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新型抗松体1-(4-乙胺-二硫) - - 西米达的固体形式:制备和物理化学表征

Marina M Marcos Valdez¹, Octavio E Fandiño¹, Sonia N Faudone²

¹Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Ciencias Farmacéuticas y Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA-CONICET), Haya de la Torre y Medina Allende, (X5000HUA) Córdoba, Argentina.

Journal of pharmaceutical sciences

|September 16, 2023

概括

该研究确定了用于治疗夏加斯病的最稳定的1 - 4 - 乙胺 - 二硫 - 二硫 (PABZI) 晶体形式. 形式I表现出卓越的溶解性,溶解性和稳定性,使其成为进一步临床前开发的理想选择.

科学领域:

固态化学固态化学
制药科学制药科学
寄生虫学的寄生虫学

背景情况:

查加斯病是由Trypanosoma cruzi引起的,需要新的治疗药物.
1-(4-乙胺-二硫) -胺醇 (PABZI) 是一种新型化合物,具有显著的抗Trypanosoma cruzi活性.
了解PABZI的固态特性对于其制药开发至关重要.

研究的目的:

为了研究1-(4-乙胺-二硫) -胺醇 (PABZI) 的多态性.
为了描述PABZI的不同晶体形式.
评估关键PABZI形式的物理化学特性和固态稳定性,用于临床前选择.

主要方法:

分离和表征PABZI的三个晶体形式.
单晶X射线衍射用于晶体结构的确定形式I.
评估可溶性,溶解率,可湿性和固态稳定性 (水分和光).

主要成果:

分离了三种不同的晶体形式的PABZI:一种无溶剂形式 (I形式) 和两种类型的溶酸盐.
与异醇溶酸盐 (PABZI-isoOH) 相比,I型具有更高的可溶性和溶解率.
形式I在湿度和UV-可见光暴露下表现出优异的固态稳定性.

结论:

多态性显著影响PABZI的物理化学性质.
形式I,无溶剂的晶体形式,由于其增强的特性,是进一步临床前研究的最有前途的候选人.
选择Form I支持PABZI作为查加斯病的潜在治疗剂的发展.

关键词:

聚合聚合聚合聚合聚合查加斯病是查加斯病的一种疾病.固态稳定性的稳定性索尔瓦特是一种溶解物.热分析是一种热分析.在X射线衍光度测试中使用X射线衍光度计.

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