第二代H1受体对手药物Bilastine的多组分形式及其增强的物理化学特性
Ananya Kar1, Lopamudra Giri2, Gowtham Kenguva1
1Department of Industrial and Engineering Chemistry, Institute of Chemical Technology-Indian Oil Bhubaneswar Campus, Bhubaneswar, India.
Bioorganic chemistry
|July 28, 2024
概括
研究人员通过创建像BIL.TA.HYD.这样的分子添加物来增强比拉斯 (BIL) 的溶解性和透性. 这些稳定的添加物显示出更好的溶解和扩散,为新的比拉斯配方铺平了道路.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药用化学 医学化学
背景情况:
- 比拉斯丁 (BIL) 是第二代抗组胺药,有效治疗慢性疹和过敏性鼻炎.
- 比尔的水溶性较差限制了其治疗潜力和配方开发.
- 开发新的BIL配方需要增强其物理化学性质.
研究的目的:
- 通过形成分子添加物来增强比拉斯 (BIL) 的物理化学特性.
- 研究新型BIL添加物的结构性,热性,溶解性和稳定性特性.
- 评估这些诱导物对改善药物输送的潜力.
主要方法:
- 合成BIL分子添加物 (盐,水合物,共晶体) 使用铁酸,2,4-二基酸,香草酸,氨酸和希普酸.
- 使用粉末X射线衍射 (PXRD),单晶X射线衍射 (SCXRD),热重力测量分析 (TGA) 和差分扫描热量测量 (DSC) 的表征.
- 在体外溶解性,溶解率,流通性和扩散性研究;在受控湿度和温度下的稳定性评估.
主要成果:
- SCXRD证实了通过联结稳定的固态结构.
- 大多数合成的BIL添加物与纯BIL相比,具有显著更高的溶解度和溶解率.
- BIL.TA.HYD显示出最高的可溶性和溶解率;BIL.TA.HYD和BIL.VA显示出增强的透性和扩散性.
- 所有合成的分子添加物在测试条件下都被发现是稳定的.
结论:
- 毕拉斯的新型分子添加物已成功合成和表征.
- 这些添加物的可溶性,溶解性和透性提高为开发先进的BIL配方提供了显著的优势.
- 这些发现支持分子添加物的潜力,以克服比拉斯等溶解不良药物的局限性.
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