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Solubility and Permeability Improvement of Allopurinol by Cocrystallization

机译：通过COCRYALIZ化的溶解性和渗透性改善Allopurinol

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摘要

Allopurinol is a xanthine oxidase inhibitor with poor solubility and permeability, which severely limit its drug absorption following the administration of some dosage forms, such as tablets and rectal suppositories. To improve the physicochemical properties, three cocrystals of allopurinol with isonicotinamide (ALP-INA), piperazine (ALP-PIP), and 2,4-dihydroxybenzoic acid (ALP-24DHBZA) were successfully prepared by a slurry or liquid-assisted grinding method. The obtained cocrystal materials were characterized by single-crystal X-ray diffraction, powder X-ray diffraction, infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analyses and were subjected to dynamic vapor sorption, dissolution, and membrane permeability studies. ALP-INA showed solubility and diffusion/membrane permeability similar to those of the parent drug. In contrast, ALP-PIP exhibited improved diffusion/membrane permeability, and ALP-24DHBZA exhibited improved dissolution behavior, respectively. These results suggest that ALP-PIP and ALP-24DHBZA have the potential to be developed as new, more efficient formulations of allopurinol.
机译：Allopurinol是一种溶解性和渗透性差的黄嘌呤氧化酶抑制剂，其在给予某种剂型（例如片剂和直肠栓剂）后严重限制其药物吸收。为了改善物理化学性质，通过浆料或液体辅助研磨方法成功制备了用异种酸（Alp-Ina），哌嗪（ALP-PIP），哌嗪（ALP-PIP），哌嗪（ALP-PIP）和2,4-二羟基苯甲酸（ALP-24dhbza）的三个聚晶醇。通过单晶X射线衍射，粉末X射线衍射，红外光谱，差示扫描量热法和热重分析，并进行动态蒸汽吸附，溶解和膜渗透性研究。 ALP-INA显示出与母体药物类似的溶解度和扩散/膜渗透性。相反，ALP-PIP表现出改善的扩散/膜渗透性，ALP-24DHBZA分别表现出改善的溶解行为。这些结果表明ALP-PIP和ALP-24DHBZA有可能开发为新嘌呤醇的新的，更有效的配方。

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  • 来源
    《Crystal growth & design》 |2020年第8期|共9页
  • 作者

    Dai Xia-Lin; Yao Jia; Wu Chao; Deng Jun-Hui; Mo Yong-Hui; Lu Tong-Bu; Chen Jia-Mei;

  • 作者单位

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Peoples R China;

    Tianjin Univ Technol Sch Chem &

    Chem Engn Tianjin Key Lab Drug Targeting &

    Bioimaging Tianjin 300384 Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Peoples R China;

    Tianjin Univ Technol Sch Mat Sci &

    Engn Inst New Energy Mat &

    Low Carbon Technol Tianjin 300384 Peoples R China;

    Tianjin Univ Technol Sch Chem &

    Chem Engn Tianjin Key Lab Drug Targeting &

    Bioimaging Tianjin 300384 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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