Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution
Publication type: Journal Article
Publication date: 2018-07-02
scimago Q2
wos Q1
SJR: 0.633
CiteScore: 5.6
Impact factor: 3.4
ISSN: 15287483, 15287505
General Chemistry
Condensed Matter Physics
General Materials Science
Abstract
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 p...
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Total citations:
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Citations from 2024:
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(6.9%)
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GOST
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Zhu B. et al. Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution // Crystal Growth and Design. 2018. Vol. 18. No. 8. pp. 4701-4714.
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Jianrong Wang J. W., Zhang Q., Li M., Mei X. Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution // Crystal Growth and Design. 2018. Vol. 18. No. 8. pp. 4701-4714.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acs.cgd.8b00684
UR - https://doi.org/10.1021/acs.cgd.8b00684
TI - Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution
T2 - Crystal Growth and Design
AU - Jianrong Wang, Jianrong Wang
AU - Zhang, Qi
AU - Li, Meiqi
AU - Mei, Xuefeng
PY - 2018
DA - 2018/07/02
PB - American Chemical Society (ACS)
SP - 4701-4714
IS - 8
VL - 18
SN - 1528-7483
SN - 1528-7505
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2018_Zhu,
author = {Jianrong Wang Jianrong Wang and Qi Zhang and Meiqi Li and Xuefeng Mei},
title = {Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution},
journal = {Crystal Growth and Design},
year = {2018},
volume = {18},
publisher = {American Chemical Society (ACS)},
month = {jul},
url = {https://doi.org/10.1021/acs.cgd.8b00684},
number = {8},
pages = {4701--4714},
doi = {10.1021/acs.cgd.8b00684}
}
Cite this
MLA
Copy
Zhu, Bin, et al. “Stable Cocrystals and Salts of the Antineoplastic Drug Apatinib with Improved Solubility in Aqueous Solution.” Crystal Growth and Design, vol. 18, no. 8, Jul. 2018, pp. 4701-4714. https://doi.org/10.1021/acs.cgd.8b00684.