生物-A联合晶体配方改善了生物可用性,并通过减轻炎症来改善素诱导的胰腺炎
Hari Priya Sripadi1, Rajwinder Kaur1, Saylee Manohar Koli2
1Department of Applied Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, Telangana, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh 201 002, India.
International journal of pharmaceutics
|November 3, 2024
概括
一种新型的生物氨酸A-尼古丁胺合晶 (BCC) 显著改善了口服生物可用性,并治疗急性胰腺炎. 这种共晶增强了溶解性,减少了炎症,提供了一个有前途的治疗方法.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 药用化学 医学化学
背景情况:
- 生物素A (BCA),一种黄类,具有药用潜力,但由于溶解性差和口服生物利用性低,因此受到阻碍.
- 同结晶是一种提高活性药物成分 (API) 物理化学和药物动力学特性的策略.
研究的目的:
- 设计和开发一种新的Biochanin A-尼古丁胺胺共晶体 (BCC),以提高BCA的口服生物利用性.
- 探索BCC的治疗潜力,以改善素诱导的急性胰腺炎 (CIAP).
- 通过组织/血清代谢物概况识别治疗点.
主要方法:
- 使用超分子合成方法的晶设计.
- 通过单晶X射线衍射,FT-IR和DSC进行表征.
- 在Cerulein诱导的急性胰腺炎 (CIAP) 模型中进行评估,包括使用Orbitrap Exploris质谱仪进行代谢分析.
主要成果:
- 与BCA相比,BCC共晶体表现出一个强大的3D结网络,增强的溶解度和改善的药物释放.
- BCC显著提高了口服生物可用性和胰腺组织度.
- BCC疗法显著降低了CIAP,减少了炎症,状细胞缩,粉酶水平,氧化应激和炎症标志物.
结论:
- 开发的BCC共晶是一种有前途的方法来增强Biochanin A的治疗潜力.
- 通过调节炎症和氧化应激,BCC有效地改善素诱导的急性胰腺炎.
- 代谢分析识别了AP的独特特征,可能有助于开发诊断工具.
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