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共无定形药物——新型单相无定形二元体系
郭慧慧1, 苗娜娜1, 李腾飞2, 郝君1, 高缘2, 张建军*1
化学进展 ›› 2014, Vol. 26 ›› Issue (0203) :478-486
共无定形药物——新型单相无定形二元体系
郭慧慧1, 苗娜娜1, 李腾飞2, 郝君1, 高缘2, 张建军*1
化学进展 ›› 2014, Vol. 26 ›› Issue (0203) :478-486
共无定形药物——新型单相无定形二元体系
Pharmaceutical Coamorphous——A Newly Defined Single-Phase Amorphous Binary System
共无定形药物是活性药物成分与其他小分子固体物质（药物或辅料）结合形成的具有单一玻璃化转变温度的单相无定形二元体系。它作为一种新的药物固体形态，可能改善药物的溶解度、溶出速率、稳定性及生物利用度等理化性质，已成为药物研发的一种新途径。本文主要对共无定形药物的定义、形成机理、制备方法、分析鉴别方法、物理化学稳定性以及溶解度和溶出速率进行综述，并对共无定形与固体分散体和共晶的比较进行了概述。
Pharmaceutical coamorphous, a kind of single-phase amorphous binary system, is formed between an active pharmaceutical ingredient (API1) and another solid small molecular compound (API2 or excipient). As a newly defined solid form, pharmaceutical coamorphous has been one new approach for drug research and development, due to its great potential in the improvement of solubility, dissolution, stability or even bioavailability. Several methods can be used for the preparation of coamorphous drugs, including quench-cooling, solvent evaporation and milling/cryo-milling. In this paper, the definition, preparation, physicochemical characterization and formation mechanism of pharmaceutical coamorphous are addressed. The comparison between coamorphous and solid dispersion or cocrystals is also presented.
Contents
1 Introduction
2 Overview of pharmaceutical coamorphous
2.1 Definition and classification of coamorphous
2.2 Comparison between coamorphous and solid dispersion
2.3 Relationship and differences of coamorphous and cocrystal
3 Formation mechanisms
3.1 Type of interaction
3.2 Flory-Huggins theory
4 Preparation of pharmaceutical coamorphous
4.1 Preparation methods
4.2 Factors affecting the formation of pharmaceutical coamorphous
5 Properties of pharmaceutical coamorphous
5.1 Identification
5.2 Stability
5.3 Solubility and dissolution
6 Outlooks
共无定形
coamorphous
[1] Radtke M. New Drugs, 2001, 3: 62.
[2] Hu J, Johnston K P, Williams R O. Int. J. Pharm., 2004, 271: 145.
[3] 马坤(Ma K), 高静(Gao J), 马磊(Ma L). 中国药科大学学报(Journal of China Pharmaceutical University), 2012, 43(5): 475.
[4] 高缘(Gao Y), 祖卉(Zu H), 张建军(Zhang J J). 化学进展(Progress in Chemistry), 2010, 22(5): 829.
[5] Lara-ochoa F, Espinosa-pérez G. Supramol. Chem., 2007, 19: 553.
[6] Morissette S L, Almarsson O, Peterson M L, Remenar J F, Read M J, Lemmo A V, Ellis S, Cima M J, Gardner C R. Adv. Drug Deliver. Rev., 2004, 56: 275.
[7] Lu Q, Zografi G. Pharm. Res., 1998, 15: 1202.
[8] Löbmann K, Laitinen R, Grohganz H, Gordon K C, Strachan C, Rades T. Mol. Pharm., 2011, 8: 1919.
[9] Descamps M, Willart J F, Dudognon E, Caron V. Journal of Pharmaceutical Science, 2007, 96: 1398.
[10] Hoppu P, Jouppila K, Rantanen J, Schantz S, Juppo A M. J. Pharm. Pharmacol., 2007, 59: 373.
[11] Schilling S U, Bruce C D, Shah N H, Malick A W, McGinity J W. Int. J. Pharm., 2008, 361: 158.
[12] Masuda T, Yoshihashi Y, Yonemochi E, Fujii K, Uekusa H, Terada K. Int. J. Pharm., 2012, 422: 160.
[13] Gao Y, Liao J, Qi X, Zhang J. Int. J. Pharm., 2013, 450: 290.
[14] Ahuja N, Katare O P, Singh B. Eur. J. Pharm. Biopharm., 2007, 65: 26.
[15] Löbnmann K, Grohganz H, Laitinen R, Strachan C, Rades T. Eur. J. Pharm. Biopharm., 2013, 85: 873.
[16] Alles M, Chieng N, Rehder S, Rantanen J, Rades T, Aaltonen J. J. Control. Release, 2009, 136: 45.
[17] Löbmann K, Strachan C, Grohganz H, Rades T, Korhonen O, Laitinen R. Eur. J. Pharm. Biopharm., 2012, 81: 159.
[18] Leuner C, Dressman J. Eur. J. Pharm. Biopharm., 2000, 50: 47.
[19] Serajuddin A T M. J. Pharm. Sci., 1999, 88: 1058.
[20] Zheng W, Jain A, Papoutsakis D, Dannenfelser R M, Panicucci R, Garad S. Drug Dev. Ind. Pharm., 2012, 38: 235.
[21] Vasconcelos T, Sarmento B, Costa P. Drug Discov. Today, 2007, 12: 1068.
[22] Janssens S, Mooter G V. J. Pharm. Pharmacol., 2009, 61: 1571.
[23] Qian F, Huang J, Hussain M A. J. Pharm. Sci., 2010, 99: 2941.
[24] Löbmann K, Laitinen R, Grohganz H, Strachan C, Rades T, Gordon K C. Int. J. Pharm., 2013, 453: 80.
[25] Yamamura S, Gotoh H, Sakamoto Y, Momose Y. Eur. J. Pharm. Biopharm., 2000, 49: 259.
[26] Yamamura S, Gotoh H, Sakamoto Y, Momose Y. Int. J. Pharm., 2002, 241: 213.
[27] Dudognon E, Willart J F, Caron V, Capet F, Larsson T, Descamps M. Solid State Commun., 2006, 138: 68.
[28] Chieng N, Aaltonen J, Saville D, Rades T. Eur. J. Pharm. Biopharm., 2009, 71: 47.
[29] Forster A, Hempenstall J, Tucker, Rades T. Drug Dev. Ind. Pharm., 2001, 27: 549.
[30] Schneider H A. Macromol. Chem. Phys., 1988, 189: 1941.
[31] Nair R, Nyamweya N, Gönen S, Martínez-Miranda L J, Hoag S W. Int. J. Pharm., 2001, 225: 83.
[32] Gupta P, Thilagavathi R, Chakraborti A K, Bansal A K. Mol. Pharm., 2005, 2: 384.
[33] Shamblin S L, Huang E Y, Zografi G. J. Therm. Anal. Calorim., 1996, 47: 1567.
[34] Taylor L S, Zografi G. J. Pharm. Sci., 1998, 87: 1615.
[35] Duer M J. Solid-State NMR Spectroscopy Principles and Applications. Blackwell Science, 2002. 391.
[36] Schantz S, Hoppu P, Juppo A M. J. Pharm. Sci., 2009, 98: 1862.
[37] Yu L. Adv. Drug Deliver. Rev., 2001, 48: 27.
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