DSC and physico-chemical properties of a substituted pyridoquinoline and its interaction study with excipients

被引:26
作者
Abbas, D. [1 ]
Kaloustian, J. [2 ]
Orneto, C. [1 ]
Piccerelle, P. [1 ]
Portugal, H. [2 ]
Nicolay, A. [2 ]
机构
[1] Univ Aix Marseille 2, Fac Pharm, INSERM, Lab Pharm Galen Pharmacotech Ind Biopharm & Cosme, F-13385 Marseille 05, France
[2] Univ Aix Marseille 2, Fac Pharm, INSERM, UMR 476,INRA 1260,Lab Chim Analyt, F-13385 Marseille, France
关键词
BG; 637; DSC; excipients; interactions; physico-chemical properties; stability;
D O I
10.1007/s10973-008-9062-7
中图分类号
O414.1 [热力学];
学科分类号
摘要
The 4,6-bis[2'(diethylamino)ethoxy]2,8,10-trimethylpyrido[3,2-g] quinoline (BG 637) is one of the compound from the pyrido[3,2-g] quinolines family. This compound had in vitro activity against the resistant cells and can reverse the multidrug resistance developed during the chemotherapeutic treatments. To characterize BG 637, techniques such as differential scanning calorimetry (DSC), Fourier transform infrared spectrometer (FTIR), ultra violet spectrophotometry (UV), gas chromatography coupled with mass spectrometry (GC/MS), nuclear magnetic resonance (NMR) and X-ray powder diffraction (XRPD) were used. Several of them were also used to show the stability of the drug during various storage conditions. DSC, FTIR and UV were used as screening techniques for assessing the compatibility of BG 637 with several commonly used pharmaceutical excipients. We compared the properties of the pure drug with those of binary mixture drug/excipient. Studied excipients were lactose monohydrate, microcrystalline cellulose, polyvinylpyrrolidone, sodium croscarmellose and magnesium stearate. Melting temperature and enthalpy of BG 637 in binary mixtures were similar to theoretical values. These results showed that BG 637 is a very stable compound and compatible with several pharmaceutical excipients.
引用
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页码:353 / 360
页数:8
相关论文
共 31 条
[1]  
ABOUTALEB AE, 1983, PHARMAZIE, V38, P473
[2]   Thermal analysis of the antiretroviral zidovudine (AZT) and evaluation of the compatibility with excipients used in solid dosage forms [J].
Araújo, AAS ;
Storpirtis, S ;
Mercuri, LP ;
Carvalho, FMS ;
dos Santos, M ;
Matos, JR .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 260 (02) :303-314
[3]   Thermal analyses of commercial magnesium stearate pseudopolymorphs [J].
Bracconi, P ;
Andrès, C ;
N'diaye, A ;
Pourcelot, Y .
THERMOCHIMICA ACTA, 2005, 429 (01) :43-51
[4]   Structural properties of magnesium stearate pseudopolymorphs:: effect of temperature [J].
Bracconi, P ;
Andrès, C ;
Ndiaye, A .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 262 (1-2) :109-124
[5]   PHYSICAL CHARACTERIZATION OF PHARMACEUTICAL SOLIDS [J].
BRITTAIN, HG ;
BOGDANOWICH, SJ ;
BUGAY, DE ;
DEVINCENTIS, J ;
LEWEN, G ;
NEWMAN, AW .
PHARMACEUTICAL RESEARCH, 1991, 8 (08) :963-973
[6]   PHARMACEUTICAL SOLIDS - A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS [J].
BYRN, S ;
PFEIFFER, R ;
GANEY, M ;
HOIBERG, C ;
POOCHIKIAN, G .
PHARMACEUTICAL RESEARCH, 1995, 12 (07) :945-954
[7]  
CHOWHAN ZT, 1993, PHAMR TECH, V17, P72
[8]  
*COUNC EUR, 2008, EDQM EUR DIR QUAL ME
[9]  
Crowley P, 2001, PHARM TECHNOL EUR, V13, P34
[10]  
Crowley P., 2001, PHARM TECHNOL, V13, P26