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Quantification of flupirtine maleate polymorphs using X-ray powder diffraction

Chinese Chemical Letters 2016年第11期27卷 1666-1672页

作者： Yu-Mei Zhao zhi-bing zheng Song Li Laboratory of Computer-Aided Drug Design & Discovery Beijing Institute of Pharmacology and Toxicology Laboratory of Structure Identification Beijing Institute of Pharmacology and Toxicology State Key Laboratory of Toxicology and Medical Countermeasures Beijing Institute of Pharmacology and Toxicology

Flupirtine maleate, a pharmaceutical compound for treating psychotic disease in clinics, has seven polymorphs. Form A, with better crystal stability and bioavailability, has been widely used as the pharmaceutical crystal form. Unfortunately, it is usually found in a polymorphic mixture with form B. In this study, pure crystal forms of A and B were prepared and characterized by X-ray powder diffraction （XRPD）, Fourier transform infrared spectroscopy （FT-IR） and thermal analysis. An XRPD-based method for the quantitative determination of the amount of the flupirtine maleate polymorphs form A and form B was also established through a systematic optimization of instrumental parameters. The results of the analytical methodology validation showed that the XPRD method had a broad quantitative range of 0- 100% （w/w）, good linear relationship, with R2= 0.999, excellent repeatability and precision and low limits of detection （LoD） of 0.15% （w/w） and quantification （LoQ） of 0.5% （w/w）. The results also showed that the single-peak method was not as good as the whole pattern in reducing the influence of the preferred orientation, but this can be compensated for by a systematic optimization of instrumental parameters and validating the analytical methodology to reduce errors and obtain a good, repeatable, sensitive, and accurate method. This XRPD method can be used to analyze mixtures of flupirtine maleate polymorphs （forms A and B） quantitatively and control the quality of the bulk drug.

关键词： Flupirtine maleate X-ray powder diffraction Quantitative analysis of polymorphs Preferred orientation Transmission

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Influence of carbon addition on mechanical properties of Fe-Mn-C twinning-induced plasticity steels

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Journal of Iron and Steel Research International 2022年第9期29卷 1446-1454页

作者： Peng Fu zhi-bing zheng Wei-ping Yang Hao-kun Yang School of Engineering Jiangxi Agricultural UniversityNanchang 330045JiangxiChina Institute of New Materials GuangdongAcademy of SciencesGuangdong Provincial iron Matrix Composite Engineering Research CenterGuangzhou 510650GuangdongChina Smart Manufacturing Division Hong Kong Productivity CouncilHong Kong 999077.China

Mechanical properties and microstructural evolution of Fe-22Mn-0.6C and Fe-22Mn-1.0C(wt.%)twinning-induced plasticity(TwIP)steels were investigated by monotonic,stress-relaxation and unloading-reloading tensile *** dynamic strain aging(DSA)effect,resulting from pinning of dislocations,effectively improved the dislocation activation volume of the two TWIP *** the meanwhile,DSA-facilitated twinning nucleation mechanism kept similar twinning capabilities of the two TWIP *** strain increasing,the formation of high-density deformation twins restricted the dislocation motion and reduced the activation volume with increasing ***,C addition simultaneously improved the ultimate tensile strength and uniform elongation,and significantly enhanced the friction stress,rather than back *** stronger short-range order effect,brought by friction stress,promotes the planar dislocation slipping,thus improving the work-hardening *** a result,the additional work-hardening capacity can be achieved in Fe-Mn-C with higher C addition.

关键词： Twinning induced plasticity steel Work-hardening rate Dynamic strain aging Short-range order Deformation twin

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Synthesis and Biological Evaluation of Novel 1, 5-Diarylpyrazole-3- carboxamide Compounds as Inhibitors of ALK5

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Chinese Chemical Letters 2006年第5期17卷 609-612页

作者： Xian Ping DAI Xing Zhou LI zhi bing zheng Song LI School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 Beijing Institute of Pharmacology ＆ Toxicology Beijing 100850

Ten new 1, 5-diarulpyrazole-3-carboxamide compounds were synthesized and their structures were identified by ^1H-NMR and FAB-MS. The primary biological tests showed that compound 4j exhibited some ALK5 inhibitory acti... 详细信息

关键词： 1,5-Diarylpyrazole-3-carboxamide synthesis inhibitors ALK5.

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Synthesis of 2-(Benzodioxol-2-yl)acetic Acids as PPARδAgonists

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Chinese Chemical Letters 2006年第8期17卷 1013-1016页

作者： Jian Lei KANG zhi bing zheng Dan QIN Li Li WANG Song LI School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Beijing 100850

A new series of compounds, 2-（benzodioxol-2-yl）acetic acids, have been synthesized. Their structures were confirmed by MS and 1H-NMR. The preliminary pharmacological screening showed that these compounds exhibited p... 详细信息

关键词： PPARδ agonists 2-(benzodioxol-2-yl)acetic acids synthesis.

