CHEMICAL ENGINEERING & TECHNOLOGY
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2018
·Vol. 41
·期 6
·1122-1131
·
IF 1.588
Ziyi Zhao,Guijin Liu,Qing Lin,Yanbin Jiang
Paracetamol (PCA) and trimethylglycine (TMG) were co-crystallized and micronized by means of the supercritical anti-solvent (SAS) process to improve the tabletability of PCA. The effects of operating conditions on particle properties were investigated in detail. Characterizations were performed to confirm the co-crystal state of PCA-TMG. The results indicated that the same crystal form with different crystal habits was prepared. The optimal PCA-TMG co-crystals presented a much larger tensile strength, higher drug content of PCA, and smaller particle size than those obtained using the ball milling (BM) process. The SAS-processed PCA-TMG co-crystals showed an enhanced solubility, dissolution rate, and tableting performance compared to that of BM.
研究领域:
药剂学
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材料科学
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产品关联
DOI
高影响因子
CRYSTAL GROWTH & DESIGN
·
2021
·
IF 4.076
Xinyuan Wang,Lei Wang,Changlin Yao,Guanying Xie,Shuhong Song,Huimin Li,Yaqian Qu,Xutang Tao
Recently, favipiravir, as a broad-spectrum antiviral drug, has gain more attention because it might be a candidate to remedy the coronavirus disease 2019 (COVID-19). To improve its poor permeability and tabletability, four multicomponent crystals of favipiravir (FPV) were prepared by a slow evaporation or liquid-assisted grinding method, including three cocrystals (FPV-theophylline, 1:1; FPV-saccharin, 1:1; FPV-5-fluorouracil, 1:1) and one salt (FPV-piperazine, 2:1). All of the crystal structures were solved by single-crystal X-ray diffraction. Interestingly, FPV-theophylline has a crystal structure similar to that of FPV, leading to similar properties, such as solubility, permeability, and tabletability. Except for FPV-theophylline, all of the other multicomponent crystals exhibit an enhanced permeability and tabletability. Our studies provide a new insight in overcoming the shortcomings of the important antiviral drug FPV.
研究领域:
药学
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材料科学
·
化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Huiling Zhou,Chenxin Duan,Huimin Qin,Chaonan Huang,Jingxuan Hou,Yanming Chen,Jin Zhu,Cangcang Xu,Jian Jin,Tao Zhuang
ABSTRACT Palbociclib (PAL), a highly selective inhibitor of cell cycle protein-dependent kinases (CDK) 4/6, is primarily used for treating advanced breast cancer. However, the use of PAL has been limited by its poor tabletability and dose-related toxic side effects. In this study, to improve the tabletability of PAL and reduce its effective dose, a flavonoid–kaempferol (KAE) was selected as the coformer to synthesize cocrystal with PAL. The novel cocrystal PAL-KAE was prepared by antisolvent cocrystallization and characterized by various techniques including X-ray diffraction (SCXRD and PXRD), thermal analysis (DSC and TG), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), Hirshfeld surface (HS), HOMO−LUMO analysis, and molecular electrostatic potential (MEP). Powder compaction experiments indicated that PAL-KAE cocrystal significantly improved the tabletability of PAL. The cytotoxicity test suggested that PAL-KAE also exerted synergistic antitumor effect against human ovarian cancer cell line OVCAR3 in MTT assay. Docking results indicated that PAL-KAE had lower binding energy with CDK 6 than PAL. Furthermore, the cocrystal PAL-KAE exhibits excellent stability in long-term testing, accelerated testing and stressing test. This paper provides a promising strategy for improving the tabletability of PAL and enhancing its anticancer activity, thus reducing the dose-related side effects of PAL.
研究领域:
药学
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材料科学
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癌症研究
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药物递送
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
IF 5.3
Yanbo Liu,Xiaolei Wang,Chenyang Zhao,Shuo Wang,Xiaogang Lian,Weiqi Chen,Lei He,Mingyang Chen,Songgu Wu,Junbo Gong
Tenofovir amibufenamide fumarate (TMF) is the first oral drug developed in Asia for the treatment of adult patients with chronic viral hepatitis B, however, further applications are limited by poor tableting performance and high sticking propensity. In this work, the spherulitic growth process of TMF has been designed and explored with the help of molecular dynamics simulation and process analysis technologies (ATR-FTIR, FBRM and EasyViewer). The spherical particles with high bulk density, good flowability and uniform particle size distribution are prepared by a simple quenching process. More importantly, experimental results show that spherical particles have higher average tensile strength (100.8% increase), higher plastic deformability and lower amount of punch sticking (87.4% decrease in 30 tablets) compared to the commercial powder products. These contributions not only shed light on the design principle of drug spherulitic growth processes, but also provide guidance for the manufacture of high-quality tablet products.
研究领域:
药学
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结晶工程
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材料科学
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药物开发
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）