Cryochemically Obtained Nanoforms of Antimicrobial Drug Substance Dioxidine and Their Physico-chemical and Structural Properties

被引:14
|
作者
Shabatina, Tatyana I. [1 ,2 ]
Vernaya, Olga I. [1 ]
Shabatin, Vladimir P. [1 ]
Evseeva, Iuliia V. [1 ,2 ]
Melnikov, Michail Ya [1 ]
Fitch, Andrew N. [3 ]
Chernyshev, Vladimir V. [1 ,4 ]
机构
[1] Moscow MV Lomonosov State Univ, Dept Chem, Leninskie Gori Build 1-3, Moscow 119991, Russia
[2] Bauman Moscow State Tech Univ, 2nd Bauman Str 5, Moscow 105905, Russia
[3] European Synchrotron Radiat Fac, BP 220, F-38043 Grenoble, France
[4] RAS, Frumkin Inst Phys Chem & Electrochem, Leninskii Prospect 31, Moscow 119071, Russia
来源
CRYSTALS | 2018年 / 8卷 / 07期
基金
俄罗斯科学基金会;
关键词
drug nanoforms; cryochemical synthesis; polymorphism; antimicrobial substances; dioxidine; POORLY SOLUBLE DRUGS; ANTIBACTERIAL ACTIVITY; PREFERRED ORIENTATION; ORAL BIOAVAILABILITY; RIETVELD REFINEMENT; POWDER DATA; UNIT-CELL; NANOCRYSTALS; DELIVERY; POLYMORPHS;
D O I
10.3390/cryst8070298
中图分类号
O7 [晶体学];
学科分类号
0702 ; 070205 ; 0703 ; 080501 ;
摘要
Nanoforms of the antimicrobial drug substance 2,3-bis-(hydroxymethyl) quinoxaline-N,N-dioxide with particles sizes between 50 and 300 nm were obtained by cryochemical modification of the initial pharmaceutical substance using a freeze-drying technique and were characterized by different physicochemical methods (FTIR, UV-Vis, H-1-NMR, DSC, TG and X-ray diffraction) and transmission electron microscopy (TEM). The data obtained from FTIR- and UV-Vis-spectroscopy confirmed the unaltered chemical structure of dioxidine molecules due to the cryochemical modification method. At the same time, X-ray diffraction and thermal analysis data show the change of the crystal structure compared to the parameters of the initial pharmaceutical dioxidine substance. A higher dissolution rate was revealed for cryomodified dioxidine nanoforms. The existence of three polymorphic crystal phases was established for cryomodified dioxidine samples possessed by some thermal activation processes: two anhydrous polymorphic phases, triclinic (T) and monoclinic (M), and one hydrated form (H).
引用
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页数:15
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