Polymorphs, Salts, and Cocrystals: What's in a Name?

被引：821

作者：

Aitipamula, Srinivasulu ^{[2
]}

Banerjee, Rahul ^{[3
]}

Bansal, Arvind K. ^{[4
]}

Biradha, Kumar ^{[5
]}

Cheney, Miranda L. ^{[6
]}

Choudhury, Angshuman Roy ^{[7
]}

Desiraju, Gautam R. ^{[1
]}

Dikundwar, Amol G. ^{[1
]}

Dubey, Ritesh ^{[1
]}

Duggirala, Nagakiran ^{[8
]}

Ghogale, Preetam P. ^{[9
]}

Ghosh, Soumyajit ^{[10
]}

Goswami, Pramod Kumar ^{[11
]}

Goud, N. Rajesh ^{[12
]}

Jetti, Ram R. K. R. ^{[13
]}

Karpinski, Piotr ^{[14
]}

Kaushik, Poonam ^{[15
]}

Kumar, Dinesh ^{[11
]}

Kumar, Vineet ^{[11
]}

Moulton, Brian ^{[8
]}

Mukherjee, Arijit ^{[1
]}

Mukherjee, Gargi ^{[5
]}

Myerson, Allan S. ^{[16
]}

Puri, Vibha

Ramanan, Arunachalam ^{[11
]}

Rajamannar, T. ^{[17
]}

Reddy, C. Malla ^{[10
]}

Rodriguez-Hornedo, Nair ^{[18
]}

Rogers, Robin D. ^{[19
]}

Row, T. N. Guru ^{[1
]}

Sanphui, Palash ^{[12
]}

Shan, Ning ^{[6
]}

Shete, Ganesh ^{[4
]}

Singh, Amit ^{[11
]}

Sun, Changquan C. ^{[20
]}

Swift, Jennifer A. ^{[21
]}

Thaimattam, Ram ^{[15
]}

Thakur, Tejender S. ^{[22
]}

Thaper, Rajesh Kumar ^{[15
]}

Thomas, Sajesh P. ^{[1
]}

Tothadi, Srinu ^{[1
]}

Vangala, Venu R. ^{[2
]}

Variankaval, Narayan ^{[23
]}

Vishweshwar, Peddy ^{[24
]}

Weyna, David R. ^{[6
]}

Zaworotko, Michael J. ^{[8
]}

机构：

[1] Indian Inst Sci, Solid State & Struct Chem Unit, Bangalore 560012, Karnataka, India

[2] ASTAR, Inst Chem & Engn Sci, Singapore 627833, Singapore

[3] Natl Chem Lab, Pune 411008, Maharashtra, India

[4] NIPER, Dept Pharmaceut, Sas Nagar 160062, Punjab, India

[5] Indian Inst Technol, Dept Chem, Kharagpur 721302, W Bengal, India

[6] Pharmaceut Inc, Tampa, FL 33612 USA

[7] Indian Inst Sci Educ & Res, Mohali 140306, Punjab, India

[8] Univ S Florida, Dept Chem, Tampa, FL 33620 USA

[9] Piramal Healthcare Ltd, Pharmaceut R&D, Bombay 400063, Maharashtra, India

[10] Indian Inst Sci Educ & Res, Dept Chem Sci, Kolkata 741252, W Bengal, India

[11] Indian Inst Technol, Dept Chem, Solid State & Mat Chem Grp, New Delhi 110016, India

[12] Univ Hyderabad, Sch Chem, Hyderabad 500046, Andhra Pradesh, India

[13] Mylan Labs Ltd, API R&D, Div Chem Res, Jinnaram Mandal 502325, AP, India

[14] Novartis Pharmaceut, E Hanover, NJ 07936 USA

[15] Ranbaxy Labs Ltd, Chem Res, Udyog Vihar Ind Area, Gurgaon 122015, Haryana, India

[16] MIT, Dept Chem Engn, Cambridge, MA 02139 USA

[17] Sun Pharma Adv Res Co Ltd, Vadodara 390020, Gujarat, India

[18] Univ Michigan, Coll Pharm, Ann Arbor, MI 48109 USA

[19] Univ Alabama, Dept Chem, Tuscaloosa, AL 35487 USA

[20] Univ Minnesota, Coll Pharm, Dept Pharmaceut, Minneapolis, MN 55455 USA

[21] Georgetown Univ, Dept Chem, Washington, DC 20057 USA

[22] Cent Drug Res Inst, CSIR, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India