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Synthesis of a new series of anti-rhinovirus compounds

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Chinese Chemical Letters 2007年第4期18卷 400-402页

作者： Shi Yong Fan Chun Lai Mi Jun Yang Song Li zhi bing zheng Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Beijing 100850 China School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

The synthesis of a series of 3,6-dichloropyridazine derivatives was described. In vitro experiment, all compounds exhibited an anti-rhinovirus activity, and one of the compounds 6g showed the comparable activity as ou... 详细信息

关键词： 3,6-Dichoropyridazine derivatives Synthesis Anti-rhinovirus

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Synthesis of Tritium and Deuterium Labelled Agmatine

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Chinese Chemical Letters 2006年第5期17卷 587-590页

作者： Hong Xia HE zhi bing zheng Lan Fu CHEN Zhan Bin ZHANG Chun HU Song LI Shenyang Pharmaceutical University Shenyang 110016 Beijing Institute of Pharmacology and Toxicology Beijing 100850 Beijing Normal University Beijing 100875

An efficient procedure for the synthesis of agmatine labelled with tritium and deuterium is reported. The final tritiated product 4 was obtained with a specific activity of 40 Ci/mmol and a radiochemical purity of 95%.

关键词： Agmatine labelled compound synthesis deuterium tritium.

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Synthesis and biological evaluation of novel 2,4,5-triaryl-1 H-pyrazol-3(2H)-ones as inhibitors of ALK5

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Chinese Chemical Letters 2008年第4期19卷 379-382页

作者： Xing Zhou Li Xian Ping Dai Kang Ying Lai Li Li Wang zhi bing zheng Song Li Beijing Institute of Pharmacology ＆ Toxicology Beijing 100850 China School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

A series of 2,4,5-triaryl substituted 1H-pyrazol-3（2H）-ones,as ALK5 inhibitors,were desigened,synthesized and evaluated in *** compounds exhibited noticeable ALK5 inhibition activities at 1μmol/L and displayed no s... 详细信息

关键词： Activin-like kinases5(ALK5) Kinase inhibitors 1H-Pyrazol-3(2H)-ones

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Synthesis of 1-aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas as TNF-αinhibitors

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Chinese Chemical Letters 2007年第8期18卷 905-908页

作者： Xin Ming Zhou zhi bing zheng Hong Ying Liu Wu Zhong Jun Hai Xiao Li Li Wang Song Li Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Beijing 100850 China School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

A new series of compounds, 1-aryl-3-（3,4-dihydro-2H-chromen-5-yl） ureas, have been synthesized and their structures were confirmed by FAB-MS and IH NMR. The preliminary pharmacological screening showed that these co... 详细信息

关键词： p38 MAPK inhibitor l-Aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas Synthesis

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Synthesis of aromatic-linked polyamine macrocyclic derivatives as HIV-1 entry inhibitors

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Chinese Chemical Letters 2007年第10期18卷 1166-1168页

作者： Jing Su Yao Liu zhi bing zheng Jun Hai Xiao Hong Lu Wu Zhong Li Li Wang Shi Bo Jiang Song Li School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China School of Pharmacy Jilin University Changchun 13002-1 China Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Beijing 100850 China Lindsley E Kimball Research Institute the New York Blood Center New York NY 10021 USA

A series of novel aromatic-linked polyamine macrocyclic derivatives have been synthesized. Their structures were confirmed by MS and ^1H NMR. These compounds exhibited potent anti-HIV-1 activities.

关键词： HIV-1 entry inhibitors Aromatic-linked polyamine Macrocyclic derivatives Synthesis

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Admittance spectroscopy characterize graphite paste for back contact of CdTe thin film solar cells

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Science China(Technological Sciences) 2010年第9期53卷 2337-2341页

作者： HE XuLin,ZHANG JingQuan,FENG LiangHuan,WU LiLi,LI Wei,ZENG GuangGen,LEI zhi,LI bing & zheng JiaGui College of Materials Science and Engineering,Sichuan University,Chengdu 610064,China College of Materials Science and Engineering Sichuan University

CdTe thin film solar cells with a doped-graphite paste back contact layer were studied using admittance spectroscopy *** positions and the capture cross sections of energy level in the forbidden band were calculated,which are the important parameters to affect solar cell *** results showed that there were three defects in the CdTe thin films solar cells with the doped-graphite paste back contact layer,whose positions in the forbidden band were close to 0.34,0.46 and 0.51 eV,respectively above the valence band,and capture cross sections were 2.23×10-16,2.41×10-14,4.38×10-13 cm2,respectively.

关键词： CdTe solar cells admittance spectroscopy deep-level defect

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