Recent advances in co-amorphous drug formulations

被引:372
作者
Dengale, Swapnil Jayant [1 ]
Grohganz, Holger [2 ]
Rades, Thomas [2 ]
Lobmann, Korbinian [2 ]
机构
[1] Manipal Univ, Manipal Coll Pharmaceut Sci, Manipal, Karnataka, India
[2] Univ Copenhagen, Dept Pharm, Copenhagen, Denmark
关键词
Co-amorphous; Solid dispersion; Poorly soluble drugs; Molecular interactions; Increased dissolution; WATER-SOLUBLE DRUGS; GLASS-TRANSITION TEMPERATURES; SOLID-STATE CHARACTERIZATION; IMPROVED PHYSICAL STABILITY; CITRIC-ACID; PHYSICOCHEMICAL PROPERTIES; ENHANCED DISSOLUTION; BINARY-SYSTEMS; AMINO-ACIDS; INTERMOLECULAR INTERACTIONS;
D O I
10.1016/j.addr.2015.12.009
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Co-amorphous drug delivery systems have recently gained considerable interest in the pharmaceutical field because of their potential to improve oral bioavailability of poorly water-soluble drugs through drug dissolution enhancement as a result of the amorphous nature of the material. A co-amorphous system is characterized by the use of only low molecular weight components that are mixed into a homogeneous single-phase co-amorphous blend. The use of only low molecular weight co-formers makes this approach very attractive, as the amount of amorphous stabilizer can be significantly reduced compared with other amorphous stabilization techniques. Because of this, several research groups started to investigate the co-amorphous formulation approach, resulting in an increasing amount of scientific publications over the last few years. This study provides an overview of the co-amorphous field and its recent findings. In particular, we investigate co-amorphous formulations from the viewpoint of solid dispersions, describe their formation and mechanism of stabilization, study their impact on dissolution and in vivo performance and briefly outline the future potentials. (c) 2016 Elsevier B.V. All rights reserved.
引用
收藏
页码:116 / 125
页数:10
相关论文
共 80 条
[1]   Towards Physico-Relevant Dissolution Testing: The Importance of Solid-State Analysis in Dissolution [J].
Aaltonen, Jaakko ;
Rades, Thomas .
DISSOLUTION TECHNOLOGIES, 2009, 16 (02) :47-54
[2]   PREPARATION AND PROPERTIES OF TABLETS PREPARED FROM FUROSEMIDE-PVP SOLID DISPERSION-SYSTEMS [J].
AKBUGA, J ;
GURSOY, A ;
YETIMOGLU, F .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1988, 14 (15-17) :2091-2108
[3]   Enhanced dissolution rate and synchronized release of drugs in binary systems through formulation: Amorphous naproxen-cimetidine mixtures prepared by mechanical activation [J].
Alleso, Morten ;
Chieng, Norman ;
Rehder, Soenke ;
Rantanen, Jukka ;
Rades, Thomas ;
Aaltonen, Jaakko .
JOURNAL OF CONTROLLED RELEASE, 2009, 136 (01) :45-53
[4]   Understanding the Behavior of Amorphous Pharmaceutical Systems during Dissolution [J].
Alonzo, David E. ;
Zhang, Geoff G. Z. ;
Zhou, Deliang ;
Gao, Yi ;
Taylor, Lynne S. .
PHARMACEUTICAL RESEARCH, 2010, 27 (04) :608-618
[5]  
[Anonymous], 2012, Drug Discov Today Technol, V9, pe71, DOI 10.1016/j.ddtec.2011.10.002
[6]   Evaluation of amorphous solid dispersion properties using thermal analysis techniques [J].
Baird, Jared A. ;
Taylor, Lynne S. .
ADVANCED DRUG DELIVERY REVIEWS, 2012, 64 (05) :396-421
[7]   Analysis of amorphous and nanocrystalline solids from their X-ray diffraction patterns [J].
Bates, Simon ;
Zografi, George ;
Engers, David ;
Morris, Kenneth ;
Crowley, Kieran ;
Newman, Ann .
PHARMACEUTICAL RESEARCH, 2006, 23 (10) :2333-2349
[8]   Prediction of glass transition temperatures: Binary blends and copolymers [J].
Brostow, Witold ;
Chiu, Rachel ;
Kalogeras, Ioannis M. ;
Vassilikou-Dova, Aglaia .
MATERIALS LETTERS, 2008, 62 (17-18) :3152-3155
[9]  
Brown C, 2014, ADV DEL SCI TECHNOL, P197, DOI 10.1007/978-1-4939-1598-9_6
[10]   Physical characterization and stability of amorphous indomethacin and ranitidine hydrochloride binary systems prepared by mechanical activation [J].
Chieng, Norman ;
Aaltonen, Jaakko ;
Saville, Dorothy ;
Rades, Thomas .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2009, 71 (01) :47-54