[23] Merck Res Labs, Summit, NJ 07901 USA

[24] Dr Reddys Labs Ltd, Integrated Prod Dev, API Finishing Technol, Hyderabad, Andhra Pradesh, India

来源：

CRYSTAL GROWTH & DESIGN | 2012年 / 12卷 / 05期

关键词：

MULTIPLE-COMPONENT CRYSTALS; PHARMACEUTICAL COCRYSTALS; CO-CRYSTALS; ACID; STATE; CARBAMAZEPINE; PROPERTY; PRODUCT; IMPROVE; SCIENCE;

D O I：

10.1021/cg3002948

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The December 2011 release of a draft United States Food and Drug Administration (FDA) guidance concerning regulatory classification of pharmaceutical cocrystals of active pharmaceutical ingredients (APIs) addressed two matters of topical interest to the crystal engineering and pharmaceutical science communities: (1) a proposed definition of cocrystals; (2) a proposed classification of pharmaceutical cocrystals as dissociable "API-excipient" molecular complexes. The Indo U.S. Bilateral Meeting sponsored by the Indo-U.S. Science and Technology Forum titled The Evolving Role of Solid State Chemistry in Pharmaceutical Science was held in Manesar near Delhi, India, from February 2-4, 2012. A session of the meeting was devoted to discussion of the FDA guidance draft. The debate generated strong consensus on the need to define cocrystals more broadly and to classify them like salts. It was also concluded that the diversity of API crystal forms makes it difficult to classify solid forms into three categories that are mutually exclusive. This perspective summarizes the discussion in the Indo-U.S. Bilateral Meeting and includes contributions from researchers who were not participants in the meeting.

引用

页码：2147 / 2152

页数：6

共 60 条

[1] Building co-crystals with molecular sense and supramolecular sensibility [J].

Aakeröy, CB ;

Salmon, DJ .

CRYSTENGCOMM, 2005, 7 :439-448

[2] Cocrystal or salt:: Does it really matter? [J].

Aakeroy, Christer B. ;

Fasulo, Meg E. ;

Desper, John .

MOLECULAR PHARMACEUTICS, 2007, 4 (03) :317-322

[3] Crystal engineering of the composition of pharmaceutical phases.: Do pharmaceutical co-crystals represent a new path to improved medicines? [J].

Almarsson, Ö ;

Zaworotko, MJ .

CHEMICAL COMMUNICATIONS, 2004, (17) :1889-1896

[4]

[Anonymous], 2011, GUID IND REG CLASS P

[5] Solubility Advantage of Amorphous Drugs and Pharmaceutical Cocrystals [J].

Babu, N. Jagadeesh ;

Nangia, Ashwini .

CRYSTAL GROWTH & DESIGN, 2011, 11 (07) :2662-2679

[6] The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics [J].

Bak, Annette ;

Gore, Anu ;

Yanez, Evelyn ;

Stanton, Mary ;

Tufekcic, Sunita ;

Syed, Rashid ;

Akrami, Anna ;

Rose, Mark ;

Surapaneni, Sekhar ;

Bostick, Tracy ;

King, Anthony ;

Neervannan, Sesha ;

Ostovic, Drazen ;

Koparkar, Arun .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 97 (09) :3942-3956

[7]

Bauer V.J., 2011, [No title captured], Patent No. [US8058437B2, 8058437, U.S. 8,058,437]

[8] PHARMACEUTICAL SALTS [J].

BERGE, SM ;

BIGHLEY, LD ;

MONKHOUSE, DC .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1977, 66 (01) :1-19

[9] Ternary and quaternary co-crystals of 1,3-cis,5-cis-cyclohexanetricarboxylic acid and 4,4′-bipyridines [J].

Bhogala, Balakrishna R. ;

Nangia, Ashwini .

NEW JOURNAL OF CHEMISTRY, 2008, 32 (05) :800-807

[10] The 2-aminopyridinium-carboxylate supramolecular heterosynthon: A robust motif for generation of multiple-component crystals [J].

Bis, JA ;

Zaworotko, MJ .

CRYSTAL GROWTH & DESIGN, 2005, 5 (03) :1169-1179

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