Cocrystallization via planetary milling: Enhancing throughput of solid-state screening methods

被引：50

作者：

Bysouth, Stephen R. ^{[1
]}

Bis, Joanna A. ^{[2
]}

Igo, David ^{[2
]}

机构：

[1] Automax SARL, F-50250 Lauvrairie, Varenguebec, France

[2] Catalent Pharma Solut, Opnform Technol TM, Morrisville, NC 27560 USA

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2011年 / 411卷 / 1-2期

关键词：

Cocrystal; Grinding; Milling; High-throughput; Automation; Solvent drop; SDG; Mechanochemical; Screening; CO-CRYSTAL; PHARMACEUTICAL COCRYSTALS; MECHANOCHEMISTRY; CARBAMAZEPINE; MICROSCOPY;

D O I：

10.1016/j.ijpharm.2011.03.037

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The application of a novel modified planetary mill, with the capacity to process 48 samples in parallel, to the rapid screening of pharmaceutical cocrystals via grinding is demonstrated for carbamazepine/saccharin, caffeine/oxalic acid, and caffeine/maleic acid cocrystals. Milling is performed directly in standard glass vials therefore no vessel decontamination is needed or sample loss occurs. Furthermore, successive sample processing can be employed without the need for additional material, making the system suitable for screening compounds of limited availability. Use of the system in an automated screening workflow of dispensing, milling, and analysis with high-throughput is also discussed. (C) 2011 Elsevier B.V. All rights reserved.

引用

页码：169 / 171

页数：3

共 19 条

[1] Applying hot-stage microscopy to co-crystal screening: A study of nicotinamide with seven active pharmaceutical ingredients [J].

Berry, David J. ;

Seaton, Colin C. ;

Clegg, William ;

Harrington, Ross W. ;

Coles, Simon J. ;

Horton, Peter N. ;

Hursthouse, Michael B. ;

Storey, Richard ;

Jones, William ;

Friscic, Tomislav ;

Blagden, Nicholas .

CRYSTAL GROWTH & DESIGN, 2008, 8 (05) :1697-1712

[2] Hierarchy of supramolecular synthons:: Persistent hydroxyl•••pyridine hydrogen bonds in cocrystals that contain a cyano acceptor [J].

Bis, Joanna A. ;

Vishweshwar, Peddy ;

Weyna, David ;

Zaworotko, Michael J. .

MOLECULAR PHARMACEUTICS, 2007, 4 (03) :401-416

[3]

BYSOUTH SR, 2008, Patent No. 7448566

[4]

BYSOUTH SR, 2006, Patent No. 2006086567

[5]

BYSOUTH SR, 2009, Patent No. 7501094

[6] Screening strategies based on solubility and solution composition generate pharmaceutically acceptable cocrystals of carbamazepine [J].

Childs, Scott L. ;

Rodriguez-Hornedo, Nair ;

Reddy, L. Sreenivas ;

Jayasankar, Adivaraha ;

Maheshwari, Chinmay ;

McCausland, Linda ;

Shipplett, Rex ;

Stahly, Barbara C. .

CRYSTENGCOMM, 2008, 10 (07) :856-864

[7] The role of solvent in mechanochemical and sonochemical cocrystal formation: a solubility-based approach for predicting cocrystallisation outcome [J].

Friscic, Tomislav ;

Childs, Scott L. ;

Rizvi, Syed A. A. ;

Jones, William .

CRYSTENGCOMM, 2009, 11 (03) :418-426

[8] Mechanisms by which moisture generates cocrystals [J].

Jayasankar, Adivaraha ;

Good, David J. ;

Rodriguez-Hornedo, Nair .

MOLECULAR PHARMACEUTICS, 2007, 4 (03) :360-372

[9] High-throughput cocrystal slurry screening by use of in situ Raman microscopy and multi-well plate [J].

Kojima, Takashi ;

Tsutsumi, Shunichirou ;

Yamamoto, Katsuhiko ;

Ikeda, Yukihiro ;

Moriwaki, Toshiya .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 399 (1-2) :52-59

[10] Factors that influence the spontaneous formation of pharmaceutical cocrystals by simply mixing solid reactants [J].

Maheshwari, Chinmay ;

Jayasankar, Adivaraha ;

Khan, Neman A. ;

Amidon, Gregory E. ;

Rodriguez-Hornedo, Nair .

CRYSTENGCOMM, 2009, 11 (03) :493-500

← 1 2 →