, Siqi ;
Wei, Yuhan ;
Ding, Xiaoyi ;
Zheng, Kai ;
Dave, Rajesh N. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2019, 557 :354-365
[9]   Surface engineered excipients: II. Simultaneous milling and dry coating for preparation of fine-grade microcrystalline cellulose with enhanced properties [J].
Chen, Liang ;
Ding, Xiaoyi ;
He, Zizhou ;
Fan, Siqi ;
Kunnath, Kuriakose T. ;
Zheng, Kai ;
Dave, Rajesh N. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2018, 546 (1-2) :125-136
[10]   Surface engineered excipients: I. improved functional properties of fine grade microcrystalline cellulose [J].
Chen, Liang ;
Ding, Xiaoyi ;
He, Zizhou ;
Huang, Zhonghui ;
Kunnath, Kuriakose T. ;
Zheng, Kai ;
Dave, Rajesh N. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2018, 536 (01) :127-137