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首页> 外文期刊>Crystal growth & design >Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution
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Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution

机译：稳定的抗肿瘤药物Apatinib的稳定的聚碳酸盐和盐水溶液中的溶解度提高

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摘要

Apatinib (APA) belongs to the targeted antineoplastic family of drugs by inhibiting the vascular endothelial cell growth factor receptor (VEGFR-2) of tyrosine kinase. APA encounters poor aqueous solubility problems, and its therapeutic dosage form, apatinib mesylate (ATM), is unstable and dissociates completely to APA in aqueous solution. Here, we synthesized and evaluated three new cocrystals of APA with adipic acid (APA + ADA), sebacic acid (APA + SEA), and D/L-mandelic acid (APA + D/L-MA), and four new salts with succinic acid (APA + SUA-H2O), salicylic acid (APA + SA), 1-hydroxy-2-naphthoic acid (APA + HNA), and saccharin (APA + SAC). All the solid forms were characterized by powder X-ray diffraction, infrared spectroscopy, differential scanning calorimetry, and dynamic vapor sorption. The molecular components and structures were confirmed by single crystal X-ray diffraction. APA + SEA is able to overcome the instability problem and has improved solubility compared with ATM. Hence, APA + SEA has the potential to be a superior candidate for this important drug.
机译：apatinib（APA）通过抑制血管内皮细胞生长因子受体（VEGFR-2）的酪氨酸激酶，属于靶向抗肿瘤家族。 APA遇到差的水溶性问题，其治疗剂型apatinib甲磺酸盐（ATM）是不稳定的，并在水溶液中完全解离。在此，我们用己二酸（APA + ADA），癸二酸（APA +海）和D / L-扁桃酸（APA + D / L-MA）合成并评估了三种新的APA的新酰基，以及四种新盐琥珀酸（APA + SU-H 2 O），水杨酸（APA + SA），1-羟基-2-萘甲酸（APA + HNA）和糖精（APA + SAC）。所有固体形式的特征在于粉末X射线衍射，红外光谱，差示扫描量热法和动态蒸汽吸附。通过单晶X射线衍射确认分子量和结构。 APA + SEA能够克服不稳定的问题，与ATM相比，改善了溶解度。因此，APA +海有可能成为这一重要药物的优越候选者。

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  • 来源
    《Crystal growth & design》 |2018年第8期|共14页
  • 作者

    Zhu Bin; Wang Jian-Rong; Zhang Qi; Li Meiqi; Guo Chunyang; Ren Guobin; Mei Xuefeng;

  • 作者单位

    East China Univ Sci &

    Technol Lab Pharmaceut Crystal Engn &

    Technol Sch Pharm Shanghai 200237 Peoples R China;

    Chinese Acad Sci Pharmaceut Analyt &

    Solid State Chem Res Ctr Shanghai Inst Mat Med Shanghai 201203 Peoples R China;

    Chinese Acad Sci Pharmaceut Analyt &

    Solid State Chem Res Ctr Shanghai Inst Mat Med Shanghai 201203 Peoples R China;

    Chinese Acad Sci Pharmaceut Analyt &

    Solid State Chem Res Ctr Shanghai Inst Mat Med Shanghai 201203 Peoples R China;

    East China Univ Sci &

    Technol Lab Pharmaceut Crystal Engn &

    Technol Sch Pharm Shanghai 200237 Peoples R China;

    East China Univ Sci &

    Technol Lab Pharmaceut Crystal Engn &

    Technol Sch Pharm Shanghai 200237 Peoples R China;

    Chinese Acad Sci Pharmaceut Analyt &

    Solid State Chem Res Ctr Shanghai Inst Mat Med Shanghai 201203 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
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