Physico-chemical characterisation of three-component co-amorphous systems generated by a melt-quench method

被引:18
作者
D'Angelo, A. [1 ]
Edgar, B. [1 ]
Hurt, A. P. [1 ]
Antonijevic, M. D. [1 ]
机构
[1] Univ Greenwich, Fac Engn & Sci, Chatham ME4 4TB, Kent, England
关键词
Co-amorphous; Stability; T-g; Crystallinity; Amorphicity; PHARMACEUTICAL SOLIDS; PHYSICAL STABILITY; DRUG FORMULATIONS; DISPERSIONS; STABILIZATION; INDOMETHACIN; ENHANCEMENT; SOLUBILITY;
D O I
10.1007/s10973-018-7291-y
中图分类号
O414.1 [热力学];
学科分类号
摘要
The purpose of this work was to evaluate the possibility of creating a ternary co-amorphous system and to determine how the properties of a co-amorphous material are altered by the addition of a selected third component. Piroxicam and indomethacin form a stable co-amorphous with the T-g above room temperature. The third component added was selected based on tendency to crystallise (benzamide, caffeine) or form amorphous (acetaminophen, clotrimazole) on cooling. Generated co-amorphous systems were characterised with TGA, HSM, DSC, FTIR and XRD. Stable ternary co-amorphous systems were successfully generated, which were confirmed using XRD, DSC and FTIR analysis. In all cases, T-g of the ternary system was lower than the T-g of the binary system, although higher than that of the individual third component. Upon storage for 4 weeks, all created ternary systems showed significantly smaller variation in T-g compared to the binary system. Stable three-component co-amorphous systems can be generated via melt-quench method using either a crystalline or an amorphous third component. Addition of third component can alter the T-g of co-amorphous system and in all cases created more stable co-amorphous system upon storage. Physical parameters may not be sufficient in predicting the resulting T-g; therefore, knowledge of chemical interaction must be brought into equation as well.
引用
收藏
页码:381 / 390
页数:10
相关论文
共 26 条
[1]   Co amorphous systems: A product development perspective [J].
Chavan, Rahul B. ;
Thipparaboina, Rajesh ;
Kumar, Dinesh ;
Shastri, Nalini R. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 515 (1-2) :403-415
[2]   Development and physicochemical characterization of solid dispersions containing praziquantel for the treatment of schistosomiasis [J].
Dametto, P. R. ;
Dametto, A. C. ;
Polese, L. ;
Ribeiro, C. A. ;
Chorilli, M. ;
de Freitas, Osvaldo .
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY, 2017, 127 (02) :1693-1706
[3]   Recent advances in co-amorphous drug formulations [J].
Dengale, Swapnil Jayant ;
Grohganz, Holger ;
Rades, Thomas ;
Lobmann, Korbinian .
ADVANCED DRUG DELIVERY REVIEWS, 2016, 100 :116-125
[4]   The Need for Restructuring the Disordered Science of Amorphous Drug Formulations [J].
Edueng, Khadijah ;
Mahlin, Denny ;
Bergstrom, Christel A. S. .
PHARMACEUTICAL RESEARCH, 2017, 34 (09) :1754-1772
[5]   Effect of composition and drying method on glass transition temperature, water sorption characteristics and surface morphology of newly designed β-lactoglobulin/retinyl palmitate/disaccharides systems [J].
Gorska, Agata ;
Szulc, Karolina ;
Ostrowska-Ligeza, Ewa ;
Brys, Joanna ;
Wirkowska-Wojdyla, Magdalena .
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY, 2017, 130 (01) :177-185
[6]  
Graeser Kirsten A, 2010, Pharmaceutics, V2, P224
[7]   Physical stability of pharmaceutical formulations: solid-state characterization of amorphous dispersions [J].
Guo, Yushen ;
Shalaev, Evgenyi ;
Smith, Scott .
TRAC-TRENDS IN ANALYTICAL CHEMISTRY, 2013, 49 :137-144
[8]   What is the true solubility advantage for amorphous pharmaceuticals? [J].
Hancock, BC ;
Parks, M .
PHARMACEUTICAL RESEARCH, 2000, 17 (04) :397-404
[9]   Enhancement of the Physical Stability of Amorphous Indomethacin by Mixing it with Octaacetylmaltose. Inter and Intra Molecular Studies [J].
Kaminska, E. ;
Adrjanowicz, K. ;
Zakowiecki, D. ;
Milanowski, B. ;
Tarnacka, M. ;
Hawelek, L. ;
Dulski, M. ;
Pilch, J. ;
Smolka, W. ;
Kaczmarczyk-Sedlak, I. ;
Kaminski, K. .
PHARMACEUTICAL RESEARCH, 2014, 31 (10) :2887-2903
[10]   The effect of Pluronic F127 on the physicochemical properties and dissolution profile of lovastatin solid dispersions [J].
Karolewicz, Bozena ;
Gajda, Maciej ;
Pluta, Janusz ;
Gorniak, Agata .
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY, 2016, 123 (03) :2283-2290